Synthesis and evaluation of sulfonamide-bearing thiazole as carbonic anhydrase isoforms hCA I and hCA II

Arslan, Mustafa

dc.contributor.authors	Kilicaslan, S; Arslan, M; Ruya, Z; Bilen, C; Ergun, A; Gencer, N; Arslan, O;
dc.date.accessioned	2020-02-24T14:18:17Z
dc.date.available	2020-02-24T14:18:17Z
dc.date.issued	2016
dc.identifier.citation	Kilicaslan, S; Arslan, M; Ruya, Z; Bilen, C; Ergun, A; Gencer, N; Arslan, O; (2016). Synthesis and evaluation of sulfonamide-bearing thiazole as carbonic anhydrase isoforms hCA I and hCA II. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 31, 1305-1300
dc.identifier.issn	1475-6366
dc.identifier.uri	https://doi.org/10.3109/14756366.2015.1128426
dc.identifier.uri	https://hdl.handle.net/20.500.12619/45112
dc.description.abstract	Sulfonamide-bearing thiazole compounds were synthesized and their inhibitory effects on the activity of purified human carbonic anhydrase I and II were evaluated. Human carbonic anhydrase isoenzymes (hCA-I and hCA-II) were purified from erythrocyte cells by affinity chromatography. The inhibitory effects of the 12 synthesized sulfonamide (5a-l) on the hydratase and esterase activities of these isoenzymes (hCA-I and hCA-II) were studied in vitro. In relation to these activities, the inhibition equilibrium constants (Ki) were determined. The results showed that all the synthesized compounds inhibited the CA isoenzyme activity. Among them 5b was found to be the most active (IC50 = 0.35 mu M; Ki: 0.33 mu M) for hCA I and hCA II.
dc.language	English
dc.publisher	TAYLOR & FRANCIS LTD
dc.subject	Pharmacology & Pharmacy
dc.title	Synthesis and evaluation of sulfonamide-bearing thiazole as carbonic anhydrase isoforms hCA I and hCA II
dc.type	Article
dc.identifier.volume	31
dc.identifier.startpage	1300
dc.identifier.endpage	1305
dc.contributor.department	Sakarya Üniversitesi/Fen-Edebiyat Fakültesi/Kimya Bölümü
dc.contributor.saüauthor	Arslan, Mustafa
dc.relation.journal	JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
dc.identifier.wos	WOS:000385270300055
dc.identifier.doi	10.3109/14756366.2015.1128426
dc.identifier.eissn	1475-6374
dc.contributor.author	Arslan, Mustafa