Summary

Name:

P-1946

Synonyms:

P1946; P 1946

Sponsor:

Pharmacor (acquired by Procyon/Ambrilia Biopharma; Canada) (no longer in operation)

Type of product:

Inhibitor

Viral family:

Retroviridae

Status:

Preclinical
Lead compound

Structure

Structure P-1946  C29H41N5O6S

Formula:

C29H41N5O6S

Molecular weight:

587.73

P-1946 

Synonyms:P1946; P 1946       Sponsor:Pharmacor (acquired by Procyon/Ambrilia Biopharma; Canada) (no longer in operation)       Type of product:Inhibitor       Mode of action:PI       Viral family:Retroviridae       Virus:HIV (Human Immunodeficiency virus)      

Details

Characteristics:
Small molecule, inhibitor of HIV protease;

Represents L-lysine derivative with sulfonamide moiety;

 

Developed as potential agent for treatment for HIV/AIDS

 

Ref.: Sévigny G et al., Antiviral Res. 2006 Jun;70(2):17-20 (www.ncbi.nlm.nih.gov/pubmed/16473417);  Stellbrink HJ. Antivir Chem Chemother. 2009;19(5):189-200. Review. (www.ncbi.nlm.nih.gov/pubmed/19483267)

Resistance:
No significant loss of activity in presence of PR mutations D30N, I50V, G48V/L90M, V82F,T/I84V, and L10R/M46I/L63P/V82T/I84V;
 

Significant loss of susceptibility to P-1946 required presence of at least 6 mutations in viral PR gene

 

Ref.: Sévigny G et al., Antiviral Res. 2006 Jun;70(2):17-20 (www.ncbi.nlm.nih.gov/pubmed/16473417)

Activity in vitro

EC50: 150 nM (HIV-1NL4.3)
 

CCIC50: 40 μM

 

Ref.: Sévigny G et al., Antiviral Res. 2006 Jun;70(2):17-20 (www.ncbi.nlm.nih.gov/pubmed/16473417)

Development status

Preclinical
Lead compound

Remarks

Amino acid derivative, acting as protease inhibitor of HIV;
 
Not affected by several key protease mutations, including I50V associated with Amprenavir resistance;
 
Lead cpnd, superseded by PL-100;
 

Pharmacor was acquired by Procyon Biopharma (later called Ambrilia Biopharma) in 2003



Formula: C29H41N5O6S
Molecular weight: 587.73