136740-99-3Relevant academic research and scientific papers
Expedient solid-phase synthesis of both symmetric and asymmetric diol libraries targeting aspartic proteases
Shi, Haibin,Liu, Kai,Leong, Wendy W.Y.,Yao, Shao Q.
supporting information; experimental part, p. 3945 - 3948 (2010/03/30)
C2-symmetric diols have been shown to be highly potent against HIV-1 protease (PR). However, gaining access to these compounds has been hampered by the need of multistep solution-phase reactions which are often tedious and inefficient. In this Letter, we have disclosed a solid-phase strategy for rapid preparation of small molecule-based, symmetric and asymmetric diols as potential HIV-1 protease inhibitors. Upon biological screening, we found one of them, SYM-5, to be a potent and selective inhibitor (Ki = 400 nM) against HIV-1 protease.
Inhibitors of retroviral proteases
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, (2008/06/13)
The present invention relates to compounds of the formula I STR1 wherein A, Y, R2, R3, R4, R5, R6, l, m and the corresponding radicals labeled with * are defined as stated in the description, a process for their preparation and their use for the inhibition of retroviral proteases.
Dipeptide Isosteres. 1. Synthesis of Dihydroxyethylene Dipeptide Isosteres via Diastereoselective Additions of Alkyllithium Reagents to N,N-Dimethylhydrazones. Preparation of Renin and HIV-1 Protease Inhibitor Transition-State Mimics
Baker, William R.,Condon, Stephen L.
, p. 3277 - 3284 (2007/10/02)
The amino and diamino dihydroxyethylene dipeptide isosteres 19a,b and 23 are important intermediates for the preparation of inhibitors of human renin and HIV-1 protease, respectively.A general synthetic strategy was developed to access both dipeptide isos
