192214-00-9Relevant articles and documents
Design of novel HIV-1 protease inhibitors incorporating isophthalamide-derived P2-P3 ligands: Synthesis, biological evaluation and X-ray structural studies of inhibitor-HIV-1 protease complex
Ghosh, Arun K.,Brindisi, Margherita,Nyalapatla, Prasanth R.,Takayama, Jun,Ella-Menye, Jean-Rene,Yashchuk, Sofiya,Agniswamy, Johnson,Wang, Yuan-Fang,Aoki, Manabu,Amano, Masayuki,Weber, Irene T.,Mitsuya, Hiroaki
, p. 5114 - 5127 (2017/09/26)
Based upon molecular insights from the X-ray structures of inhibitor-bound HIV-1 protease complexes, we have designed a series of isophthalamide-derived inhibitors incorporating substituted pyrrolidines, piperidines and thiazolidines as P2-P3 ligands for specific interactions in the S2-S3 extended site. Compound 4b has shown an enzyme Ki of 0.025 nM and antiviral IC50 of 69 nM. An X-ray crystal structure of inhibitor 4b-HIV-1 protease complex was determined at 1.33 ? resolution. We have also determined X-ray structure of 3b-bound HIV-1 protease at 1.27 ? resolution. These structures revealed important molecular insight into the inhibitor–HIV-1 protease interactions in the active site.
Nitrilase-catalyzed enantioselective synthesis of pyrrolidine- And piperidinecarboxylic acids
Winkler, Margit,Meischler, Dorith,Klempier, Norbert
, p. 1475 - 1480 (2008/09/16)
The enantioselective synthesis of the nonproteinogenic amino acids β-proline and nipecotic acids from their readily available nitriles is achieved in high enantiomeric excess by commercially available nitrilases. The presented procedure comprises not more than 4 steps, thus considerably reducing the multiple steps generally required. Amide formation is also observed for specific heterocyclic nitriles.
Constrained β-alanine based GpIIb/IIIa antagonists
Klein, Scott I.,Czekaj, Mark,Molino, Bruce F.,Valeria, Chu
, p. 1773 - 1778 (2007/10/03)
The concepts of centrally constrained and peptide based fibrinogen receptor antagonists have been successfully combined into a single series of analogs which have been demonstrated to be potent inhibitors of platelet aggregation.
