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某些新型磺胺类抑制剂对人碳酸酐酶I和II的体外抑制作用。

In vitro inhibition effects of some new sulfonamide inhibitors on human carbonic anhydrase I and II.

作者信息

Cakir Umit, Uğraş Halil Ibrahim, Ozensoy Ozen, Sinan Selma, Arslan Oktay

机构信息

Balikesir University Science & Art Faculty, Department of Chemistry, 10100 Balikesir, Turkey.

出版信息

J Enzyme Inhib Med Chem. 2004 Jun;19(3):257-61. doi: 10.1080/14756360410001689586.

Abstract

A new series of aromatic and heterocyclic sulfonamides, including six new derivatives, 2-(3-cyclohexene-1-carbamido)-1,3,4-thiadiazole-5-sulfonamide (CCTS), 4-(3-cyclohexene-1-carbamido) methyl-benzenesulfonamide (CCBS), 2-(9-octadecenoylamido)-1,3,4-thiadiazole-5-sulfonamide (ODTS), 2-(4,7,10-trioxa-tetradecanoylamido)-1,3,4-thiadiazole-5-sulfonamide (TDTS), 2-(coumarine-3-carbamido)-1,3,4-thiadiazole-5-sulfonamide (COTS) and 2-(8-methoxycoumarine-3-carbamido)-1,3,4-thiadiazole-5-sulfonamide (MCTS), has been investigated. These sulfonamides were assayed for inhibition of human carbonic anhydrase I (hCA-I) and human carbonic anhydrase II (hCA-II) which were purified by affinity chromatography.

摘要

已对一系列新的芳香族和杂环磺酰胺进行了研究,其中包括六种新衍生物,即2-(3-环己烯-1-甲酰胺基)-1,3,4-噻二唑-5-磺酰胺(CCTS)、4-(3-环己烯-1-甲酰胺基)甲基苯磺酰胺(CCBS)、2-(9-十八碳烯酰胺基)-1,3,4-噻二唑-5-磺酰胺(ODTS)、2-(4,7,10-三氧杂十四烷酰胺基)-1,3,4-噻二唑-5-磺酰胺(TDTS)、2-(香豆素-3-甲酰胺基)-1,3,4-噻二唑-5-磺酰胺(COTS)和2-(8-甲氧基香豆素-3-甲酰胺基)-1,3,4-噻二唑-5-磺酰胺(MCTS)。通过亲和色谱法纯化了人碳酸酐酶I(hCA-I)和人碳酸酐酶II(hCA-II),并对这些磺酰胺抑制这两种酶的能力进行了测定。

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