NOVEL BETULINIC PROLINE IMIDAZOLE DERIVATIVES AS HIV INHIBITORS
The present invention relates to novel betulinic proline imidazole derivatives and related compounds, compositions useful for therapeutic treatment of viral diseases and particularly HIV mediated diseases.
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(2016/01/25)
NOVEL BETULINIC ACID PROLINE DERIVATIVES AS HIV INHIBITORS
The invention relates to novel betulinic acid derivatives and related compounds, and pharmaceutical compositions useful for the therapeutic treatment of viral diseases and particularly HIV mediated diseases. These compounds are esterified in position 3 and are substituted in position 17 of the betulinic acid structure, via a linking group W, by a saturated 5-7 membered nitrogen-heterocycle.
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(2014/07/21)
Synthesis and evaluation of non-dimeric HCV NS5A inhibitors
Based on the symmetrical bidentate structure of the NS5A inhibitor BMS-790052, a series of new monodentate molecules were designed. The synthesis of 36 new non-dimeric NS5A inhibitors is reported along with their ability to block HCV replication in an HCV 1b replicon system. Among them compound 5a showed picomolar range activity along with an excellent selectivity index (SI > 90,000).
Amblard, Franck,Zhang, Hongwang,Zhou, Longhu,Shi, Junxing,Bobeck, Drew R.,Nettles, James H.,Chavre, Satish,McBrayer, Tamara R.,Tharnish, Philip,Whitaker, Tony,Coats, Steven J.,Schinazi, Raymond F.
p. 2031 - 2034
(2013/05/09)
Novel peptidyl carbamate inhibitors of the enzyme elastase
Compounds selected from the group consisting of a compound of the formula STR1 and compound of the formula STR2 wherein x is 1 or 2, Y is carbobenzoxy or benzoyl, and XR is STR3 have use as elastase enzyme inhibitors. Particularly potent are the L-proline diastereomers. Elastase Enzyme inhibitory compositions comprise a carrier and an elastase enzyme inhibiting amount of the compounds of the invention. A method of selectively inhibiting the enzyme elastase in an animal or a human in need of such treatment comprises administering to the animal or human an enzyme elastase inhibiting amount of one of the compounds of the invention or a composition thereof.
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(2008/06/13)
ONE POT SYNTHESIS AND CONFORMATION OF N-t-BUTYLOXYCARBONYL, O-PHENACYL DERIVATIVES OF PROLINE AND OTHER SECONDARY AMINO ACIDS.
Proline, 4-hydroxyproline, azetidine-2-carboxylic acid, pipecolic acid and proline containing dipeptides were converted to N-t-butyloxycarbonyl, O-phenacyl derivatives in a one pot synthesis. 1H- and 13C-NMR spectroscopy of certain derivatives (Boc-Pro-PE
Hondrelis, John,Lonergan, Greg,Voliotis, Stavros,Matsoukas, John
p. 565 - 576
(2007/10/02)
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