Polycyclic N-heterocyclic compounds. 50 [1]. Synthesis and pharmacological evaluation of 2,3,6,7-tetrahydrothieno[2,3-h]- imidazo[2,1 - f] [1,6] naphthyridines, 3,4,7,8-tetrahydro-2H-thieno[2,3-h]pyrimido[2,1- f][1,6]naphthyridines and their precursor

Kenji Sasaki, Abu Shara S. Rouf, Takashi Hirota, Naoki Nakaya

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Some novel 5-hydroxyalkylamino-1,2-dihydrothieno[2,3- h][1,6]naphthyridines were prepared by the reaction of 5-chloro-l,2- dihydrothieno[2,3-h][1,6]naphthyridine derivatives with some aminoalcohols in the presence of base. These derivatives were cyclized to the corresponding imidazo or pyrimido derivatives. The bronchodilatory activity of these compounds was evaluated on the basis of their relaxation activity to tracheal contraction induced by carbamylcholine chloride as a primary in vitro assays. Effect of some naphthyridines on carbamylcholine chloride-induced contractions of trachea in the presence or absence of milrinone or 4-(3- butoxy-4-methoxyphenyl)imidazolidin-2-one, which is inhibitor of phosphodiesterase III or IV, were also evaluated.

Original languageEnglish
Pages (from-to)461-465
Number of pages5
JournalJournal of Heterocyclic Chemistry
Issue number2
Publication statusPublished - Jan 1 1999


ASJC Scopus subject areas

  • Organic Chemistry

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