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[PMID]:28782186
[Au] Autor:Sowaileh MF; Hazlitt RA; Colby DA
[Ad] Endereço:Department of BioMolecular Sciences, University of Mississippi, University, MS, 38677, USA.
[Ti] Título:Application of the Pentafluorosulfanyl Group as a Bioisosteric Replacement.
[So] Source:ChemMedChem;12(18):1481-1490, 2017 Sep 21.
[Is] ISSN:1860-7187
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:The success of fluorinated molecules in drug design has led medicinal chemists to search for new fluorine-containing substituents. A major recently developed group is the pentafluorosulfanyl group. This group is stable under physiological conditions and displays unique physical and chemical properties. There are currently few synthetic methods to install the SF group, yet efforts to integrate this group into lead optimization continue unabated. Typically, the SF group has been used as a replacement for trifluoromethyl, tert-butyl, halogen, or nitro groups. In this review, the use of the SF group as a bioisosteric replacement for each of these three functionalities is compared and contrasted across various groups of biologically active molecules. The organization and presentation of these data should be instructive to medicinal chemists considering to design synthetic strategies to access SF -substituted molecules.
[Mh] Termos MeSH primário: Sulfetos/química
Compostos de Enxofre/química
[Mh] Termos MeSH secundário: Antiprotozoários/química
Antiprotozoários/farmacologia
Desenho de Drogas
Ácido Flufenâmico/análogos & derivados
Ácido Flufenâmico/farmacologia
Halogenação
NADH NADPH Oxirredutases/antagonistas & inibidores
NADH NADPH Oxirredutases/metabolismo
Oxirredutases atuantes sobre Doadores de Grupo CH-CH/antagonistas & inibidores
Oxirredutases atuantes sobre Doadores de Grupo CH-CH/metabolismo
Plasmodium falciparum/efeitos dos fármacos
Plasmodium falciparum/enzimologia
Ligação Proteica
Receptores de Canabinoides/química
Receptores de Canabinoides/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Antiprotozoal Agents); 0 (Receptors, Cannabinoid); 0 (Sulfides); 0 (Sulfur Compounds); 60GCX7Y6BH (Flufenamic Acid); EC 1.3.- (Oxidoreductases Acting on CH-CH Group Donors); EC 1.3.5.2 (dihydroorotate dehydrogenase); EC 1.6.- (NADH, NADPH Oxidoreductases); EC 1.8.1.12 (trypanothione reductase)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171009
[Lr] Data última revisão:
171009
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170808
[St] Status:MEDLINE
[do] DOI:10.1002/cmdc.201700356


  2 / 924 MEDLINE  
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[PMID]:28759638
[Au] Autor:Alshehri S; Shakeel F; Ibrahim M; Elzayat E; Altamimi M; Shazly G; Mohsin K; Alkholief M; Alsulays B; Alshetaili A; Alshahrani A; Almalki B; Alanazi F
[Ad] Endereço:Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
[Ti] Título:Influence of the microwave technology on solid dispersions of mefenamic acid and flufenamic acid.
[So] Source:PLoS One;12(7):e0182011, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The present studies were undertaken to develop solvent-free solid dispersions (SDs) for poorly soluble anti-inflammatory drugs mefenamic acid (MA) and flufenamic acid (FFA) in order to enhance their in vitro dissolution rate and in vivo anti-inflammatory effects. The SDs of MA and FFA were prepared using microwaves irradiation (MW) technique. Different carriers such as Pluronic F127® (PL), Eudragit EPO® (EPO), polyethylene glycol 4000 (PEG 4000) and Gelucire 50/13 (GLU) were used for the preparation of SDs. Prepared MW irradiated SDs were characterized physicochemically using differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), Fourier transform infra-red (FT-IR) spectroscopy, powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM). The physicochemical characteristics and drug release profile of SDs were compared with pure drugs. The results of DSC, TGA, FT-IR, PXRD and SEM showed that SDs were successfully prepared. In vitro dissolution rate of MA and FFA was remarkably enhanced by SDs in comparison with pure MA and FFA. The SDs of MA and FFA prepared using PEG 400 showed higher drug release profile in comparison with those prepared using PL, EPO or GLU. The dissolution efficiency for MA-PEG SD and FFA-PEG SD was obtained as 61.40 and 59.18%, respectively. Optimized SDs were also evaluated for in vivo anti-inflammatory effects in male Wistar rats. The results showed significant % inhibition by MA-PEG (87.74% after 4 h) and FFA-PEG SDs (81.76% after 4 h) in comparison with pure MA (68.09% after 4 h) and pure FFA (55.27% after 4 h) (P<0.05). These results suggested that MW irradiated SDs of MA and FFA could be successfully used for the enhancement of in vitro dissolution rate and in vivo therapeutic efficacy of both drugs.
[Mh] Termos MeSH primário: Anti-Inflamatórios/efeitos da radiação
Ácido Flufenâmico/efeitos da radiação
Ácido Mefenâmico/efeitos da radiação
Micro-Ondas
[Mh] Termos MeSH secundário: Anti-Inflamatórios/química
Ácido Flufenâmico/química
Ácido Mefenâmico/química
Solubilidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents); 367589PJ2C (Mefenamic Acid); 60GCX7Y6BH (Flufenamic Acid)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170928
[Lr] Data última revisão:
170928
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170801
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0182011


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[PMID]:28228088
[Au] Autor:Madhava G; Ramana KV; Sudhana SM; Rao DS; Kumar KH; Lokanatha V; Rani AU; Raju CN
[Ad] Endereço:Department of Chemistry, Sri Venkateswara University, Tirupati-517 502, Andhra Pradesh, India.
[Ti] Título:Aryl/heteroaryl Substituted Celecoxib Derivatives as COX-2 Inhibitors: Synthesis, Anti-inflammatory Activity and Molecular Docking Studies.
[So] Source:Med Chem;13(5):484-497, 2017.
[Is] ISSN:1875-6638
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Cyclooxygenase (COX-2) inhibitors have been developed to provide better anti-inflammatory and analgesic efficacy than those of traditional NSAIDs. Several compounds having selective COX-2 inhibitors such as SC-558, Celecoxib, Rofecoxib, Valdecoxib and Etoricoxib are marketed as new generation NSAIDs and block the production of prostaglandins (PGs) in inflammatory cells. New anti-inflammatory agents with improved potency and safety profile are still needed. OBJECTIVE: As a part of our continuation research work towards new anti-inflammatory agents, the synthesis of N-substituted aryl/heteroaryl-pyrazole-1yl benzene sulfonamide (Celecoxib) derivatives, their anti-inflammatory activity in both methods in vitro and in vivo and molecular docking study on COX-2 enzyme will be discussed in this study. METHODS: A series of N-substituted (aryl/heteroarylpyrazol-1-yl)benzenesulfonamide (Celecoxib) derivatives was synthesized and characterized them using IR, NMR (1H and 13C), mass and elemental analyses. Anti-inflammatory activity of the title compounds was evaluated by in vitro initially using albumin denaturation and membrane stabilization methods, enzymatic activity against COX-2 enzyme using colorimetric assay and then in vivo by carrageenan induced paw oedema and cotton pellet induced granuloma methods. The docking study was performed, to find the binding mode of the title compounds with the binding site of the COX-2 enzyme. RESULTS: The biological activity screening data disclosed that some of the compounds 5b, 5e, 5f and 5i exhibited potent anti-inflammatory activity in both methods, in vitro and in vivo. The enzymatic assay on COX-2 enzyme demonstrated that few compounds potently inhibit COX-2 enzyme activity with IC50 of <0.89 μM. Unexpectedly, compound 5e (IC50, 0.62±0.17 μM) showed more potent COX-2 inhibited activity than that of parent drug, celecoxib (IC50, 0.62±0.25 μM) and the standard, flufenamic acid (IC50, 0.71±0.12 μM). CONCLUSION: The bio-screening data, in vitro and in vivo anti-inflammatory activity and COX-2 enzymatic assay revealed that few N-substituteed aryl/heteroaryl-pyrazol-1-yl) benzene sulfonamides showed potent activity and compound 5e showed more potent COX-2 inhibit activity than that of parent drug, celecoxib and the standard, flufenamic acid. Moreover, all the newly synthesized title products were bonded well with good binding energies in the sight of COX-2 enzyme. Therefore, the described study might provide sustained information to the development of new series of derivatives with potent drug like activity.
[Mh] Termos MeSH primário: Anti-Inflamatórios não Esteroides/farmacologia
Celecoxib/análogos & derivados
Celecoxib/farmacologia
Inibidores de Ciclo-Oxigenase 2/farmacologia
[Mh] Termos MeSH secundário: Animais
Anti-Inflamatórios não Esteroides/síntese química
Celecoxib/síntese química
Inibidores de Ciclo-Oxigenase 2/síntese química
Diclofenaco/farmacologia
Feminino
Ácido Flufenâmico/farmacologia
Masculino
Simulação de Acoplamento Molecular
Ratos Wistar
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Cyclooxygenase 2 Inhibitors); 144O8QL0L1 (Diclofenac); 60GCX7Y6BH (Flufenamic Acid); JCX84Q7J1L (Celecoxib)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170929
[Lr] Data última revisão:
170929
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170224
[St] Status:MEDLINE
[do] DOI:10.2174/1573406413666170221093740


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[PMID]:28154263
[Au] Autor:Iino H; Fujii M; Fujino M; Kohara S; Hashizaki K; Kira H; Koizumi N; Watanabe Y; Utoguchi N
[Ad] Endereço:Department of Pharmaceutics and Biopharmaceutics, Showa Pharmaceutical University.
[Ti] Título:Influence of Characteristics of Oily Vehicle on Skin Penetration of Ufenamate.
[So] Source:Biol Pharm Bull;40(2):220-226, 2017.
[Is] ISSN:1347-5215
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:Skin penetration amounts of a highly lipophilic drug, ufenamate, prepared in four oily vehicles, including white petrolatum (WP), liquid paraffin (LP), isopropyl myristate (IPM), and isocetyl stearate (ICS), were compared. Ufenamate was mixed in each vehicle at 5% and applied at a rate of 2 mg/cm to intact, stripped, and delipidized Yucatan micropig skin. The amounts of ufenamate and IPM in the stratum corneum (SC), epidermis, and dermis were determined. The skin penetration amounts of ufenamate from liquid oils were significantly higher than those from WP; the amounts of ufenamate were in the order WP
[Mh] Termos MeSH primário: Portadores de Fármacos/metabolismo
Ácido Flufenâmico/análogos & derivados
Óleos/metabolismo
Absorção Cutânea/fisiologia
[Mh] Termos MeSH secundário: Animais
Portadores de Fármacos/química
Portadores de Fármacos/farmacologia
Ácido Flufenâmico/metabolismo
Ácido Flufenâmico/farmacologia
Óleos/química
Óleos/farmacologia
Técnicas de Cultura de Órgãos
Absorção Cutânea/efeitos dos fármacos
Suínos
Porco Miniatura
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Drug Carriers); 0 (Oils); 60GCX7Y6BH (Flufenamic Acid); 8Z7O7C1SLZ (ufenamate)
[Em] Mês de entrada:1702
[Cu] Atualização por classe:170208
[Lr] Data última revisão:
170208
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170204
[St] Status:MEDLINE
[do] DOI:10.1248/bpb.b16-00817


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[PMID]:28119077
[Au] Autor:Pongkorpsakol P; Satitsri S; Wongkrasant P; Chittavanich P; Kittayaruksakul S; Srimanote P; Chatsudthipong V; Muanprasat C
[Ad] Endereço:Graduate Program in Translational Medicine, Research Center, Faculty of Medicine Ramathibodi Hospital, Mahidol University, Rama VI Road, Rajathevi, Bangkok 10400, Thailand.
[Ti] Título:Flufenamic acid protects against intestinal fluid secretion and barrier leakage in a mouse model of Vibrio cholerae infection through NF-κB inhibition and AMPK activation.
[So] Source:Eur J Pharmacol;798:94-104, 2017 Mar 05.
[Is] ISSN:1879-0712
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Nuclear factor kappa B (NF-κB)-mediated inflammatory responses play crucial roles in the pathogenesis of diarrhea caused by the Vibrio cholerae El Tor variant (EL), which is a major bacterial strain causing recent cholera outbreaks. Flufenamic acid (FFA) has previously been demonstrated to be a potent activator of AMP-activated protein kinase (AMPK), which is a negative regulator of NF-κB signaling. This study aimed to investigate the anti-diarrheal efficacy of FFA in a mouse model of EL infection and to investigate the mechanisms by which FFA activates AMPK in intestinal epithelial cells (IEC). In a mouse closed loop model of EL infection, FFA treatment (20mg/kg) significantly abrogated EL-induced intestinal fluid secretion and barrier disruption. In addition, FFA suppressed NF-κB nuclear translocation and expression of proinflammatory mediators and promoted AMPK phosphorylation in the EL-infected mouse intestine. In T84 cells, FFA induced AMPK activation. Furthermore, FFA promoted tight junction assembly and prevented interferon gamma (IFN-γ)-induced barrier disruption in an AMPK-dependent manner. Biochemical and molecular docking analyses indicated that FFA activates AMPK via a direct stimulation of calcium/calmodulin-dependent protein kinase kinase beta (CaMKKß) activity. Collectively, our data indicate that FFA represents a class of existing drugs that may be of potential utility in the treatment of cholera caused by EL infection via AMPK-mediated suppression of NF-κB signaling in IEC.
[Mh] Termos MeSH primário: Proteínas Quinases Ativadas por AMP/metabolismo
Líquidos Corporais/secreção
Cólera/tratamento farmacológico
Ácido Flufenâmico/farmacologia
Intestinos/efeitos dos fármacos
NF-kappa B/antagonistas & inibidores
Vibrio cholerae/fisiologia
[Mh] Termos MeSH secundário: Animais
Líquidos Corporais/efeitos dos fármacos
Quinase da Proteína Quinase Dependente de Cálcio-Calmodulina/química
Quinase da Proteína Quinase Dependente de Cálcio-Calmodulina/metabolismo
Domínio Catalítico
Linhagem Celular
Cólera/enzimologia
Cólera/metabolismo
Diarreia/tratamento farmacológico
Diarreia/virologia
Modelos Animais de Doenças
Ácido Flufenâmico/metabolismo
Ácido Flufenâmico/uso terapêutico
Mucosa Intestinal/efeitos dos fármacos
Mucosa Intestinal/metabolismo
Mucosa Intestinal/patologia
Camundongos
Simulação de Acoplamento Molecular
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (NF-kappa B); 60GCX7Y6BH (Flufenamic Acid); EC 2.7.11.17 (Calcium-Calmodulin-Dependent Protein Kinase Kinase); EC 2.7.11.31 (AMP-Activated Protein Kinases)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170126
[St] Status:MEDLINE


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[PMID]:27761807
[Au] Autor:Preethi B; Shanthi V; Ramanathan K
[Ad] Endereço:Department of Biotechnology, School of Bio Sciences and Technology, VIT University, Vellore, 632014, Tamil Nadu, India.
[Ti] Título:Identification of Potential Therapeutics to Conquer Drug Resistance in Salmonella typhimurium: Drug Repurposing Strategy.
[So] Source:BioDrugs;30(6):593-605, 2016 Dec.
[Is] ISSN:1179-190X
[Cp] País de publicação:New Zealand
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Salmonella typhimurium is the main cause of gastrointestinal illness in humans, and treatment options are decreasing because drug-resistant strains have emerged. OBJECTIVE: The objective of this study was to use computational drug repurposing to identify a novel candidate with an effective mechanism of action to circumvent the drug resistance. METHODS: We used the Mantra 2.0 database to initially screen drug candidates that share similar gene expression profiles to those of quinolones. Data were further reduced using pharmacophore mapping theory. Finally, we employed molecular-simulation studies to calculate the binding affinity of the screened candidates with DNA gyrase, alongside an analysis of side effects. RESULTS: A total of 16 drug candidates from the Mantra 2.0 database were screened. The pharmacophoric features of the screened candidates were examined and nalidixic acid features compared using the PharamGist program. A total of 11 compounds with the highest pharmacophore score were considered for binding energy calculation. Finally, we analysed the side effects of the eight drug candidates that showed significant binding affinity in the simulation study. CONCLUSION: Overall, flufenamic acid and sulconazole may be potential drug candidates that could be studied in vitro to assess their resistance profile against Salmonella enterica Typhimurium.
[Mh] Termos MeSH primário: Antibacterianos/farmacologia
Avaliação Pré-Clínica de Medicamentos/métodos
Reposicionamento de Medicamentos/métodos
Farmacorresistência Bacteriana/efeitos dos fármacos
Salmonella typhimurium/efeitos dos fármacos
Inibidores da Topoisomerase II/farmacologia
[Mh] Termos MeSH secundário: Antibacterianos/metabolismo
DNA Girase/química
DNA Girase/metabolismo
Bases de Dados Factuais
Ácido Flufenâmico/metabolismo
Ácido Flufenâmico/farmacologia
Regulação Bacteriana da Expressão Gênica/efeitos dos fármacos
Imidazóis/metabolismo
Imidazóis/farmacologia
Simulação de Acoplamento Molecular
Reprodutibilidade dos Testes
Salmonella typhimurium/patogenicidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Imidazoles); 0 (Topoisomerase II Inhibitors); 5D9HAA5Q5S (sulconazole); 60GCX7Y6BH (Flufenamic Acid); EC 5.99.1.3 (DNA Gyrase)
[Em] Mês de entrada:1701
[Cu] Atualização por classe:170123
[Lr] Data última revisão:
170123
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161021
[St] Status:MEDLINE


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[PMID]:27709699
[Au] Autor:Özkaya E
[Ad] Endereço:Department of Dermatology and Venereology, Istanbul Medical Faculty, Istanbul University, 34093, Çapa-Istanbul, Turkey. profeo@istanbul.edu.tr.
[Ti] Título:Patch testing with used and unused personal products: a practical way to show contamination with contact allergens.
[So] Source:Contact Dermatitis;75(5):328-330, 2016 Nov.
[Is] ISSN:1600-0536
[Cp] País de publicação:England
[La] Idioma:eng
[Mh] Termos MeSH primário: Alérgenos/efeitos adversos
Anti-Inflamatórios não Esteroides/efeitos adversos
Antifúngicos/efeitos adversos
Dermatite Alérgica de Contato/etiologia
Contaminação de Equipamentos
Dermatoses do Pé/etiologia
Testes do Emplastro/métodos
[Mh] Termos MeSH secundário: Administração Tópica
Adulto
Idoso
Colchicina/efeitos adversos
Colchicina/análogos & derivados
Dermatite Alérgica de Contato/diagnóstico
Tendinopatia do Cotovelo/terapia
Feminino
Ácido Flufenâmico/efeitos adversos
Ácido Flufenâmico/análogos & derivados
Dermatoses do Pé/diagnóstico
Seres Humanos
Masculino
Aparelhos Ortopédicos/efeitos adversos
Sapatos/efeitos adversos
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Allergens); 0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Antifungal Agents); 60GCX7Y6BH (Flufenamic Acid); KZF0XM66JC (etofenamate); SML2Y3J35T (Colchicine); T1X8S697GT (thiocolchicoside)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170418
[Lr] Data última revisão:
170418
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161007
[St] Status:MEDLINE
[do] DOI:10.1111/cod.12626


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[PMID]:27641472
[Au] Autor:Monteillier A; Loucif A; Omoto K; Stevens EB; Lainez S; Saintot PP; Cao L; Pryde DC
[Ad] Endereço:Pfizer Neuroscience and Pain Research Unit, Portway Building, Granta Park, Great Abington, Cambridge CB21 6GS, UK.
[Ti] Título:Investigation of the structure activity relationship of flufenamic acid derivatives at the human TRESK channel K 18.1.
[So] Source:Bioorg Med Chem Lett;26(20):4919-4924, 2016 10 15.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:TRESK (Twik RElated Spinal cord K channel) is a member of the Twin Pore Domain potassium channel (K2P) family responsible for regulating neuronal excitability in dorsal root ganglion (DRG) and trigeminal (TG) neurons, peripheral neurons involved in pain transmission. As channel opening causes an outward K current responsible for cell hyperpolarisation, TRESK represents a potentially interesting target for pain treatment. However, as no crystal structure exists for this protein, the mechanisms involved in the opening action of its ligands are still poorly understood, making the development of new potent and selective openers challenging. In this work we present a structure activity relationship (SAR) of the known TRESK opener flufenamic acid (FFA) and some derivatives, investigating the functional effects of chemical modifications to build a TRESK homology model to support the biological results. A plausible binding mode is proposed, providing the first predictive hypothesis of a human TRESK opener binding site.
[Mh] Termos MeSH primário: Ácido Flufenâmico/química
Ácido Flufenâmico/farmacologia
Canais de Potássio/química
[Mh] Termos MeSH secundário: Animais
Sítios de Ligação
Células HEK293
Seres Humanos
Camundongos
Neurônios/efeitos dos fármacos
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (KCNK18 protein, human); 0 (Potassium Channels); 60GCX7Y6BH (Flufenamic Acid)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:171125
[Lr] Data última revisão:
171125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160920
[St] Status:MEDLINE


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[PMID]:27494289
[Au] Autor:Guo M; Wang K; Hamill N; Lorimer K; Li M
[Ad] Endereço:School of Pharmacy, De Montfort University , Leicester LE1 9BH, U.K.
[Ti] Título:Investigating the Influence of Polymers on Supersaturated Flufenamic Acid Cocrystal Solutions.
[So] Source:Mol Pharm;13(9):3292-307, 2016 Sep 06.
[Is] ISSN:1543-8392
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The development of enabling formulations is a key stage when demonstrating the effectiveness of pharmaceutical cocrystals to maximize the oral bioavailability for poorly water soluble drugs. Inhibition of drug crystallization from a supersaturated cocrystal solution through a fundamental understanding of the nucleation and crystal growth is important. In this study, the influence of the three polymers of polyethylene glycol (PEG), polyvinylpyrrolidone (PVP), and a copolymer of N-vinly-2-pyrrodidone (60%) and vinyl acetate (40%) (PVP-VA) on the flufenamic acid (FFA) crystallization from three different supersaturated solutions of the pure FFA and two cocrystals of FFA-NIC CO and FFA-TP CO has been investigated by measuring nucleation induction times and desupersaturation rates in the presence and absence of seed crystals. It was found that the competition of intermolecular hydrogen bonding among drug/coformer, drug/polymer, and coformer/polymer was a key factor responsible for maintaining supersaturation through nucleation inhibition and crystal growth modification in a cocrystal solution. The supersaturated cocrystal solutions with predissolved PEG demonstrated more effective stabilization in comparison to the pure FFA in the presence of the same polymer. In contrast, neither of the two cocrystal solutions, in the presence of PVP or PVP-VA, exhibited a better performance than the pure FFA with the same predissolved polymer. The study suggests that the selection of a polymeric excipient in a cocrystal formulation should not be solely dependent on the interplay of the parent drug and polymer without considering the coformer effects.
[Mh] Termos MeSH primário: Ácido Flufenâmico/química
Polímeros/química
[Mh] Termos MeSH secundário: Varredura Diferencial de Calorimetria
Cristalização
Microscopia de Polarização
Polietilenoglicóis/química
Povidona/química
Soluções/química
Espectroscopia de Infravermelho com Transformada de Fourier
Difração de Raios X
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Polymers); 0 (Solutions); 30IQX730WE (Polyethylene Glycols); 60GCX7Y6BH (Flufenamic Acid); FZ989GH94E (Povidone)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160806
[St] Status:MEDLINE
[do] DOI:10.1021/acs.molpharmaceut.6b00612


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[PMID]:27155725
[Au] Autor:Tarushi A; Kastanias P; Raptopoulou CP; Psycharis V; Kessissoglou DP; Papadopoulos AN; Psomas G
[Ad] Endereço:Department of General and Inorganic Chemistry, Faculty of Chemistry, Aristotle University of Thessaloniki, P.O. Box 135, GR-54124 Thessaloniki, Greece.
[Ti] Título:Zinc complexes of flufenamic acid: Characterization and biological evaluation.
[So] Source:J Inorg Biochem;163:332-345, 2016 Oct.
[Is] ISSN:1873-3344
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The reaction of ZnCl with the non-steroidal anti-inflammatory drug flufenamic acid (Hfluf) led to the formation of complex [Zn(fluf-O) (MeOH) ], 1. When the reaction takes places in the presence of a N,N'-donor heterocyclic ligand such as 2.2'-bipyridylamine (bipyam), 2.2'-bipyridine (bipy), 1.10-phenanthroline (phen) and 2.2'-dipyridylketone oxime (Hpko), the complexes [Zn(fluf) (bipyam)], 2, [Zn(fluf) (bipy)], 3, [Zn(fluf)(phen) (H O)](fluf)·0.2MeOH, 4·0.2MeOH and [Zn(fluf) (Hpko) ], 5 were isolated, respectively. The complexes were characterized by physicochemical and spectroscopic techniques and the crystal structures of complexes 2 and 4 were determined by X-ray crystallography. The ability of the complexes to scavenge 1.1-diphenyl-picrylhydrazyl, 2.2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) and hydroxyl radicals and to inhibit soybean lipoxygenase was evaluated; the complexes were more active than free Hfluf. The interaction of the complexes with serum albumins was investigated by fluorescence emission spectroscopy and the corresponding binding constants were calculated. UV-vis spectroscopy, viscosity measurements and fluorescence emission spectroscopy for the competitive studies of the complexes with ethidium bromide were the techniques employed to monitor the interaction of the complexes with calf-thymus DNA and revealed intercalation as the most possible mode of binding.
[Mh] Termos MeSH primário: Complexos de Coordenação/química
DNA/química
Ácido Flufenâmico/química
Substâncias Intercalantes/química
Lipoxigenase/química
Proteínas de Plantas/química
Soroalbumina Bovina/química
Zinco/química
[Mh] Termos MeSH secundário: Animais
Bovinos
Feijão de Soja/enzimologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Coordination Complexes); 0 (Intercalating Agents); 0 (Plant Proteins); 27432CM55Q (Serum Albumin, Bovine); 60GCX7Y6BH (Flufenamic Acid); 9007-49-2 (DNA); 91080-16-9 (calf thymus DNA); EC 1.13.11.12 (Lipoxygenase); J41CSQ7QDS (Zinc)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160509
[St] Status:MEDLINE



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