S. M. Rida, S. A. El‐Hawash, H. Fahmy
2006
Citations
0
Influential Citations
28
Citations
Quality indicators
Journal
Archives of Pharmacal Research
Abstract
A novel series of 1-(1-benzofuran-2-yl-ethylidene)-4-substituted thiosemicarbazides (2a-d) along with some derived ring systems: substituted-2,3-dihydro-thiazoles (3a-c, 4a-f) and thiazolidin-4-ones (5a-d and6a-d), were synthesized. In addition, cyanoacetic acid-(1-benzofuran-2-yl-ethylidene) hydrazide (7) was used to prepare another new series of compounds consisting of substituted pyridin-2)1H)-ones (8a-c); 2-thioxo-2,3-dihydro-thiazoles (9a-d) and 2-thioxo-2,3-dihydro-6H-thiazolo[4,5-d]pyrimidin-7-ones (10a-c, 11a-c). The absolute configuration of compound5c was determined by X-ray crystallography. The compounds prepared were evaluated for theirin vitro anti-HIV, anticancer, antibacterial, and antifungal activities. Among the tested compounds, compounds5c and9a produced a significant reduction H 2 the viral cytopathic effect (93.19% and 59.55%) at concentrations >2.0×10−4 M and, 2.5×10−5 M respectively. Compound9a was confirmed to have moderate anti-HIV activity. Compounds2a, 2d, and5c showed mild antifungal activity. However, none of the tested compounds showed any significant anticancer activity.