1417340-01-2Relevant academic research and scientific papers
Inhibitors of HIV-1 attachment. Part 10. the discovery and structure-activity relationships of 4-azaindole cores
Wang, Tao,Yang, Zhong,Zhang, Zhongxing,Gong, Yi-Fei,Riccardi, Keith A.,Lin, Pin-Fang,Parker, Dawn D.,Rahematpura, Sandhya,Mathew, Marina,Zheng, Ming,Meanwell, Nicholas A.,Kadow, John F.,Bender, John A.
, p. 213 - 217 (2013/02/25)
A series of 4-azaindole oxoacetic acid piperazine benzamides was synthesized and evaluated in an effort to identify an oral HIV-1 attachment inhibitor with the potential to improve upon the pre-clinical profile of BMS-378806 (7), an initial clinical compound. Modifications at the 7-position of the 4-azaindole core modulated potency significantly and SAR showed that certain compounds with a 5-membered ring heteroaryl group at that position were the most potent. Four of the compounds with the best profiles were evaluated in a rat pharmacokinetic model and all had superior oral bioavailability and lower clearance when compared with 7.
