482661-10-9

Upstream product

• 5439-11-2 2-bromo-N-(2'-chlorophenyl)acetamide 
• 149747-23-9 5-methyl-4-p-tolyl-4H-[1,2,4]triazole-3-thiol 
• 796067-59-9 (5-methyl-4-p-tolyl-4H-[1,2,4]triazol-3-ylsulfanyl)-acetic acid 
• 95-51-2 o-chloroaniline 
• 149747-23-9 5-methyl-4-(4-methylphenyl)-2,4-dihydro-3H-1,2,4-triazole-3-thione 
• 3289-76-7 N-(2-chlorophenyl)chloroacetamide 
• 152473-68-2 1-acetyl-4-(4-methylphenyl)thiosemicarbazide 
• 13278-67-6 4-(4-methylphenyl)-3-thiosemicarbazide 

Relevant academic research and scientific papers

Tri-substituted triazoles as potent non-nucleoside inhibitors of the HIV-1 reverse transcriptase

A new series of 1,2,4-triazoles was synthesized and tested against several NNRTI-resistant HIV-1 isolates. Several of these compounds exhibited potent antiviral activities against efavirenz- and nevirapine-resistant viruses, containing K103N and/or Y181C mutations or Y188L mutation. Triazoles were first synthesized from commercially available substituted phenylthiosemicarbazides, then from isothiocyanates, and later by condensing the desired substituted anilines with thiosemicarbazones.

Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors

A novel sulfanyltriazole was discovered as an HIV-1 non-nucleoside reverse transcriptase inhibitor via HTS using a cell-based assay. Chemical modifications and molecular modeling studies were carried out to establish its SAR and understand its interactions with the enzyme. These modifications led to the identification of sulfanyltriazoles with low nanomolar potency for inhibiting HIV-1 replication and promising activities against selected NNRTI resistant mutants. These novel and potent sulfanyltriazoles could serve as advanced leads for further optimization.