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Synthesis and biological evaluation of novel small non-peptidic HIV-1 PIs: the benzothiophene ring as an effective moiety.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2012 Apr 15; Vol. 22 (8), pp. 2948-50. Date of Electronic Publication: 2012 Feb 23. - Publication Year :
- 2012
-
Abstract
- Synthesis and biological evaluation of a new series of potential HIV-1 protease inhibitors incorporating different heterocycles are described. The variation of heteroatom in such molecules has displayed totally different biological activities and a benzothiophene containing inhibitor has shown high potency against wild type HIV-1 protease with IC(50)=60 nM, thanks to the lower desolvation penalty to be payed by such hydrophobic moiety.<br /> (Copyright © 2012 Elsevier Ltd. All rights reserved.)
- Subjects :
- Antiviral Agents chemistry
HIV Protease Inhibitors chemistry
Heterocyclic Compounds chemistry
Heterocyclic Compounds pharmacology
Humans
Inhibitory Concentration 50
Molecular Structure
Thiophenes chemistry
Thiophenes pharmacology
Antiviral Agents chemical synthesis
Antiviral Agents pharmacology
HIV Protease Inhibitors chemical synthesis
HIV Protease Inhibitors pharmacology
HIV-1 drug effects
Heterocyclic Compounds chemical synthesis
Thiophenes chemical synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 22
- Issue :
- 8
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 22414613
- Full Text :
- https://doi.org/10.1016/j.bmcl.2012.02.046