Chemical and Pharmaceutical Bulletin p. 1538 - 1548 (1999)
Update date:2022-07-30
Topics:
Kitano, Masafumi
Kojima, Atsuyuki
Nakano, Kazuhiro
Miyagishi, Akira
Noguchi, Tsuyoshi
Ohashi, Naohito
A series of N-(aminoiminomethyl)-1H-indole carboxamide derivatives were synthesized and their inhibitory potencies against the Na+/H+ exchanger were measured. Variation of the carbonylguanidine group at the 2- to 7- position of the indole ring system showed that a substitution at the 2- position improved the Na+/H+ exchanger inhibitory activity the most in vitro. This led to the synthesis and evaluation of an extensive series of N- (aminoiminomethyl)-1H-indole-2-carboxamide derivatives. Derivatives having an alkyl or substituted alkyl group at the 1-position of the indole ring system showed higher levels of in vitro activities. N-(aminoiminomethyl)-1-(2- phenylethyl)-1H-indole-2-carboxamide (49) had the strongest activity.
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