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Development of a selective HDAC inhibitor aimed at reactivating the HIV latent reservoir
- Source :
- Bioorganicmedicinal chemistry letters. 30(17)
- Publication Year :
- 2020
-
Abstract
- The synthesis and SAR development of a trisubstituted imidazole HDAC inhibitor is described. The compounds were synthesized with high diastereocontrol by leveraging Ellman sulfinyl imine chemistry. Structural elucidation provided insight into binding mode and supported design rational. Pharmacokinetic properties of lead compounds were determined.
- Subjects :
- CD4-Positive T-Lymphocytes
Clinical Biochemistry
Imine
Human immunodeficiency virus (HIV)
Pharmaceutical Science
medicine.disease_cause
Crystallography, X-Ray
01 natural sciences
Biochemistry
Histone Deacetylases
chemistry.chemical_compound
Inhibitory Concentration 50
Structure-Activity Relationship
Drug Discovery
medicine
HDAC inhibitor
Imidazole
Animals
Humans
Molecular Biology
010405 organic chemistry
Chemistry
Organic Chemistry
Imidazoles
Combinatorial chemistry
0104 chemical sciences
Rats
Histone Deacetylase Inhibitors
Isoenzymes
010404 medicinal & biomolecular chemistry
HIV-1
Molecular Medicine
Subjects
Details
- ISSN :
- 14643405
- Volume :
- 30
- Issue :
- 17
- Database :
- OpenAIRE
- Journal :
- Bioorganicmedicinal chemistry letters
- Accession number :
- edsair.doi.dedup.....ec48bbfb23bb75c786357864cd360370