Fluorinated betulinic acid derivatives and evaluation of their anti-HIV activity.
Bioorg Med Chem Lett
; 26(1): 68-71, 2016 Jan 01.
Article
em En
| MEDLINE
| ID: mdl-26598461
ABSTRACT
Several fluorinated derivatives of the anti-HIV maturation agent bevirimat (1) were synthesized and evaluated for anti-HIV replication activity. The modified positions were the C-2, C-3, C-28, and C-30 positions, either directly on the betulinic acid (2) skeleton or in the attached side chains. Compound 18, which has a trifluoromethyl group added to C-30 of its isopropenyl group, exhibited similar potency to 1 against HIV-1NL4-3. In total, our current studies support our prior conclusion that C-30 allylic modification is unlikely to be a pharmacophore for anti-HIV activity, but could be a meaningful route to manipulate other properties of 2-related compounds.
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MEDLINE
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Triterpenos
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HIV
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Fármacos Anti-HIV
Idioma:
En
Ano de publicação:
2016
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Article