Screening and evaluation of multi drug resistance activity of various 1,2,4-triazoles derivatives through in vitro anti tubercular

Abstract

Isoniazid (Isonicotinic acid hydrazide, INH) has been significantly used to treat Mycobacterium tuberculosis. Introduction of drugs like INH, Rifmapicin, Pyrazinamide and Streptomycin resulted in rapid decline in TB cases worldwide. Several factors lead to the emergence of resistant strains of Mycobacterium tuberculosis. HIV infection also contributed to the escalating burden of tuberculosis. In the present examination 1,2,4-triazole subordinates were planned, incorporated and exposed to in vitro antitubercular screening against Mycobacterium tuberculosis H37Rv.Lipophilicity (log P) of the compounds were also determined to establish a correlation ship between physicochemical properties and antitubercular activity. Mtb CYP121 and CYP125 are considered to be potential targets for drug design. Binding study of azoles with these enzymes have also been reported. However, enough reports are not available on Mtb CYP-ligand binding requirements to improve the MIC of Azole based antitubercular agents. Hence we conducted the docking study of our synthesized triazoles against both Mtb CYP 121 and CYP125 to establish a correlationship between antitubercular activity and receptor binding interactions. In this paper we discuss about the molecular docking studies of the synthesized mercapto and benzthio 1,2,4-triazole compounds 13-18 with different enzyme target which we have employed.