合成 3-(2-氯乙基)-2-甲基-6,7,8,9-四氢-4H-吡啶并[1,2-a]嘧啶-4-酮衍生物作为抗菌剂。

Synthesis of 3-(2-chloroethyl)-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2- a] pyrimidin-4-one derivatives as antibacterial agents.

机构信息

Department of Studies in Chemistry, University of Mysore Manasagangotri Mysore-570006, India.

出版信息

Med Chem. 2013 Mar;9(2):240-8. doi: 10.2174/1573406411309020008.

DOI:10.2174/1573406411309020008

Abstract

A series of novel 3-(2-chloroethyl)-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one aliphatic/ aromatic/ heterocyclic amine derivatives were synthesized in good yield. The synthesized compounds were characterized by 1H-NMR, FTIR and elemental analysis. All the synthesized compounds were screened for their in vitro antibacterial activity by agar well diffusion and micro dilution method against standard strains of Gram-Positive (Bacillus Subtilis MTCC 121 and Staphylococcus epidermidis 435), and Gram-negative (Xanthomonas Campestris 7903 and Pseudomonas aeruginosa MTCC 7908) bacteria. Compounds with substituted heterocyclic piperazine moiety showed good activity. In particular, compound 6i showed two fold better activity compared to the standard drug Strepyomycin sulphate.

摘要

合成了一系列新型 3-(2-氯乙基)-2-甲基-6,7,8,9-四氢-4H-吡啶并[1,2-a]嘧啶-4-酮脂肪族/芳族/杂环胺衍生物，产率较高。通过 1H-NMR、FTIR 和元素分析对合成的化合物进行了表征。采用琼脂孔扩散法和微量稀释法，对所有合成的化合物进行了体外抗菌活性筛选，以对抗革兰氏阳性（枯草芽孢杆菌 MTCC 121 和表皮葡萄球菌 435）和革兰氏阴性（野油菜黄单胞菌 7903 和铜绿假单胞菌 MTCC 7908）细菌的标准菌株。带有取代杂环哌嗪部分的化合物表现出良好的活性。特别是，化合物 6i 的活性比标准药物硫酸链霉素高两倍。