• Journal of Pharmaceutical Investigation
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• v.22 no.3
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• pp.49-63
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• 1992

Two different types of chemical manipulations of dobutamine were investigated in order to develop novel, improved cardiotonic drugs. Three new analogues of carbostyril, in which the m-hydroxy group of dobutamine was isosterically modified with an amide type carbostyril system, were synthesized from, ${\rho}-methoxyphenethylamine$ via multi-steps. Two analogues of (2'-aminoethyl)-1-hydroxy-2-pyridone system which has isosteric structural similarity with dopamine without having the COMT vulnerable m-hydroxy group were synthesized via 12 synthetic steps. Their biological stabilities in various media and inotropic activities were evaluated.

• YAKHAK HOEJI
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• v.39 no.5
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• pp.506-510
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• 1995

The 5-(2'-(N-(1-methyl-3'-carbamylphenyl)-n-propyl))aminoethyl)-8- hydroxy-4-methyl-carbostyril derivatives which have isoelectronic and isosteric structural similarity with dobutamine without having the Catechol-O-Methyltransferase (COMT) vulnerable m-hydroxy group were synthesized via 7 synthetic steps, and their stabilities in phosphate buffer solution(pH=7.4), human blood. 80% human plasma and 20% rat liver homogenate were determined in vitro condition.