作者:M. Vittoria Diurno、Orazio Mazzoni、Eugenio Piscopo、Antonio Calignano、Federico Giordano、Adele Bolognese
DOI:10.1021/jm00093a025
日期:1992.7
A new series of 2-(4- and 3-substituted phenyl)-3-[3-(N,N-dimethylamino) propyl]-1,3-thiazolidin-4-ones were synthesized, characterized, and evaluated for their ability to inhibit the contractions induced by histamine on guinea pig ileum. The measurement of pA2 values suggested that the reported compounds showed H1-antagonism. The more active compounds 5, 9, and 13 exhibited activity close to that
合成了一系列新的2-(4-和3-取代的苯基)-3- [3-(N,N-二甲基氨基)丙基] -1,3-噻唑烷丁-4-酮,表征并评价了它们的能力抑制组胺诱导的豚鼠回肠收缩。pA2值的测量表明所报道的化合物表现出H1拮抗作用。活性更高的化合物5、9和13表现出的活性接近美吡拉敏。