Results 41 to 50 of about 1,660 (188)
A Novel Antimalarial Agent that Inhibits Protein Synthesis in Plasmodium falciparum. [PDF]
Angew Chem Int Ed EnglCompound 31 represents a promising avenue for the development as an antimalarial agent with a potent activity profile (PfNF54 IC50 ± s.d. = 3.9 ± 0.4 nM). It has a novel mode of action by binding to cytosolic ribosomal subunits, thereby inhibiting protein synthesis in the parasite.
Bravo P +16 more
europepmc +2 more sources
Predicting Drug Resistance Using Deep Mutational Scanning
Molecules, 2020 Drug resistance is a major healthcare challenge, resulting in a continuous need to develop new inhibitors. The development of these inhibitors requires an understanding of the mechanisms of resistance for a critical mass of occurrences.
Gur Pines +2 more
doaj +1 more source
Growth medium-dependent antimicrobial activity of early stage MEP pathway inhibitors.
PLoS ONE, 2018 The in vivo microenvironment of bacterial pathogens is often characterized by nutrient limitation. Consequently, conventional rich in vitro culture conditions used widely to evaluate antibacterial agents are often poorly predictive of in vivo activity ...
Sara Sanders +5 more
doaj +1 more source
Lipophilic prodrugs of FR900098 are antimicrobial against Francisella novicida in vivo and in vitro and show GlpT independent efficacy. [PDF]
PLoS ONE, 2012 Bacteria, plants, and algae produce isoprenoids through the methylerythritol phosphate (MEP) pathway, an attractive pathway for antimicrobial drug development as it is present in prokaryotes and some lower eukaryotes but absent from human cells.
Elizabeth S McKenney +8 more
doaj +1 more source
Guangxi Zhiwu, 2023 Gentiana macrophylla is a traditional Chinese herbal medicine for treating jaundice, hepatitis, and stomachic and choleretic ailments, and its main secondary metabolites are secoiridiod glycosides represented by gentiopicroside.
Huanhuan FU +5 more
doaj +1 more source
The MVA pathway bypasses fosmidomycin toxicity in PfMev parasites.
, 2020 A) Diagram of the parasite cell showing that the endogenous MEP pathway is localized with the apicoplast organelle of the parasite, with IPP and DMAPP presumably being exported out of the organelle.
Hans B. Liu (8452467) +11 more
core +1 more source
Antibacterial and antitubercular activity of fosmidomycin, FR900098, and their lipophilic analogs [PDF]
Bioorganic & Medicinal Chemistry Letters, 2011 The nonmevalonate pathway (NMP) of isoprene biosynthesis is an exciting new route toward novel antibiotic development. Inhibitors against several enzymes in this pathway are currently under examination. A significant liability of many of these agents is poor cell penetration.
Eugene, Uh +7 more
openaire +2 more sources
Synergy of fosmidomycin (FR-31564) and other antimicrobial agents [PDF]
Antimicrobial Agents and Chemotherapy, 1982 Fosmidomycin (FR-31564), a phosphonic acid derivative, was combined with cefazolin, cephalexin, ampicillin, carbenicillin, ticarcillin, gentamicin, and trimethoprim. Synergy between fosmidomycin and penicillins or cephalosporins was found for 37 to 52% of the Enterobacteriaceae tested.
H C, Neu, T, Kamimura
openaire +2 more sources
Molecules, 2014 Fourteen new fosmidomycin analogues with altered metal chelating groups were prepared and evaluated for inhibition of E. coli Dxr, M. tuberculosis Dxr and the growth of P. falciparum K1 in human erythrocytes.
René Chofor +7 more
doaj +1 more source
Biologia Plantarum, 2011 Although crosstalk between cytosolic and plastidic terpenoid pathways has been validated in many plant species, we report here for the first time a striking elevation of the nucleus-encoded artemisinin biosynthesis relevant DBR2 mRNA following the ...
Q. -P. Zeng +3 more
doaj +1 more source