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Updated: Aug 6, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Substituent activity relationship studies on new azolo benzoxazepinyl oxazolidinones
Jagattaran Das1, M Sitaram Kumar, D Subrahmanyam
1Anti-infective Group, Discovery Research, Dr. Reddy's Laboratories Ltd., Miyapur, Hyderabad 500 049, India.
Abstract:
In an effort to discover potent antibacterials based on the entropically favored 'bioactive conformation' approach, a series of novel tricyclic molecules mimicking the conformationally constrained structure of Linezolid is reported. Based on the initial tricyclic molecule 1, the benzazepine derivative 2 was designed where the tricyclic structure had more flexibility around C-N bond compared to 1. While, the molecule 2 was less active, the molecule 3 showed promising antibacterial activity presumably after having obtained rigidity due to pyrrole ring. The syntheses, SAR studies, and evaluation of 3 as a lead compound are reported.
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