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...

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Bibliographic Details
Published in:Arabian journal of chemistry 2020-01, Vol.13 (1), p.1986-2000
Main Authors: Patel, Kinjal D., Vekariya, Rajesh H., Prajapati, Neelam P., Patel, Dhaval B., Patel, Hitesh D., Shaikh, Tauhid, Rajani, Dhanji P., Rajani, Smita, Shah, Naumita S., Jhala, Devendrasinh
Format: Article
Language:English
Subjects:
ADME
Anti-malarial
Anti-microbial
Anti-tuberculosis
Docking
Molecular hybridization
MTT assay
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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.
ISSN:1878-5352
1878-5379
DOI:10.1016/j.arabjc.2018.02.017