The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature. 52-90-4, Name is L-Cysteine, SMILES is N[C@@H](CS)C(O)=O, in an article , author is Shevyrin, Vadim A., once mentioned of 52-90-4, Product Details of 52-90-4.
Antimicrobial activity of amphipathic alpha,alpha-disubstituted beta-amino amide derivatives against ESBL – CARBA producing multi-resistant bacteria; effect of halogenation, lipophilicity and cationic character
The rapid emergence and spread of multi-resistant bacteria have created an urgent need for new antimicrobial agents. We report here a series of amphipathic alpha,alpha-disubstituted beta-amino amide derivatives with activity against 30 multi-resistant clinical isolates of Gram-positive and Gram-negative bacteria, including isolates with extended spectrum beta-lactamase – carbapenemase (ESBL-CARBA) production. A variety of halogenated aromatic side-chains were investigated to improve antimicrobial potency and minimize formation of Phase I metabolites. Net positive charge and cationic character of the derivatives had an important effect on toxicity against human cell lines. The most potent and selective derivative was the diguanidine derivative 4e with 3,5-di-brominated benzylic side-chains. Derivative 4e displayed minimum inhibitory concentrations (MIC) of 0.25-8 mu g/mL against Gram-positive and Gram-negative reference strains, and 2-32 mu g/mL against multi-resistant clinical isolates. Derivative 4e showed also low toxicity against human red blood cells (EC50 > 200 pg/mL), human hepatocyte carcinoma cells (HepG2: EC50>64 mu g/mL), and human lung fibroblast cells (MRC-5: EC50 > 64 mu g/mL). The broad-spectrum antimicrobial activity and low toxicity of diguanylated derivatives such as 4e make them attractive as lead compounds for development of novel antimicrobial drugs. (C) 2019 The Authors. Published by Elsevier Masson SAS.
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