کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1357001 | 981184 | 2006 | 11 صفحه PDF | دانلود رایگان |

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.
The synthesis of a series of tricyclic oxazolidinones is disclosed. SAR studies on these novel compounds and evaluation of a lead compound are reported.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry - Volume 14, Issue 23, 1 December 2006, Pages 8032–8042