Abstract
Background: Twenty one amide compounds possessing phenoxy/benzyloxy/pyridinylgroups have been synthesized by benzoylation of respective amines in presence of base with moderateto encouraging yields. Upon confirmation of structure, compounds were subjected for p38 kinase inhibitory,anti-inflammatory, antimicrobial and antitubercular activities.Method: Anti-inflammatory activity was determined using carrageenan induced rat paw edema modelwhile p38 kinase inhibitory activity was studied using ELISA method and serial dilution method wasemployed to determine MICs. Two compounds 4g and 4n showed over 30% p38 kinase inhibitory activityat 10 μM and best anti-inflammatory activity was found for compounds 4g, 4i, 4n and 4o whichexhibited to reduce paw edema over 70%. Compound 4b was observed to be the most potent againstgram +ve organisms with MIC value of 1.6 μG/mL and compound 4u displayed potent antibacterialactivity against gram negative organisms.Conclusion: Most encouraging antitubercular activity was noticed for compounds 4u, 4r and 4k with6.25, 12.5 and 12.5 μG/mL Further, in order to know the binding site interactions, a docking simulationsof compounds was performed. These preliminary results will certainly show fruitful directions toimprove the activities of compounds.
NSTL
Bentham Science Publ Ltd