Lipid conjugates of antiretroviral agents. I. Azidothymidine-monophosphate-diglyceride: anti-HIV activity, physical properties, and interaction with plasma proteins.

Abstract:

:3'-Azido-3'-deoxythymidine-5'-phosphate diglyceride (16:0/18:1 omega 9), a phosphatic acid conjugate of AZT, is active against HIV replication in H9 cells and syncytia formation in MOLT-3 cells. The activities rank as AZT greater than pure conjugate greater than conjugate in mixed liposomes, with the pure conjugate having about one-third the activity of free AZT. The compound binds very rapidly to serum lipoproteins, but not to serum albumin, alpha and beta globulins, or red cells. Pancreatic phospholipase A2 hydrolyzes it to the lysophosphatidic acid conjugate.

authors

Steim JM,Camaioni Neto C,Sarin PS,Sun DK,Sehgal RK,Turcotte JG

doi

10.1016/0006-291x(90)91414-n

subject

Has Abstract

pub_date

1990-08-31 00:00:00

pages

451-7

issue

1

eissn

0006-291X

issn

1090-2104

pii

0006-291X(90)91414-N

journal_volume

171

pub_type

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