Antiinflammatory Property of 3-Aryl-5-(n-propyl)-1,2,4-oxadiazoles and Antimicrobial Property of 3-Aryl-5-(n-propyl)-4,5-dihydro-1,2,4-oxadiazoles: Their Syntheses and Spectroscopic Studies

Oxadiazoles

“…Resonances for H5 of 4-unsubstituted 5-alkyl-4,5-dihydro-1,2,4-oxadiazoles appear at 5.4-5.7 ppm [125,162]. Chemical shifts for H5 of 5-alkyl-2,5-dihydro-1,2,4-oxadiazoles have been found at 6.1-6.3 ppm [163].…”

“…[171,172]. For 4,5-dihydro-1,2,4-oxadiazole 134, the C ¼ N absorption is shifted to around 1600 cm À1 [162,173].…”

Synthesis and biological evaluation of 2,5-disubstituted 1,3,4-oxadiazole derivatives with both COX and LOX inhibitory activity

“…Substituted 1,3,4-oxadiazoles have revealed antibacterial 21 , antimycobacterial 22 , antifungal 23 , anti-inflammatory and analgesic [24][25][26] , anticonvulsant 27 , antihyperglycemic 28 , anticancer 29 , anti-HIV-1 30 , and tyrosinase inhibitory activity 31 . 1,2,4-Oxadiazole derivatives have been reported as potent anti-inflammatory agents with selectivity for COX-2 [32][33][34] . 3-Phenyl-1,2,4-oxadiazole derivative has been reported to exhibit analgesic activity far superior than aspirin 35 .…”

“…Therefore, coumarin nucleus that incorporates the styryl carbonyl moiety into a rigid framework was selected to be a part of newly synthesized compounds. Furthermore, coumarin/chromone and related derivatives are recognized as inhibitors of both the mediators of inflammation, that is, LOX and COX pathways of AA metabolism 33,38 . Considering the proinflammatory properties of LTs and prostanoids, agents that are able to block equally the synthesis of both eicosanoids (dual inhibitors) should not only present a superior anti-inflammatory profile but also fewer side effects than NSAIDs and selective COX-2 inhibitors 39 .…”

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

“…Its metabolic profile and the ability to engage in hydrogen bonds give the oxadiazole a bioisosteric relationship with amides and esters (SANTOS FILHO, 2002). Because of the importance of their biological activities, significant progress has been observed in the synthesis of new oxadiazoles aiming to produce analgesics, antispasmodics and anti-inflammatories (SRIVASTAVA et al, 2003).…”