73323-91-8Relevant articles and documents
Searching for new antiarrhythmic agents: Evaluation of meta- hydroxymexiletine enantiomers
Catalano, Alessia,Budriesi, Roberta,Bruno, Claudio,Di Mola, Antonia,Defrenza, Ivana,Cavalluzzi, Maria Maddalena,Micucci, Matteo,Carocci, Alessia,Franchini, Carlo,Lentini, Giovanni
, p. 511 - 516 (2013/10/01)
Mexiletine is a very well-known class IB antiarrhythmic drug, whose enantiomers differ in both pharmacodynamic and pharmacokinetic properties, the (R)-isomer being the eutomer on experimental arrhythmias and in binding studies on cardiac voltage-gated sodium channels. meta-Hydroxymexiletine (MHM) is a minor metabolite of mexiletine, which has demonstrated to be more potent than the parent compound. Herein we report the synthesis and biological evaluation of MHM enantiomers for their potential antiarrhythmic activity. The same stereoselectivity pattern observed for mexiletine was found for MHM: the (R)-enantiomer of MHM was the eutomer on ac-arrhythmia also showing a negative inotropism higher than the one displayed by mexiletine and, at the same time, a decreased vasorelaxant activity on guinea-pig left atrium and guinea-pig ileum longitudinal smooth muscle.
ANDROGEN RECEPTOR MODULATING COMPOUNDS
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Page/Page column 47, (2011/05/11)
Compounds of formula (I) wherein R1 to R16, A. B and E are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as tissue-selective androgen receptor modulators (SARM) and are particularly useful as medicaments in the treatment of prostate cancer and other AR dependent conditions and diseases where AR antagonism is desired.
Novel modifications in the series of O-(2-phthalimidoethyl)-N-substituted thiocarbamates and their ring-opened congeners as non-nucleoside HIV-1 reverse transcriptase inhibitors
Spallarossa, Andrea,Cesarini, Sara,Ranise, Angelo,Bruno, Olga,Schenone, Silvia,La Colla, Paolo,Collu, Gabriella,Sanna, Giuseppina,Secci, Barbara,Loddo, Roberta
experimental part, p. 1650 - 1663 (2009/05/26)
The structure-activity relationships (SARs) of N-aryl-O-(2-phthalimidoethyl)thiocarbamates (C-TCs) and their imide ring-opened congeners (O-TCs) as non-nucleoside HIV-1 reverse transcriptase inhibitors were further investigated. The SAR strategy involved