Ranganatha V Lakshmi, Begum A Bushra, Naveen P, Zameer Farhan, Hegdekatte Raghavendra, Khanum Shaukath Ara
Department of Chemistry, Yuvaraja's College (Autonomous), University of Mysore, Mysore, Karnataka, India.
Arch Pharm (Weinheim). 2014 Aug;347(8):589-98. doi: 10.1002/ardp.201400058. Epub 2014 May 22.
A series of novel 2-(diaryl methanone)-N-(4-oxo-2-phenyl-thiazolidin-3-yl)-acetamides were synthesized by various Schiff bases of (4-benzoyl-phenoxy)-aceto hydrazide with thioglycolic acid. The structures of the newly synthesized compounds were confirmed by IR, (1) H NMR, mass spectra, and C, H, N analysis. Further, all the synthesized compounds 9a-n were evaluated for xanthine oxidase (XO) inhibition and antioxidant properties. Among all the tested compounds, 9f, 9m, and 9n demonstrated potent XO inhibition of 52, 76, and 26%, respectively, compared to the standard drug allopurinol, which is evident from in vitro and in silico analysis. On the other hand, compounds 9c, 9d, and 9k exhibit potent antioxidant properties.
通过(4-苯甲酰基-苯氧基)-乙酰肼与巯基乙酸的各种席夫碱合成了一系列新型的2-(二芳基甲酮)-N-(4-氧代-2-苯基-噻唑烷-3-基)-乙酰胺。通过红外光谱、¹H核磁共振、质谱以及碳、氢、氮分析确定了新合成化合物的结构。此外,对所有合成的化合物9a-n进行了黄嘌呤氧化酶(XO)抑制和抗氧化性能评估。在所有测试化合物中,与标准药物别嘌醇相比,9f、9m和9n分别表现出52%、76%和26%的强效XO抑制作用,这在体外和计算机模拟分析中都很明显。另一方面,化合物9c、9d和9k表现出强效的抗氧化性能。