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Carbonic Anhydrase Inhibitors. Part 551 Metal Complexes of 134-Thiadiazole-2-Sulfonamide Derivatives: In Vitro InhibitionStudies With Carbonic Anhydrase Isozymes I II and IV

机译:碳酸酐酶抑制剂。 551部分134-噻二唑-2-磺酰胺衍生物的金属配合物:体外抑制碳酸酐酶同工酶III和IV的研究

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摘要

Coordination compounds of 5-chloroacetamido-1,3,4-thiadiazole-2-sulfonamide (Hcaz) with V(IV), Cr(lll), Fe(ll), Co(ll), Ni(ll) and Cu(ll) have been prepared and characterized by standard procedures (spectroscopic, magnetic, EPR, thermogravimetric and conductimetric measurements). Some of these compounds showed very good in vitro inhibitory properties against three physiologically relevant carbonic anhydrase (CA)isozymes, i.e., CA I, II, and IV. The differences between these isozymes in susceptibility to inhibition by these metal complexes is discussed in relationship to the characteristic features of their active sites, and is rationalized in terms useful for developing isozyme-specific CA inhibitors.
机译:5-氯乙酰氨基-1,3,4-噻二唑-2-磺酰胺(Hcaz)与V(IV),Cr(III),Fe(II),Co(II),Ni(II)和Cu(II)的配位化合物)已通过标准程序(光谱,磁,EPR,热重和电导测量)进行了准备并进行了表征。这些化合物中的一些对三种生理相关的碳酸酐酶(CA)同功酶,即CA I,II和IV表现出非常好的体外抑制特性。讨论了这些同功酶之间对这些金属配合物抑制敏感性的差异,并与它们的活性位点的特征相关联,并就可用于开发同功酶特异性CA抑制剂的意义合理化了。

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