Inhibition of HIV replication by naphthalenemonosulfonic acid derivatives and a bis naphthalenedisulfonic acid compound.
Several naphthalenemonosulfonic acid analogs and a bis naphthalenedisulfonic acid have been evaluated for anti-HIV activity in assays using H9 and MOLT-3 cells. Among the naphthalenemonosulfonic acids, a 4-amino-5-hydroxy compound and a 4,5-diamino compound showed low anti-HIV activity (upto 50% inhibition) at non-toxic doses. The bis naphthalenedisulfonic acid compound demonstrated significant suppression of HIV-1 antigen expression as measured by monoclonal antibodies to p17 (95%), p24 (94%) and syncytia inhibition (82%) at a dose of 20 micrograms/ml that was non-toxic to the host cells. The bis naphthalenedisulfonic acid analog represents a new class of compounds which may be effective in the treatment of HIV infected patients. The structure activity relationship and a probable mode of action of these compounds is discussed.
Mohan
P
P
Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois, Chicago.
Singh
R
R
Wepsiec
J
J
Gonzalez
I
I
Sun
D K
DK
Sarin
P S
PS
D000911:Antibodies, Monoclonal; D000998:Antiviral Agents; D002460:Cell Line; D015683:Gene Products, gag / Q000096:biosynthesis; D015726:Giant Cells / Q000187:drug effects; D015488:HIV Antigens / Q000096:biosynthesis; D016655:HIV Core Protein p24; D015497:HIV-1 / Q000187:drug effects* / Q000502:physiology; D066298:In Vitro Techniques; D009282:Naphthalenesulfonates / Q000494:pharmacology*; D010452:Peptide Biosynthesis; D010455:Peptides; D013329:Structure-Activity Relationship; D014758:Viral Core Proteins / Q000096:biosynthesis; D014779:Virus Replication / Q000187:drug effects*; D054301:gag Gene Products, Human Immunodeficiency Virus
D000911:Antibodies, Monoclonal; D000998:Antiviral Agents; D015683:Gene Products, gag; C052407:HGP-30 peptide, Human immunodeficiency virus-1; D015488:HIV Antigens; D016655:HIV Core Protein p24; D009282:Naphthalenesulfonates; D010455:Peptides; D014758:Viral Core Proteins; D054301:gag Gene Products, Human Immunodeficiency Virus