Synthesis and characterization of 6, 6-dimethyl-6, 7-dihydro-5H-pyrazolo [5, 1-b] [1, 3] oxazine-3-carboxamide derivatives as PDE-4 inhibitors for the treatment of anti-inflammatory, analgesic and antimicrobial activities

Vikash Srivastava, Prof. Surya Pal Singh

Anti-inflammatory, analgesic, anti-bacterial, 6, 6-dimethyl-6, 7-dihydro-5H-pyrazolo [5, 1-b] [1, 3] oxazine-3-carboxamide, PDE4 inhibitor

We reveal a series of novel 6, 6-dimethyl-6, 7-dihydro-5H-pyrazolo [5, 1-b] [1, 3] oxazine- 3- carboxamide derivatives as PDE4 inhibitor for the treatment of inflammatory, analgesic and antimicrobial diseases. All compounds were evaluated for their anti-inflammatory, analgesic (compared to the reference drug Indomethacin) and antimicrobial activities (compared to the reference drug Ampicillin and Fluconazole). Compounds 5e, 5f, and 5g were found to be the more active anti-inflammatory drugs revealing potency ranging from 1 - 1.01 compared to the reference drug indomethacin. In accumulation of docking study of these highly active 3 compounds against the active site of cyclooxygenase-2 enzyme (COX-2), among the established compounds. Compounds 5e, 5f, and 5g showed multiple activities; anti-inflammatory, analgesic and anti-bacterial activities.

https://dx.doi.org/10.31873/IJEAS.7.07.07