作者
Maryam Aisyah Abdullah, Yu-Ri Lee, Siti Nurulhuda Mastuki, Sze Wei Leong, Wan Norhamidah Wan Ibrahim, Muhammad Alif Mohammad Latif, Aizi Nor Mazila Ramli, Mohd Fadhlizil Fasihi Mohd Aluwi, Siti Munirah Mohd Faudzi, Cheol-Hee Kim
发表日期
2020/11/1
期刊
Bioorganic Chemistry
卷号
104
页码范围
104277
出版商
Academic Press
简介
A series of aminated- (1–9) and sulfonamide-containing diarylpentadienones (10–18) were synthesized, structurally characterized, and evaluated for their in vitro anti-diabetic potential on α-glucosidase and DPP-4 enzymes. It was found that all the new molecules were non-associated PAINS compounds. The sulfonamide-containing series (compounds 10–18) selectively inhibited α-glucosidase over DPP-4, in which compound 18 demonstrated the highest activity with an IC50 value of 5.69 ± 0.5 µM through a competitive inhibition mechanism. Structure-activity relationship (SAR) studies concluded that the introduction of the trifluoromethylbenzene sulfonamide moiety was essential for the suppression of α-glucosidase. The most active compound 18, was then further tested for in vivo toxicities using the zebrafish animal model, with no toxic effects detected in the normal embryonic development, blood vessel …
学术搜索中的文章
MA Abdullah, YR Lee, SN Mastuki, SW Leong… - Bioorganic Chemistry, 2020