Design, Conformation, and Crystallography of 2-Naphthyl Phenyl Ethers as Potent Anti-HIV Agents
Journal Article
·
· ACS Medicinal Chemistry Letters
Catechol diethers that incorporate a 7-cyano-2-naphthyl substituent are reported as non-nucleoside inhibitors of HIV-1 reverse transcriptase (NNRTIs). Many of the compounds have 1–10 nM potencies toward wild-type HIV-1. An interesting conformational effect allows two unique conformers for the naphthyl group in complexes with HIV-RT. X-ray crystal structures for 4a and 4f illustrate the alternatives.
- Research Organization:
- Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
- Sponsoring Organization:
- USDOE; National Institutes of Health (NIH)
- OSTI ID:
- 1338989
- Journal Information:
- ACS Medicinal Chemistry Letters, Vol. 7, Issue 12; ISSN 1948-5875
- Country of Publication:
- United States
- Language:
- ENGLISH
Similar Records
Structural investigation of
2‐naphthyl
phenyl ether inhibitors bound to
WT
and
Y181C
reverse transcriptase highlights key features of the
NNRTI
binding site
Structural and Preclinical Studies of Computationally Designed Non-Nucleoside Reverse Transcriptase Inhibitors for Treating HIV infection
HIV-1 Reverse Transcriptase Structure with RNase H Inhibitor dihydroxy benzoyl naphthyl Hydrazone Bound at a Novel Site
Journal Article
·
Wed Aug 05 00:00:00 EDT 2020
· Protein Science
·
OSTI ID:1338989
+4 more
Structural and Preclinical Studies of Computationally Designed Non-Nucleoside Reverse Transcriptase Inhibitors for Treating HIV infection
Journal Article
·
Mon Feb 06 00:00:00 EST 2017
· Molecular Pharmacology
·
OSTI ID:1338989
+4 more
HIV-1 Reverse Transcriptase Structure with RNase H Inhibitor dihydroxy benzoyl naphthyl Hydrazone Bound at a Novel Site
Journal Article
·
Mon Jan 01 00:00:00 EST 2007
· ACS Chemical Biology
·
OSTI ID:1338989
+6 more