Benzimidazoles in drug discovery: a patent review

CSW Law, KY Yeong - ChemMedChem, 2021 - Wiley Online Library
Benzimidazole is a heterocyclic ring system that has been widely studied in the
pharmaceutical field. For the past decade, numerous benzimidazole derivatives have been …

[HTML][HTML] A critical review of benzimidazole: Sky-high objectives towards the lead molecule to predict the future in medicinal chemistry

S Banerjee, S Mukherjee, P Nath, A Mukherjee… - Results in …, 2023 - Elsevier
Out of several heterocyclic templates, the use of a Benzimidazole (BZ) scaffold is immensely
observed. This fused heterocycle comprises two ring nitrogen atoms placed at 1st and 3rd …

Elucidating the path to Plasmodium prolyl-tRNA synthetase inhibitors that overcome halofuginone resistance

MA Tye, NC Payne, C Johansson, K Singh… - Nature …, 2022 - nature.com
The development of next-generation antimalarials that are efficacious against the human
liver and asexual blood stages is recognized as one of the world's most pressing public …

Double drugging of prolyl-tRNA synthetase provides a new paradigm for anti-infective drug development

Y Manickam, N Malhotra, S Mishra, P Babbar… - PLoS …, 2022 - journals.plos.org
Toxoplasmosis is caused by Toxoplasma gondii and in immunocompromised patients it may
lead to seizures, encephalitis or death. The conserved enzyme prolyl-tRNA synthetase …

Recent advances of benzimidazole as anticancer agents

S Venugopal, B Kaur, A Verma… - Chemical Biology & …, 2023 - Wiley Online Library
Cancer is the second leading cause of death globally, with 9.6 million deaths yearly. As a life‐
threatening disease, it necessitates the emergence of new therapies. Resistance to current …

The pathophyiological role of aminoacyl-tRNA synthetases in digestive system diseases

W Wusiman, Z Zhang, Q Ding, M Liu - Frontiers in Physiology, 2022 - frontiersin.org
Aminoacyl-tRNA synthetases (ARSs) catalyze the ligation of amino acids to their cognate
transfer RNAs and are indispensable enzymes for protein biosynthesis in all the cells …

Cervicovaginal microbiome and urine metabolome paired analysis reveals niche partitioning of the microbiota in patients with human papilloma virus infections

N Chorna, J Romaguera, F Godoy-Vitorino - Metabolites, 2020 - mdpi.com
In this study, we evaluate the association between vaginal and cervical human
papillomavirus infections high-risk types (HPV+ H), negative controls (HPV−), the bacterial …

Repositioning and Characterization of 1-(Pyridin-4-yl)pyrrolidin-2-one Derivatives as Plasmodium Cytoplasmic Prolyl-tRNA Synthetase Inhibitors

M Okaniwa, A Shibata, A Ochida, Y Akao… - ACS Infectious …, 2021 - ACS Publications
Prolyl-tRNA synthetase (PRS) is a clinically validated antimalarial target. Screening of a set
of PRS ATP-site binders, initially designed for human indications, led to identification of 1 …

Discovery of a novel prolyl-tRNA synthetase inhibitor and elucidation of its binding mode to the ATP site in complex with l-proline

R Adachi, K Okada, R Skene, K Ogawa, M Miwa… - Biochemical and …, 2017 - Elsevier
Prolyl-tRNA synthetase (PRS) is a member of the aminoacyl-tRNA synthetase family of
enzymes and catalyzes the synthesis of prolyl-tRNA Pro using ATP, l-proline, and tRNA Pro …

Discovery and pharmacological characterization of a new class of prolyl-tRNA synthetase inhibitor for anti-fibrosis therapy

A Shibata, M Kuno, R Adachi, Y Sato, H Hattori… - PloS one, 2017 - journals.plos.org
Scleroderma has clinical characteristics including skin and other tissue fibrosis, but there is
an unmet need for anti-fibrotic therapy. Halofuginone (HF) is a well-known anti-fibrosis agent …