Design, synthesis and biological evaluation of benzoxazole derivatives as new antiinflammatory agent


ABSTRACT:

New series of methyl 2-(arylideneamino) benzoxazole -5-carboxylate derivatives were synthesized by the reaction of Schiff bases of methyl 2-aminobenzoxazole-5-carboxylate with appropriate aromatic aldehydes. The chemical structures of the synthesized compounds were confirmed by means of IR, 1HNMR, mass spectral analysis. Further, the synthesized compounds (SH1-SH9) were screened for antiinflammatory activity by using Carrageenan – induced paw edema rat model. The results showed that, compounds SH1-SH3 and SH6-SH8 were significantly (p
<0.0001) reduced the inflammation there by showed a promising antiinflammatory activity; where as the compound SH5 moderately reduced the inflammation. Only the two compounds i.e SH4 and SH9 showed very poor anti-inflammatory activity towards Carrageenan – induced paw edema rat. 

Introduction:

 Recent observations suggest that substituted benzoxazoles and related heterocycles, possess potential activity with lower toxicities in the chemotherapeutic approach in man.Careful literature survey revealed that targets containing benzoxazole moiety, either isolated from plants or accessed by total synthesis, have remarkable biological activities. For example, antimicrobial, antihistaminic, antiparasitics, herbicidal, antiviral, antiallergic and antihelmintic activities. Antiinflammatory activity of benzoxazole derivatives were also reported in the literature. The title compounds were synthesized by treating the methyl 2- aminobenzoxazole-5-carboxylate with appropriate aromatic aldehydes to get a new series of methyl 2- (arylideneamino) benzoxazole -5-carboxylate derivatives (SH1-AH9).

Further details @ http://www.jocpr.com/

For more details @ http://www.jocpr.com/articles/design-synthesis-and-biological-evaluation-of-benzoxazole-derivatives-as-new-antiinflammatory-agents.pdf

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