Gaonkar S L, Rai K M L, Prabhuswamy B
Department of Studies in Chemistry, University of Mysore, Manasagangotri, India.
Eur J Med Chem. 2006 Jul;41(7):841-6. doi: 10.1016/j.ejmech.2006.03.002. Epub 2006 Apr 17.
A series of novel 2-[4-[2-(5-ethylpyridin-2-yl)ethoxy]phenyl]-5-substituted-1,3,4-oxadiazoles were synthesized by the oxidative cyclisation of hydrazones derived from 4-[2-(5-ethylpyridin-2-yl)ethoxy]benzaldehyde and aroylhydrazines using chloramine-T as oxidant. IR, NMR and elemental analysis characterized the newly synthesized compounds. The synthesized compounds were evaluated for their antimicrobial activity and were compared with standard drugs. The compounds demonstrated potent to weak antimicrobial activity. Out of the compounds studied, compounds 8c and 8d showed significant inhibition. Compounds 8b, 8f, 8k and 8e showed moderate activity. The minimum inhibitory concentration of the compounds was in the range of 8-26 microg ml(-1) against bacteria and 8-24 microg ml(-1) against fungi. The title compounds represent a novel class of potent antimicrobial agents.
以对氯苯磺酰胺为氧化剂，通过4-[2-(5-乙基吡啶-2-基)乙氧基]苯甲醛与芳酰肼衍生的腙的氧化环化反应，合成了一系列新型的2-[4-[2-(5-乙基吡啶-2-基)乙氧基]苯基]-5-取代-1,3,4-恶二唑。通过红外光谱、核磁共振和元素分析对新合成的化合物进行了表征。对合成的化合物进行了抗菌活性评估，并与标准药物进行了比较。这些化合物表现出强效至弱效的抗菌活性。在所研究的化合物中，化合物8c和8d表现出显著的抑制作用。化合物8b、8f、8k和8e表现出中等活性。这些化合物对细菌的最低抑菌浓度在8-26微克/毫升范围内，对真菌的最低抑菌浓度在8-24微克/毫升范围内。标题化合物代表了一类新型的强效抗菌剂。
