Synthesis and antiviral activity of P1' arylsulfonamide azacyclic urea HIV protease inhibitors.

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Huang PP, Randolph JT, Klein LL, Vasavanonda S, Dekhtyar T, Stoll VS, Kempf DJ

Synthesis and antiviral activity of P1' arylsulfonamide azacyclic urea HIV protease inhibitors.

Bioorg Med Chem Lett. 2004 Aug 2;14(15):4075-8.

PubMed ID

15225729 [ View in PubMed

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Abstract

A series of novel azacyclic urea HIV protease inhibitors bearing a benzenesulfonamide group at P1' were synthesized utilizing a parallel synthesis method. Structural studies of early analogs bound in the enzyme active site were used to design more potent inhibitors. The effects of substituting the P1' benzenesulfonyl group on antiviral activity and protein binding are described.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
3-{[(5R,6R)-5-Benzyl-6-hydroxy-2,4-bis(4-hydroxybenzyl)-3-oxo-1,2,4-triazepan-1-yl]sulfonyl}benzonitril	V-1 protease	Protein	Human immunodeficiency virus 1	Unknown	Not Available	Details

Polypeptides

Name	UniProt ID
Gag-Pol polyprotein	P03366	Details