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Pesquisa : D02.886.778.823 [Categoria DeCS]
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[PMID]:29337675
[Au] Autor:Hafez HN; El-Gazzar ABA
[Ad] Endereço:1Al-Imam Mohammad Ibn Saud Islamic University (IMSIU) Faculty of Science Department of Chemistry P. O. Box 90950, Riyadh 11623 Kingdom of Saudi Arabia.
[Ti] Título:Synthesis and evaluation of antitumor activity of new 4-substituted thieno[3,2-d]pyrimidine and thienotriazolopyrimidine derivatives.
[So] Source:Acta Pharm;67(4):527-542, 2017 Dec 20.
[Is] ISSN:1846-9558
[Cp] País de publicação:Croatia
[La] Idioma:eng
[Ab] Resumo:3-Methyl-6-phenyl-2-thioxo-2,3-dihydrothieno[3,2-d]pyrimidin- 4(1H)-one (2), on treatment with phosphorous oxychoride, affored 4-chloro-3-methyl-6-phenyl -thieno[3,2-d]pyrimidine- 2(3H)-thione (3). A series of novel 6-phenyl-thieno[3,2-d]pyrimidine derivatives 4-9 bearing different functional groups were synthesized via treatment of compound 3 with different reagents. On the other hand, compound 2 was used to synthesize ethyl-[(3-methyl-6-phenyl-2-thioxo-2,3-dihydrothieno[ 3,2-d]pyrimidin-4-yl)-oxy]acetate (10), 2-hydrazinyl- -3-methyl-6-phenyl-thieno[3,2-d]pyrimidin-4(3H)-one (11), 3-methyl-2-(methyl-sulfanyl)-6-phenyl-thieno[3,2-d]pyrimidin- 4(3H)-one (12) and N-(phenyl)/4-chlorophenyl or methoxy- phenyl)-2-[(3-methyl-4-oxo-6-phenyl-3,4-dihydrothieno[ 3,2-d]pyrimidin-2-yl)-sulfanyl]-acetamide (13a-c). In addition, compound 12 was used to synthesize thieno[1,2,4] triazolopyrimidine derivatives 14 and 15 and 3-methyl-2-(methyl-sulfonyl)-6-phenyl-thieno[3,2-d]pyrimidin-4(3H)-one (16) through the reaction with the respective reagents. Moreover, the reaction of 16 with 4-phenylenediamine gave 2-[(4-aminophenyl)-amino]-3-methyl-6-phenyl-thieno[3,2-d] pyrimidin-4(3H)-one (17), which reacted with methanesulfonyl chloride to afford N-{4-[(3-methyl-4-oxo-6-phenyl-3H,4H- -thieno[3,2-d]pyrimidin-2-yl)-amino]phenyl}-methanesulfonamide (18). The majority of the newly synthesized compounds displayed potent anticancer activity, comparable to that of doxorubicin, on three human cancer cell lines, including the human breast adenocarcinoma cell line (MCF-7), cervical carcinoma cell line (HeLa) and colonic carcinoma cell line (HCT- 116). Compounds 18, 13b and 10 were nearly as active as doxorubicin whereas compounds 6, 7b and 15 exhibited marked growth inhibition, but still lower than doxorubicin.
[Mh] Termos MeSH primário: Antineoplásicos/síntese química
Tienopiridinas/síntese química
[Mh] Termos MeSH secundário: Adenocarcinoma/tratamento farmacológico
Antineoplásicos/farmacologia
Neoplasias da Mama/tratamento farmacológico
Carcinoma/tratamento farmacológico
Linhagem Celular Tumoral
Neoplasias do Colo/tratamento farmacológico
Feminino
Células HCT116/efeitos dos fármacos
Células HeLa/efeitos dos fármacos
Seres Humanos
Células MCF-7/efeitos dos fármacos
Tienopiridinas/farmacologia
Neoplasias do Colo do Útero/tratamento farmacológico
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Thienopyridines)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180131
[Lr] Data última revisão:
180131
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180117
[St] Status:MEDLINE


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[PMID]:28279968
[Au] Autor:Armstrong PC; Hoefer T; Knowles RB; Tucker AT; Hayman MA; Ferreira PM; Chan MV; Warner TD
[Ad] Endereço:From The William Harvey Research Institute, Barts & the London School of Medicine & Dentistry, Queen Mary University of London, Charterhouse Square, London, United Kingdom. p.c.armstrong@qmul.ac.uk.
[Ti] Título:Newly Formed Reticulated Platelets Undermine Pharmacokinetically Short-Lived Antiplatelet Therapies.
[So] Source:Arterioscler Thromb Vasc Biol;37(5):949-956, 2017 May.
[Is] ISSN:1524-4636
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:OBJECTIVE: Aspirin together with thienopyridine P2Y inhibitors, commonly clopidogrel, is a cornerstone of antiplatelet therapy. However, many patients receiving this therapy display high on-treatment platelet reactivity, which is a major therapeutic hurdle to the prevention of recurrent thrombotic events. The emergence of uninhibited platelets after thrombopoiesis has been proposed as a contributing factor to high on-treatment platelet reactivity. Here, we investigate the influences of platelet turnover on platelet aggregation in the face of different dual-antiplatelet therapy strategies. APPROACH AND RESULTS: Traditional light transmission aggregometry, cytometry, advanced flow cytometric imaging, and confocal microscopy were used to follow the interactions of populations of platelets from healthy volunteers and patients with stable cardiovascular disease. Newly formed, reticulated platelets overproportionately contributed to, and clustered at, the core of forming aggregates. This phenomenon was particularly observed in samples from patients treated with aspirin plus a thienopyridine, but was absent in samples taken from patients treated with aspirin plus ticagrelor. CONCLUSIONS: Reticulated platelets are more reactive than older platelets and act as seeds for the formation of platelet aggregates even in the presence of antiplatelet therapy. This is coherent with the emergence of an uninhibited subpopulation of reticulated platelets during treatment with aspirin plus thienopyridine, explained by the short pharmacokinetic half-lives of these drugs. This phenomenon is absent during treatment with ticagrelor, because of its longer half-life and ability to act as a circulating inhibitor. These data highlight the important influences of pharmacokinetics on antiplatelet drug efficacies, especially in diseases associated with increased platelet turnover.
[Mh] Termos MeSH primário: Adenosina/análogos & derivados
Aspirina/farmacocinética
Plaquetas/efeitos dos fármacos
Doença da Artéria Coronariana/tratamento farmacológico
Inibidores da Agregação de Plaquetas/farmacocinética
Antagonistas do Receptor Purinérgico P2Y/farmacocinética
Tienopiridinas/farmacocinética
Trombopoese
[Mh] Termos MeSH secundário: Adenosina/administração & dosagem
Adenosina/farmacocinética
Adolescente
Adulto
Idoso
Idoso de 80 Anos ou mais
Aspirina/administração & dosagem
Plaquetas/metabolismo
Estudos de Casos e Controles
Doença da Artéria Coronariana/sangue
Doença da Artéria Coronariana/diagnóstico
Quimioterapia Combinada
Meia-Vida
Seres Humanos
Masculino
Meia-Idade
Agregação Plaquetária/efeitos dos fármacos
Inibidores da Agregação de Plaquetas/administração & dosagem
Testes de Função Plaquetária
Antagonistas do Receptor Purinérgico P2Y/administração & dosagem
Antagonistas do Receptor Purinérgico P2Y/efeitos adversos
Tienopiridinas/administração & dosagem
Adulto Jovem
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Platelet Aggregation Inhibitors); 0 (Purinergic P2Y Receptor Antagonists); 0 (Thienopyridines); GLH0314RVC (Ticagrelor); K72T3FS567 (Adenosine); R16CO5Y76E (Aspirin)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170922
[Lr] Data última revisão:
170922
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170311
[St] Status:MEDLINE
[do] DOI:10.1161/ATVBAHA.116.308763


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[PMID]:28135086
[Au] Autor:Sundriyal S; Moniot S; Mahmud Z; Yao S; Di Fruscia P; Reynolds CR; Dexter DT; Sternberg MJ; Lam EW; Steegborn C; Fuchter MJ
[Ad] Endereço:Department of Chemistry, Imperial College London , London SW7 2AZ, U.K.
[Ti] Título:Thienopyrimidinone Based Sirtuin-2 (SIRT2)-Selective Inhibitors Bind in the Ligand Induced Selectivity Pocket.
[So] Source:J Med Chem;60(5):1928-1945, 2017 Mar 09.
[Is] ISSN:1520-4804
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Sirtuins (SIRTs) are NAD-dependent deacylases, known to be involved in a variety of pathophysiological processes and thus remain promising therapeutic targets for further validation. Previously, we reported a novel thienopyrimidinone SIRT2 inhibitor with good potency and excellent selectivity for SIRT2. Herein, we report an extensive SAR study of this chemical series and identify the key pharmacophoric elements and physiochemical properties that underpin the excellent activity observed. New analogues have been identified with submicromolar SIRT2 inhibtory activity and good to excellent SIRT2 subtype-selectivity. Importantly, we report a cocrystal structure of one of our compounds (29c) bound to SIRT2. This reveals our series to induce the formation of a previously reported selectivity pocket but to bind in an inverted fashion to what might be intuitively expected. We believe these findings will contribute significantly to an understanding of the mechanism of action of SIRT2 inhibitors and to the identification of refined, second generation inhibitors.
[Mh] Termos MeSH primário: Sirtuína 2/antagonistas & inibidores
Tienopiridinas/farmacologia
[Mh] Termos MeSH secundário: Sítios de Ligação
Cristalografia por Raios X
Ligantes
Simulação de Acoplamento Molecular
Relação Estrutura-Atividade
Tienopiridinas/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Ligands); 0 (Thienopyridines); EC 3.5.1.- (Sirtuin 2)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170922
[Lr] Data última revisão:
170922
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170131
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jmedchem.6b01690


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[PMID]:27575814
[Au] Autor:Soden PA; Zettervall SL; Ultee KH; Landon BE; O'Malley AJ; Goodney PP; DeMartino RR; Arya S; Schermerhorn ML; Society for Vascular Surgery Vascular Quality Initiative
[Ad] Endereço:Division of Vascular and Endovascular Surgery, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, Mass.
[Ti] Título:Dual antiplatelet therapy is associated with prolonged survival after lower extremity revascularization.
[So] Source:J Vasc Surg;64(6):1633-1644.e1, 2016 Dec.
[Is] ISSN:1097-6809
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Dual antiplatelet therapy (DAPT) after coronary stenting prolongs survival by preventing both in-stent thrombosis and other cardiovascular atherothrombotic events. Patients with peripheral artery disease (PAD) typically have a heavy burden of unrevascularized coronary artery disease and also stand to benefit from increased atherothrombotic protection with DAPT. The potential benefit of DAPT compared with aspirin alone in patients with PAD is not well described. METHODS: We identified all patients undergoing an initial elective lower extremity revascularization (bypass or endovascular) from 2003 to 2016 in the Vascular Quality Initiative registry discharged on aspirin or aspirin plus a thienopyridine antiplatelet agent (DAPT). We first estimated models predicting the likelihood of receiving DAPT and then used inverse probability weighting to account for baseline differences in the likelihood of receiving DAPT and compared late survival. For sensitivity analysis, we also performed Cox proportion hazard modeling on the unweighted cohorts and generated adjusted survival curves. RESULTS: We identified 57,041 patients undergoing lower extremity revascularization (28% bypass). Of 15,985 bypasses (69% for critical limb ischemia [CLI]), 38% were discharged on DAPT. Of 41,056 endovascular interventions (39% for CLI), 69% were discharged on DAPT. Analyses using inverse probability weighting demonstrated a small survival benefit to DAPT at 1 year for bypass (93% vs 92% [P = .001]) and endovascular interventions (93% vs 92% [P = .005]) that was sustained through 5 years of follow-up (bypass, 80% vs 78% [P = .004]; endovascular, 76% vs 73% [P = .002]). When stratified by severity of PAD, DAPT had a survival benefit for patients with CLI undergoing bypass (5 years, 70% vs 66% [P = .04]) and endovascular intervention (5 years, 71% vs 67% [P = .01]) but not for patients with claudication (bypass, 89% vs 88% [P = .36]; endovascular, 87% vs 85% [P = .46]). The protective effect of DAPT was similar when using Cox proportional hazard models after bypass (hazard ratio, 0.81 [95% confidence interval, 0.72-0.90]) and endovascular intervention (hazard ratio, 0.89 [95% confidence interval, 0.83-0.95]). CONCLUSIONS: DAPT at time of discharge was associated with prolonged survival for patients with CLI undergoing lower extremity revascularization but not for those with claudication. Further research is needed to quantify the risks associated with DAPT and to identify subgroups at increased risk of thrombotic and bleeding complications to guide medical management of patients with PAD.
[Mh] Termos MeSH primário: Aspirina/uso terapêutico
Claudicação Intermitente/cirurgia
Isquemia/cirurgia
Extremidade Inferior/irrigação sanguínea
Doença Arterial Periférica/cirurgia
Inibidores da Agregação de Plaquetas/uso terapêutico
Tienopiridinas/uso terapêutico
Procedimentos Cirúrgicos Vasculares/mortalidade
[Mh] Termos MeSH secundário: Idoso
Idoso de 80 Anos ou mais
Aspirina/efeitos adversos
Distribuição de Qui-Quadrado
Estado Terminal
Quimioterapia Combinada
Feminino
Seres Humanos
Claudicação Intermitente/diagnóstico por imagem
Claudicação Intermitente/mortalidade
Isquemia/diagnóstico por imagem
Isquemia/mortalidade
Masculino
Meia-Idade
Doença Arterial Periférica/diagnóstico por imagem
Doença Arterial Periférica/mortalidade
Inibidores da Agregação de Plaquetas/efeitos adversos
Modelos de Riscos Proporcionais
Sistema de Registros
Estudos Retrospectivos
Fatores de Risco
Índice de Gravidade de Doença
Tienopiridinas/efeitos adversos
Fatores de Tempo
Resultado do Tratamento
Estados Unidos
Procedimentos Cirúrgicos Vasculares/efeitos adversos
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Platelet Aggregation Inhibitors); 0 (Thienopyridines); R16CO5Y76E (Aspirin)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170515
[Lr] Data última revisão:
170515
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160831
[St] Status:MEDLINE


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[PMID]:27505343
[Au] Autor:Calogiuri GF; Al-Sowaidi S; Nettis E; Cortellini G; Macchia L; Vacca A; Kounis NG
[Ad] Endereço:Pneumology Department Civil Hospital "NinettoMelli"S. Pietro Vernotico, Brindisi, Italy; Section of Allergology and Clinical Immunology, Department of Internal Medicine, Immunology and Infectious Diseases, University of Bari Medical School, Bari, Italy. Electronic address: gf.calogiuri@libero.it.
[Ti] Título:A joint allergist/cardiologist classification for thienopyridines hypersensitivity reactions based on their symptomatic patterns and its impact on the management strategies.
[So] Source:Int J Cardiol;222:509-14, 2016 Nov 01.
[Is] ISSN:1874-1754
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:The role and importance of thienopyridines such as ticlopidine, clopidogrel, and prasugrel is well-established for several indications, ranging from prevention of acute coronary syndromes to percutaneous coronary interventions, where the dual antiplatelet therapy represents the gold standard to avoid denovo coronary stenosis. However, there is a significant cohort of patients with coronary artery disease who may manifest hypersensitivity reactions to thienopyridines. The examination of the various case reports from medical literature leads to identify mainly four clinical patterns of hypersensitivity to thienopyridines which involves more frequently cutaneous, hematologic, and articular tissues, therefore the kind and predominance of clinical symptoms may determine a different clinical approach to overcome or neutralize thienopyridines hypersensitivity.
[Mh] Termos MeSH primário: Alergistas
Cardiologistas
Gerenciamento Clínico
Hipersensibilidade a Drogas/classificação
Hipersensibilidade a Drogas/terapia
Tienopiridinas/classificação
[Mh] Termos MeSH secundário: Hipersensibilidade a Drogas/diagnóstico
Seres Humanos
Papel do Médico
Tienopiridinas/efeitos adversos
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Thienopyridines)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171003
[Lr] Data última revisão:
171003
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160810
[St] Status:MEDLINE


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[PMID]:27100112
[Au] Autor:Chandrasekhar J; Baber U; Mehran R; Aquino M; Sartori S; Yu J; Kini A; Sharma S; Skurk C; Shlofmitz RA; Witzenbichler B; Dangas G
[Ad] Endereço:Icahn School of Medicine at Mount Sinai, One Gustave L. Levy Place, PO Box 1030, New York, NY, USA.
[Ti] Título:Impact of an integrated treatment algorithm based on platelet function testing and clinical risk assessment: results of the TRIAGE Patients Undergoing Percutaneous Coronary Interventions To Improve Clinical Outcomes Through Optimal Platelet Inhibition study.
[So] Source:J Thromb Thrombolysis;42(2):186-96, 2016 Aug.
[Is] ISSN:1573-742X
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Assessment of platelet reactivity alone for thienopyridine selection with percutaneous coronary intervention (PCI) has not been associated with improved outcomes. In TRIAGE, a prospective multicenter observational pilot study we sought to evaluate the benefit of an integrated algorithm combining clinical risk and platelet function testing to select type of thienopyridine in patients undergoing PCI. Patients on chronic clopidogrel therapy underwent platelet function testing prior to PCI using the VerifyNow assay to determine high on treatment platelet reactivity (HTPR, ≥230 P2Y12 reactivity units or PRU). Based on both PRU and clinical (ischemic and bleeding) risks, patients were switched to prasugrel or continued on clopidogrel per the study algorithm. The primary endpoints were (i) 1-year major adverse cardiovascular events (MACE) composite of death, non-fatal myocardial infarction, or definite or probable stent thrombosis; and (ii) major bleeding, Bleeding Academic Research Consortium type 2, 3 or 5. Out of 318 clopidogrel treated patients with a mean age of 65.9 ± 9.8 years, HTPR was noted in 33.3 %. Ninety (28.0 %) patients overall were switched to prasugrel and 228 (72.0 %) continued clopidogrel. The prasugrel group had fewer smokers and more patients with heart failure. At 1-year MACE occurred in 4.4 % of majority HTPR patients on prasugrel versus 3.5 % of primarily non-HTPR patients on clopidogrel (p = 0.7). Major bleeding (5.6 vs 7.9 %, p = 0.47) was numerically higher with clopidogrel compared with prasugrel. Use of the study clinical risk algorithm for choice and intensity of thienopyridine prescription following PCI resulted in similar ischemic outcomes in HTPR patients receiving prasugrel and primarily non-HTPR patients on clopidogrel without an untoward increase in bleeding with prasugrel. However, the study was prematurely terminated and these findings are therefore hypothesis generating.
[Mh] Termos MeSH primário: Tomada de Decisão Clínica/métodos
Intervenção Coronária Percutânea/métodos
Tienopiridinas/uso terapêutico
[Mh] Termos MeSH secundário: Idoso
Algoritmos
Hemorragia/induzido quimicamente
Seres Humanos
Meia-Idade
Inibidores da Agregação de Plaquetas/uso terapêutico
Testes de Função Plaquetária/utilização
Cloridrato de Prasugrel/uso terapêutico
Estudos Prospectivos
Medição de Risco/métodos
Ticlopidina/análogos & derivados
Ticlopidina/uso terapêutico
Resultado do Tratamento
[Pt] Tipo de publicação:JOURNAL ARTICLE; MULTICENTER STUDY; OBSERVATIONAL STUDY
[Nm] Nome de substância:
0 (Platelet Aggregation Inhibitors); 0 (Thienopyridines); A74586SNO7 (clopidogrel); G89JQ59I13 (Prasugrel Hydrochloride); OM90ZUW7M1 (Ticlopidine)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:171101
[Lr] Data última revisão:
171101
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160422
[St] Status:MEDLINE
[do] DOI:10.1007/s11239-016-1357-0


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[PMID]:26853836
[Au] Autor:Leung E; Pilkington LI; van Rensburg M; Jeon CY; Song M; Arabshahi HJ; De Zoysa GH; Sarojini V; Denny WA; Reynisson J; Barker D
[Ad] Endereço:Auckland Cancer Society Research Centre, The University of Auckland, New Zealand; Department of Molecular Medicine and Pathology, The University of Auckland, New Zealand. Electronic address: e.leung@auckland.ac.nz.
[Ti] Título:Synthesis and cytotoxicity of thieno[2,3-b]quinoline-2-carboxamide and cycloalkyl[b]thieno[3,2-e]pyridine-2-carboxamide derivatives.
[So] Source:Bioorg Med Chem;24(5):1142-54, 2016 Mar 01.
[Is] ISSN:1464-3391
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Seventy nine derivatives of thieno[2,3-b]quinolines, tetrahydrothieno[2,3-b]quinoline, dihydrocyclopenta[b]thieno[3,2-e]pyridine, cyclohepta[b]thieno[3,2-e]pyridine and hexahydrocycloocta[b]thieno[3,2-e]pyridine were either synthesized or obtained commercially and tested for their antiproliferative activity against HCT116, MDA-MB-468 and MDA-MB-231 human cancer cell lines. The most potent eight compounds were active against all cell lines with IC50 values in the 80-250nM range. In general hexahydrocycloocta[b]thieno[3,2-e]pyridines were most active with increasing activity observed as larger cycloalkyl rings were fused to the pyridine ring.
[Mh] Termos MeSH primário: Antineoplásicos/química
Antineoplásicos/farmacologia
Proliferação Celular/efeitos dos fármacos
Quinolinas/química
Quinolinas/farmacologia
Tienopiridinas/química
Tienopiridinas/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos/síntese química
Linhagem Celular Tumoral
Ensaios de Seleção de Medicamentos Antitumorais
Seres Humanos
Neoplasias/tratamento farmacológico
Quinolinas/síntese química
Relação Estrutura-Atividade
Tienopiridinas/síntese química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Quinolines); 0 (Thienopyridines); 0 (quinoline-3-carboxamide)
[Em] Mês de entrada:1610
[Cu] Atualização por classe:161230
[Lr] Data última revisão:
161230
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160209
[St] Status:MEDLINE


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[PMID]:26758983
[Au] Autor:Nylander S; Schulz R
[Ad] Endereço:AstraZeneca R&D, Mölndal, Sweden.
[Ti] Título:Effects of P2Y12 receptor antagonists beyond platelet inhibition--comparison of ticagrelor with thienopyridines.
[So] Source:Br J Pharmacol;173(7):1163-78, 2016 Apr.
[Is] ISSN:1476-5381
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The effect and clinical benefit of P2Y12 receptor antagonists may not be limited to platelet inhibition and the prevention of arterial thrombus formation. Potential additional effects include reduction of the pro-inflammatory role of activated platelets and effects related to P2Y12 receptor inhibition on other cells apart from platelets. P2Y12 receptor antagonists, thienopyridines and ticagrelor, differ in their mode of action being prodrugs instead of direct acting and irreversibly instead of reversibly binding to P2Y12 . These key differences may provide different potential when it comes to additional effects. In addition to P2Y12 receptor blockade, ticagrelor is unique in having the only well-documented additional target of inhibition, the equilibrative nucleoside transporter 1. The current review will address the effects of P2Y12 receptor antagonists beyond platelets and the protection against arterial thrombosis. The discussion will include the potential for thienopyridines and ticagrelor to mediate anti-inflammatory effects, to conserve vascular function, to affect atherosclerosis, to provide cardioprotection and to induce dyspnea.
[Mh] Termos MeSH primário: Adenosina/análogos & derivados
Fenômenos Fisiológicos Cardiovasculares/efeitos dos fármacos
Inibidores da Agregação de Plaquetas/farmacologia
Antagonistas do Receptor Purinérgico P2Y/farmacologia
Receptores Purinérgicos P2Y12/metabolismo
Tienopiridinas/farmacologia
[Mh] Termos MeSH secundário: Adenosina/farmacologia
Adenosina/uso terapêutico
Animais
Aterosclerose/fisiopatologia
Aterosclerose/prevenção & controle
Plaquetas/efeitos dos fármacos
Plaquetas/fisiologia
Cardiotônicos/farmacologia
Cardiotônicos/uso terapêutico
Transportador Equilibrativo 1 de Nucleosídeo/antagonistas & inibidores
Seres Humanos
Inflamação/sangue
Inibidores da Agregação de Plaquetas/uso terapêutico
Antagonistas do Receptor Purinérgico P2Y/uso terapêutico
Tienopiridinas/uso terapêutico
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Cardiotonic Agents); 0 (Equilibrative Nucleoside Transporter 1); 0 (Platelet Aggregation Inhibitors); 0 (Purinergic P2Y Receptor Antagonists); 0 (Receptors, Purinergic P2Y12); 0 (Thienopyridines); GLH0314RVC (Ticagrelor); K72T3FS567 (Adenosine)
[Em] Mês de entrada:1612
[Cu] Atualização por classe:170403
[Lr] Data última revisão:
170403
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160114
[St] Status:MEDLINE
[do] DOI:10.1111/bph.13429


  9 / 195 MEDLINE  
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[PMID]:26599501
[Au] Autor:McNamara LE; Liyanage N; Peddapuram A; Murphy JS; Delcamp JH; Hammer NI
[Ad] Endereço:Department of Chemistry and Biochemistry, University of Mississippi , University, Mississippi 38677, United States.
[Ti] Título:Donor-Acceptor-Donor Thienopyrazines via Pd-Catalyzed C-H Activation as NIR Fluorescent Materials.
[So] Source:J Org Chem;81(1):32-42, 2016 Jan 04.
[Is] ISSN:1520-6904
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:A series of thienopyrazine-based donor-acceptor-donor (D-A-D) near-infrared (NIR) fluorescent compounds were synthesized through a rapid, palladium-catalyzed C-H activation route. The dyes were studied through computational analysis, electrochemical properties analysis, and characterization of their photophysical properties. Large Stokes shifts of approximately 175 nm were observed, which led to near-infrared emission. Computational evaluation shows that the origin of this large Stokes shift is a significant molecular reorganization particularly about the D-A bond. The series exhibits quantum yields of up to φ = >4%, with emission maxima ranging from 725 to 820 nm. The emission is strong in solution, in thin films, and also in isolation at the single-molecule level. Their stable emission at the single-molecule level makes these compounds good candidates for single-molecule photon sources in the near-infrared.
[Mh] Termos MeSH primário: Corantes Fluorescentes/química
Paládio/química
Tienopiridinas/química
[Mh] Termos MeSH secundário: Catálise
Ligações de Hidrogênio
Estrutura Molecular
Oxirredução
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T; RESEARCH SUPPORT, U.S. GOV'T, NON-P.H.S.
[Nm] Nome de substância:
0 (Fluorescent Dyes); 0 (Thienopyridines); 5TWQ1V240M (Palladium)
[Em] Mês de entrada:1605
[Cu] Atualização por classe:160104
[Lr] Data última revisão:
160104
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:151125
[St] Status:MEDLINE
[do] DOI:10.1021/acs.joc.5b01958


  10 / 195 MEDLINE  
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[PMID]:25952285
[Au] Autor:Galeone M; Scarfì F; Bassi A; Massi D; Difonzo EM; Francalanci S
[Ad] Endereço:Division of Dermatology, Department of Surgery and Translational Medicine, University of Florence, Florence, Italy - massimiliano.galeone@gmail.com.
[Ti] Título:Lichenoid dermatitis caused by thienopyridine derivatives.
[So] Source:G Ital Dermatol Venereol;151(5):565-6, 2016 Oct.
[Is] ISSN:1827-1820
[Cp] País de publicação:Italy
[La] Idioma:eng
[Mh] Termos MeSH primário: Erupção por Droga/etiologia
Erupções Liquenoides/induzido quimicamente
Tienopiridinas/efeitos adversos
[Mh] Termos MeSH secundário: Erupção por Droga/diagnóstico
Erupção por Droga/patologia
Seres Humanos
Erupções Liquenoides/diagnóstico
Erupções Liquenoides/patologia
Masculino
Meia-Idade
Tienopiridinas/administração & dosagem
Ticlopidina/administração & dosagem
Ticlopidina/efeitos adversos
Ticlopidina/análogos & derivados
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Thienopyridines); A74586SNO7 (clopidogrel); OM90ZUW7M1 (Ticlopidine)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170417
[Lr] Data última revisão:
170417
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150509
[St] Status:MEDLINE



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