非甾体抗炎药取代四氢咔唑衍生物的合成及抗菌活性研究

Mustafa H. Mahdi, A. Dawood, D. Q. Shaheed
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引用次数: 1

摘要

以非甾体抗炎药(NSAIDs)为原料,环己酮(chnn)与苯基肼(p.h.z)反应生成四氢咔唑(THCZ),后者与酮洛芬(NSAID)通过酰胺键反应生成取代的THCZ,通过1H、13C NMR和FTIR光谱对化合物的化学结构进行了验证。通过对接研究和体外实验对合成的化合物进行抑菌活性研究,发现化合物具有较好的抑菌活性,但体外实验也表明化合物的抑菌活性为弱至中等。
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Synthesis and study of antimicrobial activity of some tetrahydrocarbazole derivatives substituted with NSAID
New tetrahydrocarbazole derivatives substituted at the heteroatom (N) by non-steroidal anti-inflammatory drug (NSAIDs) were synthesized by reaction of cyclohehexanon (C.H.N.) with phenyl hydrazine (P.H.Z.) to form tetrahydrocarbazole (THCZ), where the latter is reacted with NSAID (Ketoprofen) via amide bond to yield substituted THCZ, compounds chemical structures were verified by: 1H, 13C NMR and FTIR spectroscopy. Antifungal activity of the synthesized compounds was investigated by docking study and in vitro test to reveal good antifungal activity, but the in vitro test also showed that the compounds have weak to moderate antibacterial activity.
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