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

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 c...

Full description

Bibliographic Details
Main Authors: Kinjal D. Patel, Rajesh H. Vekariya, Neelam P. Prajapati, Dhaval B. Patel, Hitesh D. Patel, Tauhid Shaikh, Dhanji P. Rajani, Smita Rajani, Naumita S. Shah, Devendrasinh Jhala
Format: Article
Language:English
Published: Elsevier 2020-01-01
Series:Arabian Journal of Chemistry
Online Access:http://www.sciencedirect.com/science/article/pii/S187853521830056X
Description
Summary: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
ISSN:1878-5352