FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2023663604> ?p ?o ?g. }

• W2023663604 endingPage "2067" @default.
• W2023663604 startingPage "2060" @default.
• W2023663604 abstract "Systematic modifications of HIV protease inhibitor (2R,3S,4S)-4-[[(benzyloxycarbonyl)-L-valyl]-amino]-3-hydroxy-2-[(4- methoxybenzyl)amino]-5-phenylpentanoyl)-L-valine 2-(aminomethyl)- benzimidazole amide led to a novel series of inhibitors with shortened, modified carboxy terminus. Their synthesis, in vitro enzyme inhibitory data, and antiviral activities are reported. Of particular interest are derivatives featuring the (1S,2R)-1-amino-2-hydroxyindan moiety at the P2'-position since some of them exhibit substantial oral bioavailability in mice. The influence of aqueous solubility and structural parameters on the oral resorption of the inhibitors is discussed. Optimum enhancement of oral bioavailability was observed with L-tert-leucine in P2-position, resulting in the discovery of (2R,3S,4S)-4-[[(benzyloxycarbonyl)-L-tert-leucyl]- amino]-3-hydroxy-2-[(4-methoxybenzyl)amino]-5-phenylpentanoic acid (1S,2R)-1-amino-2-hydroxyindan amide which combines high antiviral activity (IC50 = 250 nM) with a good pharmacokinetic profile (AUC = 82.5 microM.h at a dose of 125 mg/kg po in mice)." @default.
• W2023663604 created "2016-06-24" @default.
• W2023663604 creator A5004847119 @default.
• W2023663604 creator A5014989436 @default.
• W2023663604 creator A5037775787 @default.
• W2023663604 creator A5038950669 @default.
• W2023663604 creator A5046439140 @default.
• W2023663604 creator A5047269655 @default.
• W2023663604 creator A5068790599 @default.
• W2023663604 date "1996-01-01" @default.
• W2023663604 modified "2023-10-13" @default.
• W2023663604 title "Inhibitors of Human Immunodeficiency Virus Type 1 Protease Containing 2-Aminobenzyl-Substituted 4-Amino-3-hydroxy-5-phenylpentanoic Acid: Synthesis, Activity, and Oral Bioavailability" @default.
• W2023663604 cites W1574841922 @default.
• W2023663604 cites W1966966267 @default.
• W2023663604 cites W1970101430 @default.
• W2023663604 cites W1991670386 @default.
• W2023663604 cites W1996325896 @default.
• W2023663604 cites W2013043801 @default.
• W2023663604 cites W2019261111 @default.
• W2023663604 cites W2024180247 @default.
• W2023663604 cites W2028400775 @default.
• W2023663604 cites W2042631213 @default.
• W2023663604 cites W2056213705 @default.
• W2023663604 cites W2063155149 @default.
• W2023663604 cites W2063825413 @default.
• W2023663604 cites W2065631521 @default.
• W2023663604 cites W2131202861 @default.
• W2023663604 cites W2306404279 @default.
• W2023663604 cites W2316906870 @default.
• W2023663604 cites W240501384 @default.
• W2023663604 cites W4211162080 @default.
• W2023663604 doi "https://doi.org/10.1021/jm9508696" @default.
• W2023663604 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/8642565" @default.
• W2023663604 hasPublicationYear "1996" @default.
• W2023663604 type Work @default.
• W2023663604 sameAs 2023663604 @default.
• W2023663604 citedByCount "35" @default.
• W2023663604 countsByYear W20236636042012 @default.
• W2023663604 countsByYear W20236636042013 @default.
• W2023663604 countsByYear W20236636042015 @default.
• W2023663604 countsByYear W20236636042019 @default.
• W2023663604 countsByYear W20236636042020 @default.
• W2023663604 crossrefType "journal-article" @default.
• W2023663604 hasAuthorship W2023663604A5004847119 @default.
• W2023663604 hasAuthorship W2023663604A5014989436 @default.
• W2023663604 hasAuthorship W2023663604A5037775787 @default.
• W2023663604 hasAuthorship W2023663604A5038950669 @default.
• W2023663604 hasAuthorship W2023663604A5046439140 @default.
• W2023663604 hasAuthorship W2023663604A5047269655 @default.
• W2023663604 hasAuthorship W2023663604A5068790599 @default.
• W2023663604 hasConcept C112705442 @default.
• W2023663604 hasConcept C114373084 @default.
• W2023663604 hasConcept C178790620 @default.
• W2023663604 hasConcept C181199279 @default.
• W2023663604 hasConcept C181389837 @default.
• W2023663604 hasConcept C185592680 @default.
• W2023663604 hasConcept C202751555 @default.
• W2023663604 hasConcept C2776568683 @default.
• W2023663604 hasConcept C2776714187 @default.
• W2023663604 hasConcept C2776980637 @default.
• W2023663604 hasConcept C2777056448 @default.
• W2023663604 hasConcept C2777573094 @default.
• W2023663604 hasConcept C2777752497 @default.
• W2023663604 hasConcept C2778439535 @default.
• W2023663604 hasConcept C2778484023 @default.
• W2023663604 hasConcept C515207424 @default.
• W2023663604 hasConcept C55493867 @default.
• W2023663604 hasConcept C71240020 @default.
• W2023663604 hasConcept C71924100 @default.
• W2023663604 hasConcept C98274493 @default.
• W2023663604 hasConceptScore W2023663604C112705442 @default.
• W2023663604 hasConceptScore W2023663604C114373084 @default.
• W2023663604 hasConceptScore W2023663604C178790620 @default.
• W2023663604 hasConceptScore W2023663604C181199279 @default.
• W2023663604 hasConceptScore W2023663604C181389837 @default.
• W2023663604 hasConceptScore W2023663604C185592680 @default.
• W2023663604 hasConceptScore W2023663604C202751555 @default.
• W2023663604 hasConceptScore W2023663604C2776568683 @default.
• W2023663604 hasConceptScore W2023663604C2776714187 @default.
• W2023663604 hasConceptScore W2023663604C2776980637 @default.
• W2023663604 hasConceptScore W2023663604C2777056448 @default.
• W2023663604 hasConceptScore W2023663604C2777573094 @default.
• W2023663604 hasConceptScore W2023663604C2777752497 @default.
• W2023663604 hasConceptScore W2023663604C2778439535 @default.
• W2023663604 hasConceptScore W2023663604C2778484023 @default.
• W2023663604 hasConceptScore W2023663604C515207424 @default.
• W2023663604 hasConceptScore W2023663604C55493867 @default.
• W2023663604 hasConceptScore W2023663604C71240020 @default.
• W2023663604 hasConceptScore W2023663604C71924100 @default.
• W2023663604 hasConceptScore W2023663604C98274493 @default.
• W2023663604 hasIssue "10" @default.
• W2023663604 hasLocation W20236636041 @default.
• W2023663604 hasLocation W20236636042 @default.
• W2023663604 hasOpenAccess W2023663604 @default.
• W2023663604 hasPrimaryLocation W20236636041 @default.
• W2023663604 hasRelatedWork W1992578052 @default.
• W2023663604 hasRelatedWork W2020700034 @default.
• W2023663604 hasRelatedWork W2026927343 @default.

• next