3,4-Dihydropyrimidinone-coumarin analogues as a new class of selective agent against S. aureus: Synthesis, biological evaluation and molecular modelling study

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• 作者：Nirmala S. Naik^a ; Lokesh A. Shastri^a ; ^{drlashastri@kud.ac.in} ; Shrinivas D. Joshi^b ; Sheshagiri R. Dixit^b ; Bahubali M. Chougala^a ; S. Samundeeswari^a ; Megharaj Holiyachi^a ; Farzanabi Shaikh^a ; Jyoti Madar^a ; Rashmi Kulkarni^a ; Vinay Sunagar^c
• 关键词：Coumarin ; Matrix metalloproteinases ; S. aureus ; DNA gyrase ; Gelatin zymography
• 刊名：Bioorganic & Medicinal Chemistry
• 出版年：2017
• 出版时间：15 February 2017
• 年：2017
• 卷：25
• 期：4
• 页码：1413-1422
• 全文大小：1865 K
• 卷排序：25

文摘

An efficient protocol has been developed for the synthesize of dihydropyrimidin-2(1H)-one/thione derivatives of coumarin from substituted 4-formylcoumarins and ethylacetoacetate using urea/thiourea in the presence of catalytic amount of ceric ammonium nitrate. The tested compounds have exhibited promising in vitro potency with low MIC values against the drug susceptive S. aureus strain with low MIC values ranging from 0.2 to 6.25 μg/mL. The in vivo anti-inflammatory potency of all the compounds by gelatin zymography is comparable to that of tetracycline. Biological studies indicate that the synthesized materials to be promising candidates in rational strategy to S. aureus potential risks in general.