217490-11-4Relevant academic research and scientific papers
A synthetic route to a novel type of conformationally constrained N-aryloxazolidinones
Griera, Rosa,Cantos-Llopart, Carme,Amat, Mercedes,Bosch, Joan,Del Castillo, Juan-C.,Huguet, Joan
, p. 2515 - 2517 (2005)
The synthesis of N-aryloxazolidinone 1, a conformationally constrained analog of linezolid embodying a tricyclic pyrrolo[1,2-a][4,1]benzoxazepine moiety as the N-aryl substituent, is reported. The synthetic route involves the successive construction of th
Substituent activity relationship studies on new azolo benzoxazepinyl oxazolidinones
Das, Jagattaran,Sitaram Kumar,Subrahmanyam,Sastry,Prasad Narasimhulu,Laxman Rao,Kannan,Roshaiah,Awasthi, Riti,Patil, Santosh N.,Sarnaik,Rao Mamidi,Selvakumar,Iqbal, Javed
, p. 8032 - 8042 (2007/10/03)
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.
