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Design of a series of bicyclic HIV-1 integrase inhibitors. Part 2: azoles: effective metal chelators.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2010 Oct 01; Vol. 20 (19), pp. 5909-12. Date of Electronic Publication: 2010 Jul 27. - Publication Year :
- 2010
-
Abstract
- Synthesis of a diverse set of azoles and their utilizations as an amide isostere in the design of HIV integrase inhibitors is described. The Letter identified thiazole, oxazole, and imidazole as the most promising heterocycles. Initial SAR studies indicated that these novel series of integrase inhibitors are amenable to lead optimization. Several compounds with low nanomolar inhibitory potency are reported.<br /> (Copyright © 2010 Elsevier Ltd. All rights reserved.)
- Subjects :
- Azoles chemical synthesis
Azoles pharmacology
Bridged Bicyclo Compounds chemical synthesis
Bridged Bicyclo Compounds pharmacology
Chelating Agents chemical synthesis
Chelating Agents pharmacology
Drug Design
HIV Integrase metabolism
HIV Integrase Inhibitors chemical synthesis
HIV Integrase Inhibitors pharmacology
HIV-1 drug effects
Humans
Structure-Activity Relationship
Azoles chemistry
Bridged Bicyclo Compounds chemistry
Chelating Agents chemistry
HIV Integrase chemistry
HIV Integrase Inhibitors chemistry
Metals chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 20
- Issue :
- 19
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 20727753
- Full Text :
- https://doi.org/10.1016/j.bmcl.2010.07.081