Antituberculosis drugs: ten years of research
YL Janin - Bioorganic & medicinal chemistry, 2007 - Elsevier
Tuberculosis is today amongst the worldwide health threats. As resistant strains of
Mycobacterium tuberculosis have slowly emerged, treatment failure is too often a fact …
Mycobacterium tuberculosis have slowly emerged, treatment failure is too often a fact …
Novel targets for tuberculosis drug discovery
K Mdluli, M Spigelman - Current opinion in pharmacology, 2006 - Elsevier
Since the determination of the Mycobacterium tuberculosis genome sequence, various
groups have used the genomic information to identify and validate targets as the basis for …
groups have used the genomic information to identify and validate targets as the basis for …
Diverse, high-quality test set for the validation of protein− ligand docking performance
MJ Hartshorn, ML Verdonk, G Chessari… - Journal of medicinal …, 2007 - ACS Publications
A procedure for analyzing and classifying publicly available crystal structures has been
developed. It has been used to identify high-resolution protein− ligand complexes that can …
developed. It has been used to identify high-resolution protein− ligand complexes that can …
Machine learning-based drug design for identification of thymidylate kinase inhibitors as a potential anti-Mycobacterium tuberculosis
The rise of antibiotic-resistant Mycobacterium tuberculosis (Mtb) has reduced the availability
of medications for tuberculosis therapy, resulting in increased morbidity and mortality …
of medications for tuberculosis therapy, resulting in increased morbidity and mortality …
Current status of some antituberculosis drugs and the development of new antituberculous agents with special reference to their in vitro and in vivo antimicrobial …
H Tomioka - Current pharmaceutical design, 2006 - ingentaconnect.com
Tuberculosis (TB) is a growing international health concern, since it is the leading infectious
cause of death in the world today. In particular, the increasing prevalence of multidrug …
cause of death in the world today. In particular, the increasing prevalence of multidrug …
Discovery of pyrimidine-tethered benzothiazole derivatives as novel anti-tubercular agents towards multi- and extensively drug resistant Mycobacterium tuberculosis
LR Hemeda, MA El Hassab… - Journal of Enzyme …, 2023 - Taylor & Francis
In this study, new benzothiazole–pyrimidine hybrids (5a–c, 6, 7a–f, and 8–15) were
designed and synthesised. Two different functionalities on the pyrimidine moiety of lead …
designed and synthesised. Two different functionalities on the pyrimidine moiety of lead …
Mycobacterium tuberculosis Cell Wall Permeability Model Generation Using Chemoinformatics and Machine Learning Approaches
S Nagamani, GN Sastry - ACS omega, 2021 - ACS Publications
The drug-resistant strains of Mycobacterium tuberculosis (M. tb) are evolving at an alarming
rate, and this indicates the urgent need for the development of novel antitubercular drugs …
rate, and this indicates the urgent need for the development of novel antitubercular drugs …
Structure Guided Lead Generation for M. tuberculosis Thymidylate Kinase (Mtb TMK): Discovery of 3-Cyanopyridone and 1,6-Naphthyridin-2-one as Potent Inhibitors
M Naik, A Raichurkar, BS Bandodkar… - Journal of medicinal …, 2015 - ACS Publications
M. tuberculosis thymidylate kinase (Mtb TMK) has been shown in vitro to be an essential
enzyme in DNA synthesis. In order to identify novel leads for Mtb TMK, we performed a high …
enzyme in DNA synthesis. In order to identify novel leads for Mtb TMK, we performed a high …
In silico design and synthesis of tetrahydropyrimidinones and tetrahydropyrimidinethiones as potential thymidylate kinase inhibitors exerting anti-TB activity against …
KN Venugopala, C Tratrat, M Pillay… - Drug Design …, 2020 - Taylor & Francis
Background and Purpose Tuberculosis has been reported to be the worldwide leading
cause of death resulting from a sole infectious agent. The emergence of multidrug-resistant …
cause of death resulting from a sole infectious agent. The emergence of multidrug-resistant …
Thymidylate kinase: an old topic brings new perspectives
Thymidylate kinase (TMPK) is a key enzyme for pyrimidine synthesis that catalyzes the
phosphorylation of thymidine 5'-monophosphate (dTMP) in the presence of ATP and Mg2+ …
phosphorylation of thymidine 5'-monophosphate (dTMP) in the presence of ATP and Mg2+ …