Inhibitors of FabI, an enzyme drug target in the bacterial fatty acid biosynthesis pathway

H Lu, PJ Tonge - Accounts of chemical research, 2008 - ACS Publications
The modern age of drug discovery, which had been slowly gathering momentum during the
early part of the twentieth century, exploded into life in the 1940s with the isolation of …

Recent advances in drug discovery against Mycobacterium tuberculosis: Metal-based complexes

CB Scarim, RL de Farias, AV de Godoy Netto… - European Journal of …, 2021 - Elsevier
Metal-based drugs are privileged motifs that act as primary pharmacophores in bioactive
compounds for various diseases, including tuberculosis (TB). This potentially life-threatening …

An exceptionally potent inhibitor of human CD73

CE Bowman, RG da Silva, A Pham, SW Young - Biochemistry, 2019 - ACS Publications
We recently reported the initiation of a Phase I clinical trial with AB680, a potent human
CD73 inhibitor, being developed for the treatment of solid tumors (NCT03677973). We …

Discovery of New Inhibitors of Mycobacterium tuberculosis InhA Enzyme Using Virtual Screening and a 3D-Pharmacophore-Based Approach

I Pauli, RN Dos Santos, DC Rostirolla… - Journal of chemical …, 2013 - ACS Publications
Mycobacterium tuberculosis InhA (Mt InhA) is an attractive enzyme to drug discovery efforts
due to its validation as an effective biological target for tuberculosis therapy. In this work, two …

[HTML][HTML] The use of biodiversity as source of new chemical entities against defined molecular targets for treatment of malaria, tuberculosis, and T-cell mediated …

LA Basso, LHP Silva, AG Fett-Neto… - Memórias do Instituto …, 2005 - SciELO Brasil
The modern approach to the development of new chemical entities against complex
diseases, especially the neglected endemic diseases such as tuberculosis and malaria, is …

Targeting InhA, the FASII enoyl-ACP reductase: SAR studies on novel inhibitor scaffolds

P Pan, PJ Tonge - Current topics in medicinal chemistry, 2012 - ingentaconnect.com
The bacterial type II fatty acid biosynthesis (FASII) pathway is an essential but unexploited
target for drug discovery. In this review we summarize SAR studies on inhibitors of InhA, the …

Nontoxic Metal–Cyclam Complexes, a New Class of Compounds with Potency against Drug-Resistant Mycobacterium tuberculosis

M Yu, G Nagalingam, S Ellis, E Martinez… - Journal of Medicinal …, 2016 - ACS Publications
Tuberculosis (TB) accounted for 1.5 million deaths in 2014, and new classes of anti-TB
drugs are required. We report a class of functionalized 1, 8-disubstituted cyclam derivatives …

Ruthenium (II) phosphine/picolinate complexes as antimycobacterial agents

FR Pavan, G Von Poelhsitz, FB do Nascimento… - European Journal of …, 2010 - Elsevier
The synthesis, characterization and the anti-Mycobacterium tuberculosis (MTB) activities of
three ruthenium complexes containing the 2-pyridinecarboxylic acid anion (picolinate), with …

[HTML][HTML] Unprecedented in Vitro Antitubercular Activitiy of Manganese(II) Complexes Containing 1,10-Phenanthroline and Dicarboxylate Ligands: Increased Activity …

P McCarron, M McCann, M Devereux… - Frontiers in …, 2018 - frontiersin.org
Mycobacterium tuberculosis is the etiologic agent of tuberculosis. The demand for new
chemotherapeutics with unique mechanisms of action to treat (multi) resistant strains is an …

Antitubercular activity of Ru (II) isoniazid complexes

I de Aguiar, A Tavares, AC Roveda Jr… - European Journal of …, 2015 - Elsevier
Despite the resistance developed by the Mycobacterium tuberculosis (MTb) strains,
isoniazid (INH) has been recognized as one of the best drug for treatment of Tuberculosis …