1,2,3-Triazole fused with pyridine/pyrimidine as new template for antimicrobial agents: Regioselective synthesis and identification of potent N-heteroarenes

  • Bioorg Med Chem Lett. 2018 Nov 1;28(20):3302-3306. doi: 10.1016/j.bmcl.2018.09.021.
Nagaraju Marepu  1 ,  Sunandamma Yeturu  2 ,  Manojit Pal  3
Affiliations
  • 1. Department of Chemistry, Acharya Nagarjuna University, Nagarjunanagar, Guntur 522510, Andhra Pradesh, India.
  • 2. Department of Chemistry, Acharya Nagarjuna University, Nagarjunanagar, Guntur 522510, Andhra Pradesh, India. Electronic address: [email protected].
  • 3. Dr Reddy's Institute of Life Sciences, University of Hyderabad Campus, Gachibowli, Hyderabad 500 046, India. Electronic address: [email protected].
PMID: 30243590 DOI: 10.1016/j.bmcl.2018.09.021
Abstract

The 1,2,3-triazole ring fused with pyridine/pyrimidine was explored as new template for the identification of potential antimicrobial agents. The regioselective synthesis of these pre-designed N-heteroarenes was achieved via exploring the application of Buchwald's strategy (i.e. C-N bond formation/reduction/diazotization/cyclization sequence) to the N-heteroarene system. Two of them showed promising Antibacterial (comparable to streptomycin) and several showed potent Antifungal (comparable to mancozeb) activities.

Keywords
1,2,3-Triazole; Antibacterial; Antifungal; Buchwald’s strategy; Pyridine.
Products