Photochemistry Department (Heterocyclic Unit), National Research Center, Dokki, Giza, Egypt.
Arch Pharm (Weinheim). 2011 Aug;344(8):543-51. doi: 10.1002/ardp.201100020. Epub 2011 Jun 16.
In an effort to establish new candidates with improved analgesic and anti-inflammatory activities, we reported here the synthesis and in-vivo analgesic and anti-inflammatory evaluation of various series of 2-substituted-3a,4,9,9a-tetrahydro-4,9-benzeno-benz[f]isoindole-1,3-diones: [4-Bromobutoxy] 6, 5-bromopentoxy 7, [4-(4-phenylpiperazin-1-yl)butoxy] 9, [5-(4-phenylpiperazin-1-yl)pentoxy] 10, 2-(2(4)-(4-phenylpiperazin-1-yl)-2-oxoethyl/4-oxobutyl 17, 19, [2(4)-(4-methylpiperazin-1-yl]-2-oxoethyl/4-oxobutyl 20, 22, [2(4)-morpholino-2-oxoethyl/4-oxobutyl] 23, 25, and 2(4)-(piperidin-1-yl)2-oxoethyl/4-oxobutyl) 26 and 28. The newly synthesized compounds were characterized by (IR, (1)H-, (13)C-NMR, and mass spectra). The representative compounds were evaluated as analgesic and anti-inflammatory activities. Compounds 9, 19, 22, 25, and 28 exhibited activities higher than the reference drug.
为了寻找具有更好镇痛和抗炎活性的新候选药物，我们在此报告了一系列 2-取代-3a,4,9,9a-四氢-4,9-苯并[f]异吲哚-1,3-二酮的合成及体内镇痛和抗炎评价：[4-溴丁氧基] 6, 5-溴戊氧基 7, [4-(4-苯并哌嗪-1-基)丁氧基] 9, [5-(4-苯并哌嗪-1-基)戊氧基] 10, 2-(2(4)-(4-苯并哌嗪-1-基)-2-氧代乙基/4-氧代丁基 17, 19, [2(4)-(4-甲基哌嗪-1-基]-2-氧代乙基/4-氧代丁基 20, 22, [2(4)-吗啉-2-氧代乙基/4-氧代丁基] 23, 25, 和 2(4)-(哌啶-1-基)2-氧代乙基/4-氧代丁基 26 和 28。新合成的化合物通过（IR、（1）H-NMR、（13）C-NMR 和质谱）进行了表征。代表性化合物被评估为镇痛和抗炎活性。化合物 9、19、22、25 和 28 的活性高于参考药物。
