- Inhibitors of HIV-1 attachment. Part 10. the discovery and structure-activity relationships of 4-azaindole cores
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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.
- 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.
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p. 213 - 217
(2013/02/25)
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- Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives
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This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.
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