Synthesis of new series of thiazol-(2(3H)-ylideneamino)benzenesulfonamide derivatives as carbonic anhydrase inhibitors
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Tarih
2020
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
Wiley
Erişim Hakkı
info:eu-repo/semantics/closedAccess
Özet
Human carbonic anhydrase I and II isoenzymes (hCA I and II) are important metabolic enzymes. In this study, a new series of thiazol-(2(3H)-ylideneamino)benzenesulfonamide derivatives were synthesized and also some inhibition parameters including IC50(hydratese) and inhibition constant values (K-i, esterase) were determined. All studied compounds exhibited potent inhibition against these enzymes. They inhibited carbonic anhydrases (CAs) with the IC(50)values of 113 to 395.8 nM (K-i = 77.38-319.59 nM) for hCA I and 91.9 to 516 nM (K-i = 62.79-425.89 nM) for hCA II. Among the compounds,5cwas found to be the most active one (K-i: 77.38 nM) for hCA I and5gwas found for hCA II with the value of 62.79 nM.
Açıklama
Anahtar Kelimeler
2-iminothiazoline, carbonic anhydrase, enzyme inhibitor, sulfonamide
Kaynak
Journal of Biochemical and Molecular Toxicology
WoS Q Değeri
Q2
Scopus Q Değeri
Q2
Cilt
34
Sayı
12
