2-Mercapto-N-(azolyl) benzenesulphonamides III. Synthesis of some new 2-mercapto-N-(5-amino-1,2,4-triazol-3-yl) benzenesulphonamide derivatives with potential anti-HIV or anticancer activity.
A series of 2-mercapto-4-R1-5-R2-N-[1-R4-5-(R3-amino)-1,2,4- triazol-3-yl] benzenesulphonamides [IIa-IIg, IIIa-IIId] was obtained by the reaction of N-(1,1-dioxo-6-R1-7-R2- 1,2,4-benzodithiazin-3-yl)-N'-R3-guanidines [Ia-Ig] with some hydrazines in methanol or pyridine medium. The mechanism for the reaction has been suggested. Preliminary screening data indicated that compounds [IIIa-IIIb] exhibit moderate anti HIV activity, and compounds [IIIa-IIId] anticancer activity. Some structure-activity relationships are also discussed.
Brzozowski
Z
Z
Department of Drug Technology, Faculty of Farmacy, Medical University, Gdańsk, Poland.
D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001555:Benzene Derivatives / Q000138:chemical synthesis* / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy; D013329:Structure-Activity Relationship; D013438:Sulfhydryl Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology
D019380:Anti-HIV Agents; D000970:Antineoplastic Agents; D001555:Benzene Derivatives; D013438:Sulfhydryl Compounds; D013449:Sulfonamides