Synthesis, anti-inflammatory and antimicrobial activities of new 1,2,4-oxadiazoles peptidomimetics

Oxadiazoles

“…Succinic [199] and glutaric anhydrides [200] are excellent substrates for reaction with amidoximes, giving 1,2,4-oxadiazol-5-yl carboxylic acids 141 and 142, respectively: the obtained compounds are excellent substrates for coupling to amino acid derivatives (Scheme 13.47).…”

1,2,4-oxadiazole: A Brief Review from the Literature About the Synthesis and Pharmacological Applications

“…The compounds with decapentil group in C5 of 1,2,4-oxadiazole have higher anti-inflammatory activity , because the compounds with longer hydrocarbon chains are able to enter in cells more quickly, and leave more slowly than those with shorter chains, due to its increased hydrophobicity , or perhaps, the smaller molecules , such as isopropyl group at C5, for example, are excreted more rapidly. Some 1,2,4-oxadiazole peptidomimetic ( Figure 4) were also tested for their antiinflammatory activity by Leite et al (2000). The compounds 3a, 3b, 3c, 3d, 3f and 3g significantly inhibited the induced edema by carrageenan in rat´s paw, depending on the dose employed.…”

A Convenient Synthesis and Cytotoxic Activity of 3-Aryl-5-Pentyl-1,2,4-Oxadiazoles From Carboxylic Acid Esters and Arylamidoximes Under Solvent-Free Conditions

“…6 Biologically relevant compounds containing the 1,2,4-oxadiazole moiety also include HIV integrase inhibitors, 7 antituberculostatic agents 8 and antikinetoplastid agents. 9 They are also reported as inhibitors of tyrosine kinase, 10 bacterial and human DNA topoisomerases, 11 and human neutrophil elastase. 12 Many 1,2,4-oxadiazoles 3,5-disubstituted have been shown to be bioactive compounds.…”