Synthesis and QSAR Study of Novel N-(3-chloro-2-oxo-4-substituted azetidin-1-yl) isonicotinamide derivatives as Anti mycobacterial Agents

A series of N-(3-chloro-2-oxo-4-substituted azetidin-1-yl) isonicotinamide 2(a-j) have been synthesized under microwave irradiation and evaluated for their in vitro anti-mycobacterial activity against M. tuberculosis H37Rv using tube dilution method. Some of the compounds exhibited a significant anti mycobacterial activity when compared with first line drugs such as isoniazid (INH) and rifampicin (RIP).Stepwise multiple linear regression analysis was performed to derive QSAR models which were further evaluated for statistical significance and predictive power by internal and external validation. The QSAR model indicate that the thermodynamic descriptors (Molar refractivity), electronic descriptors (dipole moment), principal moment inertia, play an important role for anti mycobacterial activities.

Author(s): Anna Pratima G. Nikaljea, Mudassir Pathan, Ashok S. Narute, Mangesh S. Ghodke and D. Rajani

Abstract | PDF

Share This Article