Connor D T, Cetenko W A, Mullican M D, Sorenson R J, Unangst P C, Weikert R J, Adolphson R L, Kennedy J A, Thueson D O, Wright C D
Department of Chemistry, Parke-Davis Pharmaceutical Research Division, Warner-Lambert Company, Ann Arbor, Michigan 48105.
J Med Chem. 1992 Mar 6;35(5):958-65. doi: 10.1021/jm00083a023.
The synthesis and antiallergic activity of a series of novel benzothiophene-, benzofuran-, and naphthalenecarboxamidotetrazoles are described. A number of the compounds inhibit the release of histamine from anti-IgE stimulated basophils obtained from allergic donors. Optimal inhibition is exhibited in benzothiophenes with a 3-alkoxy substituent in combination with a 5-methoxy, 6-methoxy, or a 5,6-dimethoxy group. Compound 13c (CI-959) also inhibited respiratory burst of human neutrophils and the release of mediators from anti-IgE-stimulated human chopped lung.
本文描述了一系列新型苯并噻吩、苯并呋喃和萘羧酸酰胺四唑的合成及其抗过敏活性。许多化合物可抑制来自过敏供体的抗IgE刺激的嗜碱性粒细胞释放组胺。在具有3-烷氧基取代基并与5-甲氧基、6-甲氧基或5,6-二甲氧基组合的苯并噻吩中表现出最佳抑制作用。化合物13c（CI-959）还可抑制人中性粒细胞的呼吸爆发以及抗IgE刺激的人切碎肺组织中介质的释放。
