143225-31-4Relevant articles and documents
Benzoxazole and benzothiazole amides as novel pharmacokinetic enhancers of HIV protease inhibitors
Jonckers, Tim H.M.,Rouan, Marie-Claude,Hache, Geerwin,Schepens, Wim,Hallenberger, Sabine,Baumeister, Judith,Sasaki, Jennifer C.
supporting information; experimental part, p. 4998 - 5002 (2012/09/07)
A new class of benzoxazole and benzothiazole amide derivatives exhibiting potent CYP3A4 inhibiting properties was identified. Extensive lead optimization was aimed at improving the CYP3A4 inhibitory properties as well as overall ADME profile of these amide derivatives. This led to the identification of thiazol-5-ylmethyl (2S,3R)-4-(2-(ethyl(methyl)amino)-N-isobutylbenzo[d]oxazole- 6-carboxamido)-3-hydroxy-1-phenylbutan-2-ylcarbamate (C1) as a lead candidate for this class. This compound together with structurally similar analogues demonstrated excellent 'boosting' properties when tested in dogs. These findings warrant further evaluation of their properties in an effort to identify valuable alternatives to Ritonavir as pharmacokinetic enhancers.
Ethylaziridine derivatives and their preparation methods
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, (2008/06/13)
This invention is related to new ethylaziridine derivatives of formula (I) and their preparation. The compounds are useful synthetic intermediates for the synthesis of HIV protease inhibitors and oligopeptide mimetics.
Discovery of a Novel Class of Potent HIV-1 Protease Inhibitors Containing the (R)-(Hydroxyethyl)urea Isostere
Getman, Daniel P.,DeCrescenzo, Gary A.,Heintz, Robert M.,Reed, Kathryn L.,Talley, John J.,et al.
, p. 288 - 291 (2007/10/02)
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