Drug Designing: Open Access
Open Access

Synthesis of novel 1, 2, 3-triazole tethered β-carboline derivatives with cytotoxic and anti-bacterial activities

2^nd International Conference and Expo on Drug Discovery & Designing

October 27-29, 2016 Rome, Italy

Peyman Salehi, Kosar Babanezhad, Morteza Bararjanian, Maryam Esmailzadeh, Mohammad-Ali Esmaeili and Atousa Aliahmadi

Shahid Beheshti University, Iran

Posters & Accepted Abstracts: Drug Des

Abstract :

Introduction: �²-Carbolines have a great importance because of their various pharmacological activities such as sedative, anxiolytic, anticonvulsant, hypnotic, anticancer, antiparasitic, antiviral, antithrombotic and antimicrobial. Methods: In this paper the synthesis of new �²-carboline derivatives possessing the 1, 2, 3-triazole ring at C-1 substituent from L-tryptophan by Pictet-Spengler reaction followed by a Huisgen 1, 3-dipolar addition is reported. In vitro cytotoxicity and antibacterial activity of synthetic compounds were investigated. Results: Methyl 1-(3-((1-(3,4-dichlorophenyl)-1H-1,2,3-triazol-4-yl)methoxy)phenyl)-�²-carboline-3-carboxylate(7f) showed the highest cytotoxic activity with IC50 values of 46 and 32 �¼M against Hela and HepG2 cell lines, respectively. Compounds 7d and 7i (possessing 4-bromophenyl substituent) and 5c showed excellent inhibition activity for Enterococcus faecium with MIC of 8 �¼g/mL. Conclusion: The results demonstrated that the presence of 1, 2, 3-triazole rings in �²-carboline derivatives improve their biological activities.

Biography :

Email: p-salehi@sbu.ac.ir