[HTML][HTML] Application of fragment-based drug discovery to versatile targets
Q Li - Frontiers in molecular biosciences, 2020 - frontiersin.org
Fragment-based drug discovery (FBDD) is a powerful method to develop potent small-
molecule compounds starting from fragments binding weakly to targets. As FBDD exhibits …
molecule compounds starting from fragments binding weakly to targets. As FBDD exhibits …
Fragment-to-lead medicinal chemistry publications in 2020
IJP De Esch, DA Erlanson, W Jahnke… - Journal of medicinal …, 2021 - ACS Publications
Fragment-based drug discovery (FBDD) continues to evolve and make an impact in the
pharmaceutical sciences. We summarize successful fragment-to-lead studies that were …
pharmaceutical sciences. We summarize successful fragment-to-lead studies that were …
[HTML][HTML] Design and synthesis of novel antimicrobial agents
Z Breijyeh, R Karaman - Antibiotics, 2023 - mdpi.com
The necessity for the discovery of innovative antimicrobials to treat life-threatening diseases
has increased as multidrug-resistant bacteria has spread. Due to antibiotics' availability over …
has increased as multidrug-resistant bacteria has spread. Due to antibiotics' availability over …
Mycobacterium enoyl acyl carrier protein reductase (InhA): A key target for antitubercular drug discovery
MS Prasad, RP Bhole, PB Khedekar, RV Chikhale - Bioorganic Chemistry, 2021 - Elsevier
Enoyl acyl carrier protein reductase (InhA) is a key enzyme involved in fatty acid synthesis
mainly mycolic acid biosynthesis that is a part of NADH dependent acyl carrier protein …
mainly mycolic acid biosynthesis that is a part of NADH dependent acyl carrier protein …
Novel 2-arylthiazolidin-4-one-thiazole hybrids with potent activity against Mycobacterium tuberculosis
DIA Othman, A Hamdi, MM Abdel-Aziz, SM Elfeky - Bioorganic Chemistry, 2022 - Elsevier
Abstract Substituted aldehydes, ethyl 2-(2-amino-thiazol-4-yl) acetate), and 2-
mercaptoacetic acid, in a three-component one-pot green synthetic approach afforded 2 …
mercaptoacetic acid, in a three-component one-pot green synthetic approach afforded 2 …
[HTML][HTML] Mycobacterial drug discovery
KA Abrahams, GS Besra - RSC Medicinal Chemistry, 2020 - pubs.rsc.org
Mycobacterium tuberculosis is the causative pathogen of the pulmonary disease
tuberculosis. Despite the availability of effective treatment programs, there is a global pursuit …
tuberculosis. Despite the availability of effective treatment programs, there is a global pursuit …
[HTML][HTML] A practical perspective on the roles of solution NMR spectroscopy in drug discovery
Q Li, CB Kang - Molecules, 2020 - mdpi.com
Solution nuclear magnetic resonance (NMR) spectroscopy is a powerful tool to study
structures and dynamics of biomolecules under physiological conditions. As there are …
structures and dynamics of biomolecules under physiological conditions. As there are …
[HTML][HTML] A fragment-based approach to assess the ligandability of ArgB, ArgC, ArgD and ArgF in the L-arginine biosynthetic pathway of Mycobacterium tuberculosis
P Gupta, SE Thomas, SA Zaidan, MA Pasillas… - Computational and …, 2021 - Elsevier
The L-arginine biosynthesis pathway consists of eight enzymes that catalyse the conversion
of L-glutamate to L-arginine. Arginine auxotrophs (argB/argF deletion mutants) of …
of L-glutamate to L-arginine. Arginine auxotrophs (argB/argF deletion mutants) of …
Exploring the plasticity of the InhA substrate-binding site using new diaryl ether inhibitors
R Tamhaev, E Grosjean, H Ahamed, M Chebaiki… - Bioorganic …, 2024 - Elsevier
Tuberculosis (TB), caused by Mycobacterium tuberculosis (Mtb), remains a worldwide
scourge with more than 10 million people affected yearly. Among the proteins essential for …
scourge with more than 10 million people affected yearly. Among the proteins essential for …
Safe Polycationic Dendrimers as Potent Oral In Vivo Inhibitors of Mycobacterium tuberculosis: A New Therapy to Take Down Tuberculosis
S Mignani, VD Tripathi, D Soam, RP Tripathi… - …, 2021 - ACS Publications
The long-term treatment of tuberculosis (TB) sometimes leads to nonadherence to treatment,
resulting in multidrug-resistant (MDR) and extensively drug-resistant (XDR) tuberculosis …
resulting in multidrug-resistant (MDR) and extensively drug-resistant (XDR) tuberculosis …