An efficient synthesis of hydroxyethylene dipeptide isosteres: the core unit of potent HIV-1 protease inhibitors
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چکیده
منابع مشابه
Design and synthesis of HIV-1 protease inhibitors incorporating oxazolidinones as P2/P2' ligands in pseudosymmetric dipeptide isosteres.
A series of novel HIV-1 protease inhibitors based on two pseudosymmetric dipeptide isosteres have been synthesized and evaluated. The inhibitors were designed by incorporating N-phenyloxazolidinone-5-carboxamides into the hydroxyethylene and (hydroxyethyl)hydrazine dipeptide isosteres as P2 and P2' ligands. Compounds with (S)-phenyloxazolidinones attached at a position proximal to the central h...
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چکیده ندارد.
Design of new potent HTLV-1 protease inhibitors: in silico study
HTLV-1 and HIV-1 are two major causes for severe T-cell leukemia disease and acquired immune deficiency syndrome (AIDS). HTLV-1 protease, a member of aspartic acid protease family, plays important roles in maturation during virus replication cycle. The impairment of these proteases results in uninfectious HTLV-1virions.Similar to HIV-1protease deliberate mutations that confer drug resistance on...
متن کاملP - 03 towards the Synthesis of Monofluoroalkene - Based Dipeptide Isosteres
Phenols are attractive starting materials for organic synthesis due to their availability from both petrochemical and renewable sources, and their ubiquity in natural products and biologically active molecules. Nevertheless, direct methods for their functionalization often suffer from poor selectivity or poor atom-economy. This presentation will describe recent efforts from our group to develop...
متن کاملHIV-1 protease inhibitors.
Treatment of human immunodeficiency virus type 1 (HIV-1) infection with regimens that include protease inhibitors (PIs) has contributed to marked improvements in HIV-related disease progression and mortality. Five PIs are approved by the US Food and Drug Administration and have potent activity in vitro. PIs with 2 nucleoside analogue reverse transcriptase inhibitors have demonstrated prolonged ...
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ژورنال
عنوان ژورنال: The Journal of Organic Chemistry
سال: 1991
ISSN: 0022-3263,1520-6904
DOI: 10.1021/jo00023a009