Regioselective synthesis and biological evaluation of bis(indolyl)methane derivatized 1,4-disubstituted 1,2,3-bistriazoles as anti-infective agents

• Published in: Bioorganic & medicinal chemistry letters 2009-07, Vol.19 (13), p.3611-3614
• Main Authors: Damodiran, M., Muralidharan, D., Perumal, Paramasivan T.
• Format: Article
• Language: English
• Subjects: Anti-Infective Agents - chemical synthesis; Anti-Infective Agents - chemistry; Anti-Infective Agents - pharmacology; Antibacterial activity; Antibacterial agents; Antibiotics. Antiinfectious agents. Antiparasitic agents; Antifungal activity; Antifungal agents; Biological and medical sciences; Click chemistry; General aspects; Medical sciences; Methane - analogs & derivatives; Methane - chemical synthesis; Microbial Sensitivity Tests; Pharmacology. Drug treatments; Stereoisomerism; Triazole; Triazoles - chemical synthesis; Triazoles - chemistry; Triazoles - pharmacology
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2009.04.131

The regioselective synthesis of 1,4-disubstituted 1,2,3-bistriazoles from a variety of N-propargyl bis(indolyl)methanes with sodium azide using CuI as the catalyst in polyethyleneglycol-400 is reported. This process is of considerable synthetic advantages in terms of high atom economy, low environmental impact, mild reaction condition and good yields. The synthesized compounds have also been screened for their biological activity. The regioselective synthesis of 1,4-disubstituted 1,2,3-bistriazoles from a variety of N-propargyl bis(indolyl)methanes with sodium azide using CuI as the catalyst in polyethyleneglycol-400 is reported. This process is of considerable synthetic advantages in terms of high atom economy, low environmental impact, mild reaction condition and good yields. The synthesized compounds have also been screened for their biological activity.