Anticancer Activity of New 1,2,3-Triazole-Amino Acid Conjugates

Design, Synthesis of New Amino Acid Derivatives and Evaluate DNA Binding Activity, Anticancer and Antimicrobial Activity

The present review covers the recent synthetic amino acid derivatives with chemical transformations to peptide derivatives. The amino acids were used as starting keys for synthesis peptides and pseudopeptides derived from pyridinine, coumarine, imaddizole, pyrazole phthalyl, qunolinine and sulfonamide rings. these biomolecules have diverse biological and pharmacological actions, as antimicrobia...

Design, Modeling and Synthesis of 1,2,3-Triazole-Linked Nucleoside-Amino Acid Conjugates as Potential Antibacterial Agents.

Copper-catalyzed azide-alkyne cycloadditions (CuAAC or click chemistry) are convenient methods to easily couple various pharmacophores or bioactive molecules. A new series of 1,2,3-triazole-linked nucleoside-amino acid conjugates have been designed and synthesized in 57-76% yields using CuAAC. The azido group was introduced on the 5'-position of uridine or the acyclic analogue using the tosyl-a...

Microwave-assisted one-pot synthesis and anti-biofilm activity of 2-amino-1H-imidazole/triazole conjugates.

A microwave-assisted protocol was developed for the construction of 2-amino-1H-imidazole/triazole conjugates starting from the previously described 2-hydroxy-2,3-dihydro-1H-imidazo[1,2-a]pyrimidin-4-ium salts. The process involves a one-pot hydrazinolysis/Dimroth-rearrangement of these salts followed by a ligand-free copper nanoparticle-catalyzed azide-alkyne Huisgen cycloaddition. The 2-amino-...

Quinone-Amino Acid Conjugates Targeting Leishmania Amino Acid Transporters

The aim of the present study was to investigate the feasibility of targeting Leishmania transporters via appropriately designed chemical probes. Leishmania donovani, the parasite that causes visceral leishmaniasis, is auxotrophic for arginine and lysine and has specific transporters (LdAAP3 and LdAAP7) to import these nutrients. Probes 1-15 were originated by conjugating cytotoxic quinone fragm...

New Perturbation Model for Prediction of Amino Acid and Peptide Activity Coefficients