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KMID : 0043320060290010016
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Archives of Pharmacal Research
2006 Volume.29 No. 1 p.16 ~ p.25
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Synthesis and In Vitro Evaluation of Some Novel Benzofuran
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Samia M. Rida
Soad A. M. El-Hawash
Aly A. Hazza
Hesham T. Y. Fahmy
Mostafa M. M. El-Meligy
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Abstract
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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 and 6a-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 compound 5c was determined by X-ray crystallography. The compounds prepared were evaluated for their in vitro anti-HIV, anticancer, antibacterial, and antifungal activities. Among the tested compounds, compounds 5c and 9a produced a significant reduction ㅐㄹthe viral cytopathic effect (93.19% and 59.55%) at concentrations >2.0×10-4 M and 2.5×10-5 respectively. Compound 9a was confirmed to have moderate anti-HIV activity. Compounds 2a, 2d, and 5c showed mild antifungal activity. However, none of the tested compounds showed any significant anticancer activity.
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KEYWORD
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2-Acetylbenzofuran, Thiosemicarbazides, Caynoacetic acid hydrazide, Dihydro-thiazole, Pyridin-2(1H)-ones, Thiazolo[4,5-d]pyrimidines, Anti-HIV-1, Anticancer, Antimicrobial activity
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