Synthesis of Some Novel Oxadiazole and Oxadiazoline Analogues for Their Antiinflammatory Activity

Abstract

The search for newer non-steroidal antiin‰ammatory drugs (NSAIDs) and the importance of oxadiazoles as antiin‰ammatory agents prompted us to undertake the synthesis of some novel oxadiazole and related analogues with unreported antiin‰ammatory activities. The antiin‰ammatory potential of the compounds was investigated using the carrageenan-induced rat paw edema method and cotton pellet-induced granuloma method. Some compounds demonstrated marked antiin‰ammatory activities. The antiin‰ammatory activity of oxadiazoles at doses of 100 mg/kg was shown by their ability to provide 28 55％, 21 36％, and 27 49％ protection against carrageenan-induced rat paw edema, moist cotton pellet-induced, and dry cotton pellet-induced granuloma, respectively. On the other hand, the antiin‰ammatory properties of oxadiazolines at doses of 100 mg/kg was re‰ected by their ability to provide 15 47％, 22 39％, and 23 47 ％ protection against carrageenan-induced rat paw edema, moist cotton pellet-induced, and dry cotton pellet-induced granuloma, respectively. Structure-activity relationships among synthesized compounds were also studied.

Design and synthesis of some novel 3-[5-(4-substituted) phenyl-1,3,4-oxadiazole-2yl]-2-phenylquinazoline-4(3H)-ones as possible anticonvulsant agent

“…Substituted aryl semicarbazones (2) were prepared according to the method reported in the literature using semicarbazide hydrochloride and substituted aldehydes in alcohol (Furniss et al, 2005a, b). 2-Amino-5-aryl-1,3,4-oxadiazoles (3) were prepared by cyclization of semicarbazones of the corresponding aromatic aldehydes in the presence of bromine in glacial acetic acid (Rajak et al, 2007). N-benzoyl anthranilic acid (5) was prepared by reaction of anthranilic acid with benzoyl chloride.…”

Synthesis, anticonvulsant and neurotoxic activity of some new 2,5-disubstituted-1,3,4-oxadiazoles

“…Substituted aryl semicarbazones were prepared according to the method reported in the literature using semicarbazide hydrochloride and substituted aldehydes in alcohol (Furniss et al, 2005a). 2-Amino-5-aryl-1,3,4-oxadiazoles (1) were prepared by cyclization of semicarbazones of the corresponding aromatic aldehydes in the presence of bromine in glacial acetic acid (Rajak et al, 2007). Substituted oxadiazole amines (1) were treated with sodium cyanate in the presence of glacial acetic acid according to the known urea method to yield substituted phenyl urea derivatives (2) (Furniss et al, 2005b).…”

Relationship Between the structure of Newly Synthesized derivatives of 1,3,4-oxadiazole Containing 2-Methylphenol and their Antioxidant and Antibacterial Activities

“…Recently, 1,3,4-oxadiazoles derivatives exhibited broad spectrum of biological activates likewise antitumor 16 ,antiproliferative 17 , a-glucosidase inhibitors 18 ,anti-inflammatory [19][20][21] ,antibacterial 22 , antifungals 23,24 as well the antioxidant ability [25][26][27] . Many researchers have reported that the substituent group at ortho of phenols possess directly control to improve or disprove the antioxidant capacity [28][29][30][31][32] .…”