咪唑并[2,1 - b]苯并噻唑酸及一些具有抗炎和镇痛活性的相关化合物的合成与构效关系研究
Synthesis and SAR study of imidazo[2,1-b]benzothiazole acids and some related compounds with anti-inflammatory and analgesic activities.
作者信息
Palagiano F, Arenare L, De Caprariis P, Grandolini G, Ambrogi V, Perioli L, Filippelli W, Falcone G, Rossi F
机构信息
Dipartimento di Chimica Farmaceutica e Tossicologica, Facoltà di Farmacia, Università degli Studi di Napoli Federico II, Italy.
出版信息
Farmaco. 1996 Jul;51(7):483-91.
Some (un)substituted imidazo[2,1-b]benzothiazole carboxylic or acetic acids and some related compounds, i.e. imidazo[2,1-b]naphthol[2,1-d]thiazole, 4H-imidazo[2,1-c][1,4]benzothiazine, 4,5-dihydroimidazo[2,1-d][1,5]benzothiazepine carboxylic and acetic acids were synthesized and tested in vivo in order to study the structure-activity relationships (SAR) of their antiinflammatory and analgesic activities. Pharmacological assays confirmed the interest of this class of compounds as potential antiinflammatory and analgesic drugs with low side effects.
合成了一些（未）取代的咪唑并[2,1-b]苯并噻唑羧酸或乙酸以及一些相关化合物，即咪唑并[2,1-b]萘酚[2,1-d]噻唑、4H-咪唑并[2,1-c][1,4]苯并噻嗪、4,5-二氢咪唑并[2,1-d][1,5]苯并硫氮杂卓羧酸和乙酸，并在体内进行了测试，以研究它们抗炎和镇痛活性的构效关系（SAR）。药理试验证实了这类化合物作为具有低副作用的潜在抗炎和镇痛药的价值。
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