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[PMID]: | 28161252 |
[Au] Autor: | Abdel-Aziz AA; Angeli A; El-Azab AS; Abu El-Enin MA; Supuran CT |
[Ad] Endereço: | Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia; Department of Medicinal Chemistry, Faculty of Pharmacy, University of Mansoura, Mansoura 35516, Egypt; Università degli Studi di Firenze, NEUROFARBA Dept., Sezione di Scienze Farmaceutiche, |
[Ti] Título: | Synthesis and biological evaluation of cyclic imides incorporating benzenesulfonamide moieties as carbonic anhydrase I, II, IV and IX inhibitors. |
[So] Source: | Bioorg Med Chem;25(5):1666-1671, 2017 Mar 01. | [Is] ISSN: | 1464-3391 |
[Cp] País de publicação: | England |
[La] Idioma: | eng |
[Ab] Resumo: | A group of cyclic imides was synthesized by reaction of amino-substituted benzenesulfonamides with a series of acid anhydrides such as succinic, maleic, tetrahydrophthalic, pyrazine-2,3-dicarboxylic acid anhydride, and substituted phthalic anhydrides. The synthesized sulfonamides were evaluated as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors against the human (h) isoforms hCA I, II, IV and IX, involved in a variety of diseases among which glaucoma, retinitis pigmentosa, etc. Some of these sulfonamides showed effective inhibitory action (in the nanomolar range) against the cytosolic isoform hCA II and the transmembrane, tumor-associated one hCA IX, making them interesting candidates for preclinical evaluation in glaucoma or various tumors in which the two enzymes are involved. hCA I and IV were on the other hand less inhibited by these sulfonamides, with inhibition constants in the micromolar range. |
[Mh] Termos MeSH primário: |
Inibidores da Anidrase Carbônica/síntese química Inibidores da Anidrase Carbônica/farmacologia Imidas/síntese química Imidas/farmacologia Sulfonamidas/química
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[Mh] Termos MeSH secundário: |
Espectroscopia de Ressonância Magnética Nuclear de Carbono-13 Inibidores da Anidrase Carbônica/química Seres Humanos Imidas/química Espectroscopia de Prótons por Ressonância Magnética Relação Estrutura-Atividade
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[Pt] Tipo de publicação: | JOURNAL ARTICLE |
[Nm] Nome de substância:
| 0 (Carbonic Anhydrase Inhibitors); 0 (Imides); 0 (Sulfonamides); 98-10-2 (benzenesulfonamide) |
[Em] Mês de entrada: | 1708 |
[Cu] Atualização por classe: | 170808 |
[Lr] Data última revisão:
| 170808 |
[Sb] Subgrupo de revista: | IM |
[Da] Data de entrada para processamento: | 170206 |
[St] Status: | MEDLINE |
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