35085-34-8Relevant academic research and scientific papers
Rational Design, Synthesis, and Preliminary Structure-Activity Relationships of α-Substituted-2-Phenylcyclopropane Carboxylic Acids as Inhibitors of Salmonella typhimurium O-Acetylserine Sulfhydrylase
Pieroni, Marco,Annunziato, Giannamaria,Beato, Claudia,Wouters, Randy,Benoni, Roberto,Campanini, Barbara,Pertinhez, Thelma A.,Bettati, Stefano,Mozzarelli, Andrea,Costantino, Gabriele
, p. 2567 - 2578 (2016/04/10)
Cysteine is a building block for several biomolecules that are crucial for living organisms. The last step of cysteine biosynthesis is catalyzed by O-acetylserine sulfydrylase (OASS), a highly conserved pyridoxal 5′-phosphate (PLP)-dependent enzyme, present in different isoforms in bacteria, plants, and nematodes, but absent in mammals. Beside the biosynthesis of cysteine, OASS exerts a series of moonlighting activities in bacteria, such as transcriptional regulation, contact-dependent growth inhibition, swarming motility, and induction of antibiotic resistance. Therefore, the discovery of molecules capable of inhibiting OASS would be a valuable tool to unravel how this protein affects the physiology of unicellular organisms. As a continuation of our efforts toward the synthesis of OASS inhibitors, in this work we have used a combination of computational and spectroscopic approaches to rationally design, synthesize, and test a series of substituted 2-phenylcyclopropane carboxylic acids that bind to the two S. typhymurium OASS isoforms at nanomolar concentrations.
BETA-MERCAPTO-PROPANAMIDE DERIVATIVES USEFUL IN THE TREATMENT OF CARDIOVASCULAR DISEASES
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, (2008/06/13)
Compounds of formula STR1 wherein R, R 1, R 2, Het and n have the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain them as active ingredients are described. The compounds of formula I are useful in the treatment of cardiovascular diseases.
Beta-mercapto-propanamide derivatives useful in the treatment of cardiovascular diseases
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, (2008/06/13)
Compounds of formula wherein R, R1, R2, Het and nhave the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain them as active ingredients are described. The compounds of formula I are useful in the treatment of cardiovascular diseases.
