Synthesis and Antimicrobial Activity of Fluorine Containing Pyrazole-clubbed Dihydropyrimidinones

被引:26
作者
Desai, N. C. [1 ]
Vaghani, H. V. [2 ]
Patel, B. Y. [1 ]
Karkar, T. J. [1 ]
机构
[1] Maharaja Krishnakumarsinhji Bhavnagar Univ, Dept Chem DST FIST Sponsored & UGC NON SAP, Div Med Chem, Mahatma Gandhi Campus, Bhavnagar 364002, Gujarat, India
[2] Ganpat Univ, Dept Chem, Mehsana Urban Inst Sci, Ganpat Vidyanagar 384012, India
关键词
Pyrazole; dihydropyrimidinones; Biginelli adduct; antimicrobial screening; cytotoxicity; POTENTIAL ANTITUBERCULAR AGENTS; CALCIUM-CHANNEL BLOCKERS; BIOLOGICAL EVALUATION; MEDICINAL CHEMISTRY; IN-VITRO; DERIVATIVES; INHIBITORS; THIAZOLE; ANALOGS;
D O I
10.4172/pharmaceutical-sciences.1000351
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
In the present communication synthesis of pyrazole-containing dihydropyrimidinone motifs (4a-o) and their antimicrobial activity and cytotoxicity were reported. The newly synthesized compounds were characterized using infrared, proton nuclear magnetic resonance, carbon-13 nuclear magnetic resonance and mass spectral techniques. Compounds 4b, 4c, 4f, 4g, 4i and 4j were the most active derivatives identified during antimicrobial activity screening. On the basis of antibacterial activities, it was observed that compounds 4b and 4c exhibited activity against methicillin resistant Staphylococcus aureus with minimum inhibitory concentrations of 12.5 and 6.25 mu g/ml, respectively. From structure activity relationship studies, it could be concluded that electron withdrawing groups played a crucial role in enhancing antimicrobial and cytotoxic effects of title compounds. In addition, the results of the cytotoxicity studies indicated that compounds 4b, 4c, 4g and 4j possessed lower levels of cytotoxicity.
引用
收藏
页码:242 / 252
页数:11
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