2-(2'-Pyridyl) Benzimidazole Analogs and their β-Glucuronidase Inhibitory Activity.

Autor: Kamil, Arfa, Akhtar, Shamim, Noureen, Shagufta, Saify, Zafar Saied, Jahan, Sarwat, Khan, Khalid Mohammed, Rahim, Fazal, Mushtaq, Nousheen, Arif, Muhammad, Perveen, Shahnaz, Chaudhary, Muhammad Iqbal
Předmět:
Zdroj: Journal of the Chemical Society of Pakistan; 8/31/2015, Vol. 37 Issue 4, p787-791, 5p
Abstrakt: Synthesis of 2-(2'-pyridyl) benzimidazole analogs 1-11 have been carried out and evaluated for in vitro β-glucuronidase inhibitory potential. The compounds 4 (IC50 = 4.06 ± 0.34 µM), 5 (IC50 = 09.63 ± 0.81 µM), 1 (IC50 = 19.66 ± 0.44 µM), 7 (IC50 = 24.75 ± 0.25 µM), 6 (IC50 = 26.30 ± 1.37 µM), and 3 (IC50 = 32.11 ± 0.89 µM), showed β-glucuronidase inhibitory activity superior to the standard D-saccharic acid 1,4-lactone, with (IC50 = 48.4 ± 1.25 µM). Based on structure-activity relationship, we discover a new class of potent β-glucuronidase inhibitors. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index