title: Synthesis and pharmacological evaluation of new 4-2-(7-heterocyclemethoxynaftalen-2-ylmethoxy)ethylbenzoic acids as LTD(4)-antagonists.
abstract: A group of new 4-[2-(7-heterocyclemethoxynaftalen-2-ylmethoxy)ethyl]benzoic acids have been synthesized and pharmacologically evaluated as LTD(4)-antagonists. Thiazole derivatives, especially 4-[2-[7-(4-cyclobutylthiazole-2-ylmethoxyl)naphthalen- 2-ylmetho-xy]et hyl]benzoic acid, present considerable activity and improved pharmacokinetic profiles in comparison with our quinoline containing lead molecule confirming the interest of our compounds as potentially oral antiasthmatics and that the 4-alkylthiazole system can be considered as bioisosteric of the quinoline ring at least in our series of compounds.
authors.affiliation: Departament de Química Organica, Universitat of Barcelona, Martí Franques, 1-11, E-08028, Barcelona, Spain.
authors.forename: B
authors.initials: B
authors.lastname: Ballart
authors.forename: J
authors.initials: J
authors.lastname: Martí
authors.forename: D
authors.initials: D
authors.lastname: Velasco
authors.forename: F
authors.initials: F
authors.lastname: López-Calahorra
authors.forename: J
authors.initials: J
authors.lastname: Pascual
authors.forename: M
authors.initials: M
authors.lastname: Luisa García
authors.forename: F
authors.initials: F
authors.lastname: Cabré
authors.forename: D
authors.initials: D
authors.lastname: Mauleón
mesh_terms: D000818:Animals; D001565:Benzoates / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D004341:Drug Evaluation; D006168:Guinea Pigs; D017998:Leukotriene D4 / Q000037:antagonists & inhibitors*; D008297:Male; D051379:Mice
chemical_list: D001565:Benzoates; D017998:Leukotriene D4