Article 2024 · 10 citations

Sulfonamide derivatives with benzothiazole scaffold: Synthesis and carbonic anhydrase I-II inhibition properties

Ozturk, Cansu, Kalay, Erbay, Gerni, Serpil, Balci, Neslihan, Tokali, Feyzi Sinan, Aslan, Osman Nuri, Polat, Emrah

Abstract

The secondary sulfonamide derivatives containing benzothiazole scaffold (1-10) were synthesized to determine their inhibition properties on two physiologically essential human carbonic anhydrases isoforms (hCAs, EC, 4.2.1.1), hCA I, and hCA II. The inhibitory effects of the compounds on hCA I and hCA II isoenzymes were investigated by comparing their IC50 and Ki values. The Ki values of compounds (1-10) against hCA I and hCA II are in the range of 0.052 +/- 0.022-0.971 +/- 0.280 and 0.025 +/- 0.010-0.682 +/- 0.335, respectively. Some of these inhibited the enzyme more effectively than the standard drug, acetazolamide. In particular, compounds 5 and 4 were found to be most effective on hCA I and hCA II.

Keywords

benzothiazole moiety human carbonic anhydrase I human carbonic anhydrase II inhibition secondary sulfonamide derivatives BACTERIAL VITRO

WoS Categories

Biochemistry & Molecular Biology Biotechnology & Applied Microbiology

Sustainable Development Goals

Good Health and Well-being

Citation

Journal: BIOTECHNOLOGY AND APPLIED BIOCHEMISTRY
Year: 2024
Volume: 71
Issue: 1
Pages: 223-231
ISSN: 0885-4513
eISSN: 1470-8744
DOI: 10.1002/bab.2534
WoS UID: WOS:001102034900001

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