Abstract
A novel series of imidazo[2,1-b]thiazole-sulfonyl piperazine conjugates (9aa-ee) has been synthesized and evaluated for carbonic anhydrase (CA, EC 4.2.1.1) inhibitory potency against four isoforms: The cytosolic isozyme hCA I, II and trans-membrane tumor-associated isoform hCA IX and hCA XII, taking acetazolamide (AAZ) as standard drug, using a stopped flow CO2 hydrase assay. The results revealed that most of the compounds showed selective activity against hCA II whereas none of them were active against hCA I, IX, XII (Ki > 100 µM). The physiologically dominant cytosolic isoform hCA II was inhibited by these molecules with inhibition constants in the range of 57.7–98.2 µM. This new derivative, thus, selectively inhibits hCA II over the hCA I, IX, XII isoforms, which may be used for further understanding the physiological roles of some of these isoforms in various pathologies.
Highlights
Carbonic anhydrases (CAs, EC 4.2.1.1) are a group of zinc containing metalloenzymes that effectively catalyze the reversible hydration of CO2 to bicarbonate and proton, an important reaction for many physiological processes
We have reported the synthesis of imidazo[2,1-b]thiazole-sulfonyl piperazine the reported values)
(9aa-ee), which are designed tothe target synthesized compounds we reported of imidazo[2,1-b]thiazole-sulfonyl piperazine associated isoforms, human carbonic anhydrases (hCAs)
Summary
Carbonic anhydrases (CAs, EC 4.2.1.1) are a group of zinc containing metalloenzymes that effectively catalyze the reversible hydration of CO2 to bicarbonate and proton, an important reaction for many physiological processes. It is important to develop an effective approach that can selectively inhibit these isoforms involved in different diseases. Imidazo[2,1-b]thiazole-guanylhydrazone is Imidazo[2,1-b]thiazole-guanylhydrazone is aa promising promisinglead leadwith withpotent potentanticancer anticanceractivity activityagainst againsta number of cancer cell lines [5]. These fused heterocycles exhibit potent anticancer activity through a number of cancer cell lines [5]. Sharma and Supuran et al have reported a series of benzenesulfonamide bearing imidazothiadiazole and thiazolotriazole hybrids as carbonic anhydrases benzenesulfonamide bearing imidazothiadiazole and thiazolotriazole hybrids as carbonic.
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