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Inhibitors of HIV-1 attachment: The discovery and structure-activity relationships of tetrahydroisoquinolines as replacements for the piperazine benzamide in the 3-glyoxylyl 6-azaindole pharmacophore.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2016 Jan 01; Vol. 26 (1), pp. 160-7. Date of Electronic Publication: 2015 Nov 05. - Publication Year :
- 2016
-
Abstract
- 6,6-Fused ring systems including tetrahydroisoquinolines and tetrahydropyrido[3,4-d]pyrimidines have been explored as possible replacements for the piperazine benzamide portion of the HIV-1 attachment inhibitor BMS-663068. In initial studies, the tetrahydroisoquinoline compounds demonstrate sub-nanomolar activity in a HIV-1 pseudotype viral infection assay used as the initial screen for inhibitory activity. Analysis of SARs and approaches to optimization for an improved drug-like profile are examined herein.<br /> (Copyright © 2015 Elsevier Ltd. All rights reserved.)
- Subjects :
- Cell Survival drug effects
Dose-Response Relationship, Drug
HIV Envelope Protein gp120 antagonists & inhibitors
HIV Envelope Protein gp120 genetics
HIV Fusion Inhibitors chemical synthesis
HIV Infections drug therapy
HIV Infections genetics
HeLa Cells
Humans
Molecular Structure
Structure-Activity Relationship
Tetrahydroisoquinolines chemical synthesis
Tetrahydroisoquinolines chemistry
Virus Replication drug effects
Aza Compounds chemistry
Benzamides chemistry
Drug Discovery
HIV Fusion Inhibitors chemistry
HIV Fusion Inhibitors pharmacology
HIV-1 drug effects
Indoles chemistry
Piperazines chemistry
Tetrahydroisoquinolines pharmacology
Virus Attachment drug effects
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 26
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 26584882
- Full Text :
- https://doi.org/10.1016/j.bmcl.2015.11.009