Premium
Polycyclic N ‐Heterocyclic compounds. 50 . 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‐2 H ‐thieno‐[2,3‐ h ]pyrimido[2,1‐ f ][1,6]naphthyridines and their precursor
Author(s) -
Sasaki Kenji,
Rouf Abu Shara S.,
Hirota Takashi,
Nakaya Naoki
Publication year - 1999
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.5570360221
Subject(s) - chemistry , milrinone , chloride , contraction (grammar) , medicinal chemistry , in vitro , benzoyl chloride , stereochemistry , organic chemistry , biochemistry , hemodynamics , medicine
Some novel 5‐hydroxyalkylamino‐1,2‐dihydrothieno[2,3‐ h ][1,6]naphthyridines were prepared by the reaction of 5‐chloro‐1,2‐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.