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Updated: Jun 12, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Synthesis and molecular modeling studies of 3-chloro-4-substituted-1-(8-hydroxy-quinolin-5-yl)-azetidin-2-ones as
Santosh S Chhajed1, Puranik Manisha, Virupaksha A Bastikar
1Department of Pharmaceutical Chemistry, SMBT College of Pharmacy, Dhamangaon, Dist-Nasik, MS, India. santosh_chhajed@rediffmail.com
Abstract:
A series of 3-chloro-4-substituted-1-(8-hydroxy-quinolin-5-yl)-azetidin-2-ones were synthesized and evaluated for their in vitro anti-filarial activity. To pre-assess the anti-filarial behavior of synthesized compounds (V(a-f)) on a structural basis, automated docking studies were carried out with Molecular Design Suite (MDS v 3.5) into the active site of glutathione-S-transferase (GST) enzyme; scoring functions of these compounds at the active site of the GST enzyme were used for correlation with observed activity. Compounds V(e) and V(f) have shown good affinity for receptor GST, as well as in vitro anti-filarial potency.
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