Design, synthesis and evaluation of novel hydroxyamides as orally available anticonvulsants

…, PW Lenkowski, I Choudhury-Mukherjee, SH Ko…

Index: Schenck, Hilary A.; Lenkowski, Paul W.; Choudhury-Mukherjee, Indrani; Ko, Seong-Hoon; Stables, James P.; Patel, Manoj K.; Brown, Milton L. Bioorganic and Medicinal Chemistry, 2004 , vol. 12, # 5 p. 979 - 993

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Citation Number: 64

Abstract

Themisone, also known as Atrolactamide, was found, in the 1950s, to be a very potent anticonvulsant. It was hypothesized that the-CF3 substitution would maintain the anticonvulsant activity. Anticonvulsant testing of our novel compounds by the National Institute of Health's Anticonvulsant Screening Project of the Antiepileptic Drug Discovery Program identified analogue 1, 3, 3, 3-trifluoro-2-hydroxy-2-phenyl-propionamide, to have ...