Results 301 to 310 of about 154,675 (336)

Identification and Substrate Specificity of β-Ketoacyl (Acyl Carrier Protein) Synthase III (mtFabH) from Mycobacterium tuberculosis

, 2000
Keum-Hwa Choi, Laurent Kremer, Gurdyal S. Besra, Charles O. Rock   +3 more
openalex   +1 more source

Isoniazid‐Dihydropyrimidinone Molecular Hybrids: Design, Synthesis, Antitubercular Activity, and Cytotoxicity Investigations with Computational Validation

ChemMedChem, EarlyView.
Antitubercular evaluation of a novel library of isoniazid‐dihydropyrimidinone molecular hybrids (8a–8n) discloses a potent compound with MIC = 0.39μg mL−1 against M. tuberculosis mc26230. Cytotoxicity, stability, and in silico studies, including molecular docking and ADME/T (absorption, distribution, metabolism, excretion, and toxicity) analysis ...
Gobind Kumar, Pule Seboletswe, Sahil Mishra, Neha Manhas, Safiyah Ghumran, Nagaraju Kerru, Françoise Roquet‐Banères, Maëlle Foubert, Laurent Kremer, Gaurav Bhargava, Parvesh Singh   +10 more
wiley   +1 more source

Systematic Review on 1,2,3‐Oxadiazoles, 1,2,4‐Oxadiazoles, and 1,2,5‐Oxadiazoles in the Antimycobacterial Drug Discovery

ChemMedChem, EarlyView.
The review focuses on relationships of oxadiazole derivative structures and their antimycobacterial activity including target structures in mycobacteria, in vitro or in vivo pharmacokinetic parameters, and toxicity. Apart from direct antimycobacterial activity, some 1,2,4‐oxadiazole derivatives can potentiate the antimycobacterial effect of ethionamide
Marta Kučerová‐Chlupáčová
wiley   +1 more source

Modifying the Thioester Linkage Affects the Structure of the Acyl Carrier Protein. [PDF]

Angew Chem Int Ed Engl, 2019
Sztain T, Patel A, Lee DJ, Davis TD, McCammon JA, Burkart MD.   +5 more
europepmc   +1 more source

Is Mycobacterial InhA a Suitable Target for Rational Drug Design?

ChemMedChem, EarlyView.
InhA is the target of isoniazid, a first‐line antituberculosis drug. Isoniazid is, in fact, a prodrug that needs to be activated. Researchers are trying to develop direct inhibitors of InhA. This includes the resolution of crystallographic structures. The Protein Data Bank contains over a hundred InhA structures.
Julien Rizet, Laurent Maveyraud, David Rengel, Valérie Guillet, Gabriel Publicola, Frédéric Rodriguez, Christian Lherbet, Lionel Mourey   +7 more
wiley   +1 more source

Improved C5‐amide bioisosteres for human neuraminidase 1 inhibitors based on 2‐deoxy‐2,3‐didehydro‐N‐acetyl neuraminic acid (DANA)

ChemMedChem, Accepted Article.
Neuraminidase enzymes (NEU) play a crucial role in many physiological and pathological conditions. Humans have four isoenzymes of NEU and their specific roles continue to be investigated. Isoenzyme‐selective inhibitors are needed as research tools and may lead to future therapeutics.
Mostafa Radwan, Elisa Garcia Carvajal, Christopher W Cairo   +2 more
wiley   +1 more source

Cancer therapy‐related cardiotoxicity is associated with distinct alterations of the myocardial lipidome

European Journal of Heart Failure, EarlyView.
Lipidome changes in anthracycline‐induced cardiotoxicity (AIC). Aims Anthracyclines are key components of various chemotherapy regimens, but their clinical utility is limited by severe cardiotoxic side effects. Previous studies have suggested that anthracycline‐induced cardiotoxicity (AIC) may be driven by alterations in myocardial lipid metabolism ...
Vera M. Braun, Anna Foryst‐Ludwig, Ulf Landmesser, István Baczkó, Hendrik Milting, Ulrich Kintscher, Niklas Beyhoff   +6 more
wiley   +1 more source

On the Synthesis of [1,3]Azaphospholo[4,5‐f]quino(xa)lines and 2,3‐Dihydro‐[1,3]azaphospholo[4,5‐f]quino(xa)line 1‐oxides

European Journal of Organic Chemistry, EarlyView.
Syntheses of quinoline and quinoxaline derivatives fused with phosphacycles were developed from commercially available quinolin‐6‐amine and quinoxalin‐6‐amine. Abstract Despite their potential in areas such as medicinal chemistry and organic materials, scaffolds in which quinoline and quinoxaline are fused to phosphacycles such as 1,3‐oxaphosphole, 1,3‐
Mohamed Ali Dridi, Mohamed Hasyeoui, Frédéric Lassagne, William Erb, Charline Piroud, Thomas Robert, Stéphane Bach, Ali Samarat, Soufiane Touil, Florence Mongin   +9 more
wiley   +1 more source

Synthetic Biology‐Based Engineering Living Therapeutics for Antimicrobial Application

Exploration, EarlyView.
This perspective highlights synthetic biology‐driven antibacterial strategies, focusing on three innovative approaches: engineered bacteriophages for precision bacterial targeting, reprogrammed microbes that detect quorum‐sensing signals or metabolites to release antimicrobials, and engineering mammalian cells that recognize pathogen‐associated ...
Shun Huang, Shuihao Zhao, Haijie Zhao, Mingzhang Wen, Zhong Guo   +4 more
wiley   +1 more source

Self‐Emulsifying Biocatalysis Based on an Amphipathic Protein BslA‐Modified Esterase Functioning as a Fine‐Tuned System for Oil Hydrolysis

Food Bioengineering, EarlyView.
BslA is a promising tool to create an robust self‐emulsifying biocatalysis platform by reducing the droplet sizes of emulsion and improving its stability. It could guarantee the efficient hydrolysis of astaxanthin esters catalyzed by Est3‐14 without extra emusifier, increasing the yield of free astaxanthin to 184 μg·mL−1.
Xiaoxuan Yao, Kunpeng Gao, Hao Dong, Qian Sun, Jingyuan Liu, Yang Hu, Jianan Sun, Xiangzhao Mao   +7 more
wiley   +1 more source