Synthesis and Bio-Evaluation of Novel N-(4-(8-Methoxy-2-Oxo-2H-Chromen-3-Yl) Thiazol-2-Yl) Amide Derivatives

Nilay Shah, P. N. Patel, D. Rajani, Denish C. Karia
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Abstract

In present work, novel derivatives of substituted N-(4-(8-methoxy-2-oxo-2H-chromen-3-yl) thiazol-2-yl) amide have been synthesized. The solvent free reaction of 2-Hydroxy-3-methoxybenzaldehyde with Ethyl acetoacetate in presence of Piperidine catalyst produces 3-acetyl-8-methoxy-2H-chromen-2-one (C). Compound C was α- brominated using CuBr2 and subsequently cyclized using Thiourea to produce 3-(2-aminothiazol-4-yl)-8-methoxy-2H-chromen-2-one as main scaffold (E). This scaffold E was finally reacted with different Acid chloride to isolate title compound derivatives. The chemical structures of synthesized compounds were confirmed by 1H-NMR, FT-IR and Mass spectral/LCMS analysis. The synthesized compounds were screened for potential Antimicrobial, Antifungal and Antimalarial activity.
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新型N-(4-(8-甲氧基-2-氧基- 2h -铬-3-基)噻唑-2-基)酰胺衍生物的合成及生物评价
本文合成了取代的N-(4-(8-甲氧基-2-氧-2- h -铬-3-基)噻唑-2-基)酰胺的新衍生物。在哌替啶催化下,2-羟基-3-甲氧基苯甲醛与乙酰乙酸乙酯无溶剂反应生成3-乙酰基-8-甲氧基- 2h -铬-2- 1 (C),化合物C用CuBr2进行α-溴化,然后用硫脲环化得到3-(2-氨基噻唑-4-基)-8-甲氧基- 2h -铬-2- 1作为主支架(E),该支架E最后与不同的氯化酸反应分离出标题化合物衍生物。通过1H-NMR、FT-IR和质谱/LCMS对合成化合物的化学结构进行了确证。对合成的化合物进行了潜在的抗菌、抗真菌和抗疟疾活性筛选。
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