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M9650415.TXT
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1996-03-09
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Document 0415
DOCN M9650415
TI Correlation of anti-HIV potency with lipophilicity in a series of
cosalane analogs having normal alkenyl and phosphodiester chains as
cholestane replacements.
DT 9605
AU Keyes RF; Golebiewski WM; Cushman M; Department of Medicinal Chemistry
and Pharmacognosy, School of; Pharmacy, Purdue University, West
Lafayette, Indiana 47907, USA.
SO J Med Chem. 1996 Jan 19;39(2):508-14. Unique Identifier : AIDSLINE
MED/96145185
AB In order to define the role of the cholestane moiety in the anti-HIV
agent cosalane, a series of cosalane analogs was synthesized in which
the cholestane ring system was replaced by normal alkenyl and
phosphodiester substituents having varied chain lengths and
lipophilicities. The compounds containing simple alkenyl substituents
were found to be more potent as inhibitors of the cytopathic effect of
HIV-1 in cell culture than the phosphodiesters. In addition, the
potencies of the alkene congeners correlated positively with chain
length and lipophilicity of the alkene. The results indicate that the
cholestane moiety of cosalane functions as a lipophilic accessory
appendage to escort the dichlorodisalicylmethane pharmacophore to a
lipid environment.
DE Antiviral Agents/CHEMISTRY/METABOLISM/*PHARMACOLOGY Aurintricarboxylic
Acid/*ANALOGS & DERIVATIVES/CHEMISTRY/ METABOLISM/PHARMACOLOGY Cells,
Cultured Cytopathogenic Effect, Viral/DRUG EFFECTS Human HIV-1/*DRUG
EFFECTS/PATHOGENICITY Lipids/*METABOLISM Spectrum Analysis Support,
U.S. Gov't, P.H.S. JOURNAL ARTICLE
SOURCE: National Library of Medicine. NOTICE: This material may be
protected by Copyright Law (Title 17, U.S.Code).