《Design, Synthesis, Biological Evaluation, and X-ray Studies of HIV-1 Protease Inhibitors with Modified P2′ Ligands of Darunavir》 was written by Ghosh, Arun K.; Fyvie, W. Sean; Brindisi, Margherita; Steffey, Melinda; Agniswamy, Johnson; Wang, Yuan-Fang; Aoki, Manabu; Amano, Masayuki; Weber, Irene T.; Mitsuya, Hiroaki. Product Details of 78191-00-1This research focused onxray HIV1 protease inhibitor darunavir; crystal structure; HIV-1 protease inhibitors; P2′ ligands; drug resistance; pharmacokinetics; structure-based design. The article conveys some information:
The structure-based design, synthesis, and biol. evaluation of a series of nonpeptidic HIV-1 protease inhibitors with rationally designed P2′ ligands are described. The inhibitors are designed to enhance backbone binding interactions, particularly at the S2′ subsite. Synthesis of inhibitors was carried out efficiently. The stereochem. of alc. functionalities of the P2′ ligands was set by asym. reduction of the corresponding ketone using (R,R)- or (S,S)-Noyori catalysts. A number of inhibitors displayed very potent enzyme inhibitory and antiviral activity. Inhibitors I and II showed enzyme Ki values of 27.9 and 49.7 pM and antiviral activity of 6.2 and 3.9 nM, resp. These inhibitors also remained quite potent against darunavir-resistant HIV-1 variants. An x-ray structure of inhibitor I in complex with HIV-1 protease revealed key interactions in the S2′ subsite.N-Methoxy-N-methylacetamide(cas: 78191-00-1Product Details of 78191-00-1) was used in this study.
N-Methoxy-N-methylacetamide(cas: 78191-00-1) belongs to anime. Aniline, ethanolamines, and several other amines are major industrial commodities used in making rubber, dyes, pharmaceuticals, and synthetic resins and fibres and for a host of other applications. Most of the numerous methods for the preparation of amines may be broadly divided into two groups: (1) chemical reduction (replacement of oxygen with hydrogen atoms in the molecule) of members of several other classes of organic nitrogen compounds and (2) reactions of ammonia or amines with organic compounds.Product Details of 78191-00-1
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics