Oesterlin R, Bell M R, Hlavac A G, McGarry R H, Gelotte K O, Bradford J C, Rozitis J
J Med Chem. 1980 Aug;23(8):945-8. doi: 10.1021/jm00182a024.
The synthesis of 1,3-disubstituted 2,4,5,6-tetrahydro-4,6,6-trimethyl-2-phenylcyclopenta[c]pyrrole-4-carboxamides is reported. The derivatives included R1 = R3 = H, R1 = CH2OH with R3 = H (16) or CH3, R1 = CH3 with R3 = CH2OH (17), and R1 = R3 = CH2OH. The monohydroxymethyl derivatives were as active as the parent cyclopentapyrrole, where R1 = R3 = CH3 (1), when administered orally in the pyloric ligated rat. The compounds lacking one or both CH3 groups at C-1 or C-3 were much less active. Compounds 16 and 17 inhibited histamine-induced gastric acid secretion in the dog.
报道了1,3 - 二取代的2,4,5,6 - 四氢 - 4,6,6 - 三甲基 - 2 - 苯基环戊并[c]吡咯 - 4 - 甲酰胺的合成。衍生物包括R1 = R3 = H、R1 = CH2OH且R3 = H（16）或CH3、R1 = CH3且R3 = CH2OH（17）以及R1 = R3 = CH2OH。在幽门结扎的大鼠中口服给药时，单羟甲基衍生物的活性与母体环戊并吡咯（其中R1 = R3 = CH3，即化合物1）相当。在C - 1或C - 3处缺少一个或两个CH3基团的化合物活性则低得多。化合物16和17可抑制犬体内组胺诱导的胃酸分泌。
