Synthesis and biological evaluation of some 1,3,4-oxadiazole derivatives

被引:137
|
作者
Manjunatha, K. [1 ]
Poojary, Boja [1 ]
Lobo, Prajwal L. [1 ]
Fernandes, Jennifer [2 ]
Kumari, N. Suchetha [3 ]
机构
[1] Mangalore Univ, Dept Chem, Mangalagangothri 574199, Karnataka, India
[2] NGSM Coll Pharm, Dept Pharmachem, Derlakatte 574160, Karnataka, India
[3] KS Hegde Med Acad, Dept Biochem, Derlakatte 574162, Karnataka, India
关键词
1,3,4-Oxadiazol-2-thiones; Ibuprofen; 4-Methylthiophenyl; Antimicrobial activity; Anti-inflammatory activity; NONSTEROIDAL ANTIINFLAMMATORY DRUGS; ANTIMICROBIAL ACTIVITIES; CIPROFLOXACIN;
D O I
10.1016/j.ejmech.2010.08.039
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The acid hydrazides (2) derived from ibuprofen and 4-methylthiophenyl acetic acids have been subjected to cyclization with carbon disulphide under basic conditions to yield 1,3,4-oxadiazol-2-thiones (3) which on aminomethylation with formaldehyde and secondary amines afforded a series of Mannich bases (4 and 5). Purity of the compounds has been confirmed by TLC. Structures of these compounds were established on the basis of elemental analyses and spectral studies. The newly synthesized compounds were evaluated for their anti-inflammatory, analgesic, ulcerogenic and antimicrobial activities. (C) 2010 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码:5225 / 5233
页数:9
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