Synthesis of N'-(Quinazolin-4-yl)isonicotinohydrazides and their biological screening, docking and ADME studies

Abstract

A wide range of 4-chloro-3,4-dihydroquinazolines hybrid isoniazid derivatives were synthesised efficiently via reaction of 4-chloro-3,4-dihydroquinazolines with isoniazid in the presence of catalytic amount of N,N-diisopropylethylamine (DIPEA) under refluxing methanol. All the title molecules were characterized by 13C NMR, 1H NMR, Mass and IR spectroscopy. All the compounds were tested for anti-malarial, anti-microbial and anti-tuberculosis activities. They were further tested for the cytotoxic feature. In-silico molecular docking study and ADME properties were also studied for the title molecules. Keywords: Molecular hybridization, Anti-malarial, Anti-microbial, Anti-tuberculosis, MTT assay, Docking, ADME