Synthesis and pharmacological screening of some new triazoles.
3,5-Dinitrobenzoic acid hydrazide (1) treated with substituted phenyl isothiocyanates (2a-2d) in dry benzene yields N'-aryl-N4-(3,5-dinitrophenyl) thiosemicarbazides (3-6), which cyclizes in NaOH solution yielding 1-aryl-5-(3,5-dinitrophenyl)-2-mercapto-1,3,4-triazoles (7-10). The reaction of the appropriate 7-10 respectively with chloroacetic acid and 4-chlorobenzoic acid in NaOH solution gave 1-aryl-5-(3.5-dinitrophenyl)-2-mercapto methyl/phenyl carboxy-1,3,4-triazoles (11-18). All the compounds were found to be relatively non toxic (ALD greater than 1000 mg/kg), whereas in their gross CNS observations the compounds were found to be psychotropic. They increased or decreased spontaneous locomotor activity and at high doses produced writhing and mild hypothermia. Some of them mildly affected the cardiovascular system and showed antiinflammatory activity.
Agarwal
S
S
Chemistry Department, Lucknow University, India.
Pande
A
A
Saxena
V K
VK
Chowdhury
S R
SR
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis; D002415:Cats; D002490:Central Nervous System / Q000187:drug effects; D055598:Chemical Phenomena; D002621:Chemistry; D007035:Hypothermia / Q000139:chemically induced; D008124:Locomotion / Q000187:drug effects; D008970:Molecular Weight; D011619:Psychotropic Drugs / Q000138:chemical synthesis; D051381:Rats; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity
D000894:Anti-Inflammatory Agents, Non-Steroidal; D011619:Psychotropic Drugs; D014230:Triazoles