Review on the Synthesis and Therapeutic Potential of Pyrido[2,3-d], [3,2-d], [3,4-d] and [4,3-d]pyrimidine Derivatives

JF Campos, T Besson, S Berteina-Raboin - Pharmaceuticals, 2022 - mdpi.com
The objective of this review is to list the structures composed of a pyridopyrimidine moiety
which have shown a therapeutic interest or have already been approved for use as …

Discovery of novel antibacterial agents: Recent developments in D‐alanyl‐D‐alanine ligase inhibitors

Y Qin, L Xu, Y Teng, Y Wang… - Chemical Biology & Drug …, 2021 - Wiley Online Library
Bacterial infections can cause serious problems that threaten public health over a long
period of time. Moreover, the continuous emergence of drug‐resistant bacteria necessitates …

Identification of novel chemical scaffolds inhibiting trypanothione synthetase from pathogenic trypanosomatids

D Benítez, A Medeiros, L Fiestas… - PLoS neglected …, 2016 - journals.plos.org
Background The search for novel chemical entities targeting essential and parasite-specific
pathways is considered a priority for neglected diseases such as trypanosomiasis and …

ProBiS-ligands: a web server for prediction of ligands by examination of protein binding sites

J Konc, D Janežič - Nucleic acids research, 2014 - academic.oup.com
The ProBiS-ligands web server predicts binding of ligands to a protein structure. Starting
with a protein structure or binding site, ProBiS-ligands first identifies template proteins in the …

Pharmacomodulations of the benzoyl-thiosemicarbazide scaffold reveal antimicrobial agents targeting D-alanyl-D-alanine ligase in bacterio

A Ameryckx, L Pochet, G Wang, E Yildiz… - European Journal of …, 2020 - Elsevier
Abstract d-Alanyl-d-alanine ligase (Ddl) is a validated and attractive target among the
bacterial enzymes involved in peptidoglycan biosynthesis. In the present work, we …

1-(2-Hydroxybenzoyl)-thiosemicarbazides are promising antimicrobial agents targeting D-alanine-D-alanine ligase in bacterio

A Ameryckx, L Thabault, L Pochet, S Leimanis… - European Journal of …, 2018 - Elsevier
The bacterial cell wall and the enzymes involved in peptidoglycan synthesis are privileged
targets for the development of novel antibacterial agents. In this work, a series of 1-(2 …

Modeling enzyme-ligand binding in drug discovery

J Konc, S Lešnik, D Janežič - Journal of Cheminformatics, 2015 - Springer
Enzymes are one of the most important groups of drug targets, and identifying possible
ligand-enzyme interactions is of major importance in many drug discovery processes. Novel …

Discovery of the first inhibitors of bacterial enzyme D-aspartate ligase from Enterococcus faecium (Aslfm)

V Škedelj, A Perdih, M Brvar, A Kroflič… - European Journal of …, 2013 - Elsevier
The d-aspartate ligase of Enterococcus faecium (Asl fm) is an attractive target for the
development of narrow-spectrum antibacterial agents that are active against multidrug …

A convenient synthesis of novel 5-aryl-pyrido [2, 3-d] pyrimidines and screening of their preliminary antibacterial properties

L Saikia, B Das, P Bharali, AJ Thakur - Tetrahedron Letters, 2014 - Elsevier
Exploiting the diene nature of 6-[1-aza-2-(dimethylamino) prop-l-enyl]-1, 3-dimethyluracil (2),
novel 5-aryl-pyrido [2, 3-d] pyrimidines (5a–h) have been synthesized. The reaction …

In Silico, in Vitro and in Vivo Study of Substituted Imidazolidinone Sulfonamides as Antibacterial Agents

D Hodyna, V Kovalishyn, M Kachaeva… - Chemistry & …, 2023 - Wiley Online Library
New substituted imidazolidinone sulfonamides have been developed using a rational drug
design strategy. Predictive QSAR models for the search of new antibacterials were created …