Kennedy, Andrew J. published the artcileSynthesis and antimicrobial evaluation of amixicile-based inhibitors of the pyruvate-ferredoxin oxidoreductases of anaerobic bacteria and Epsilonproteobacteria, Recommanded Product: 2-Bromo-4-methoxybenzoic acid, the main research area is aminoalkyl nitrothiazolyl benzamide preparation SAR antibacterial docking PFOR inhibitor.
Synthesis of the amixicile scaffolds I [R = CH2NH3, (CH2)3NH3, 4-piperidinyl, etc.; R1 = H, F; R2 = H, Me, F, Cl, CF3; R3 = H, Me, OMe, F, Cl, CN, CF3] and study of their direct pyruvate-ferredoxin oxidoreductases (PFOR) inhibition assays, and MIC tests against Clostridium difficile, Campylobacter jejuni, and Helicobacter pylori guided by docking simulations was interrogated. Docking simulations revealed that the nitro group present in nitazoxanide interacts with the protonated N4′-aminopyrimidine of thiamine pyrophosphate. The ortho-propylamine on the benzene ring formed an electrostatic interaction with an aspartic acid moiety (B456) of PFOR that correlated with improved PFOR-inhibitory activity and potency by MIC tests. Aryl substitution with electron-withdrawing groups and substitutions of the propylamine with other alkyl amines or nitrogen-containing heterocycles both improved PFOR inhibition and, in many cases, biol. activity against C. difficile. Docking simulation results correlated well with mechanistic enzymol. and NMR studies that show members of this class of antimicrobials to be specific inhibitors of vitamin B1 function by proton abstraction, which is both novel and likely to limit mutation-based drug resistance.
Antimicrobial Agents and Chemotherapy published new progress about Amines Role: PAC (Pharmacological Activity), PRP (Properties), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), PREP (Preparation), USES (Uses). 74317-85-4 belongs to class bromides-buliding-blocks, name is 2-Bromo-4-methoxybenzoic acid, and the molecular formula is C8H7BrO3, Recommanded Product: 2-Bromo-4-methoxybenzoic acid.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary