743392-72-5Relevant academic research and scientific papers
Synthesis and anticonvulsant activity of a new class of 2- [(arylalkyl)amino]alkanamide derivatives
Pevarello, Paolo,Bonsignori, Alberto,Dostert, Philippe,Heidempergher, Franco,Pinciroli, Vittorio,Colombo, Maristella,McArthur, Robert A.,Salvati, Patricia,Post, Claes,Fariello, Ruggero G.,Varasi, Mario
, p. 579 - 590 (1998)
Although most epilepsies are adequately treated by conventional antiepileptic therapy, there remains an unfulfilled need for safer and more effective anticonvulsant agents. Starting from milacemide, a weak anticonvulsant, and trying to elucidate its mechanism of action, we discovered a structurally novel class of potent and preclinically safe anticonvulsants. Here we report the structure-activity relationship (SAR) study within this series of compounds. Different parts of the structural lead 2-[[4-(3-chlorobenzoxy)benzyl]amino]acetamide (6) were thus varied (Figure 1), and many potent anticonvulsants were found. As an outcome of this study, 57 ((S)-2-[[4-(3-fluorobenzoxy)benzyl]amino]propanamide methanesulfonate, PNU-151774E) emerged as a promising candidate for further development for its potent anticonvulsant activity and outstanding therapeutic indexes (TIs) in different animal tests.
N-phenylalkyl substituted α-amino carboxamide derivatives and process for their preparation
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, (2008/06/13)
N-phenylalkyl substituted α-amino carboxamide derivatives of formula (I) STR1 wherein R is C1 -C8 alkyl, C3 -C8 cycloalkyl, furyl, thienyl, pyridyl or unsubstituted or substituted phenyl; A is a --(CH2/sub
