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Bioorg Med Chem Lett. 2013 Sep 15;23(18):5209-12. doi: 10.1016/j.bmcl.2013.06.093. Epub 2013 Jul 8.

Extension into the entrance channel of HIV-1 reverse transcriptase--crystallography and enhanced solubility.

Author information

1
Department of Chemistry, Yale University, New Haven, CT 06520-8107, USA.

Abstract

Non-nucleoside inhibitors of HIV-1 reverse transcriptase (HIV-RT) are reported that feature extension into the entrance channel near Glu138. Complexes of the parent anilinylpyrimidine 1 and the morpholinoethoxy analog 2j with HIV-RT have received crystallographic characterization confirming the designs. Measurement of aqueous solubilities of 2j, 2k, the parent triazene 2a, and other NNRTIs demonstrate profound benefits for addition of the morpholinyl substituent.

KEYWORDS:

Anti-HIV agent; Crystal structures; Drug solubility; NNRTI

PMID:
23899617
PMCID:
PMC3761378
DOI:
10.1016/j.bmcl.2013.06.093
[Indexed for MEDLINE]
Free PMC Article

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