Pharmacophore based synthesis of 3-chloroquinoxaline-2-carboxamides as serotonin3 (5-HT3) receptor antagonist
Pharmacophore based synthesis of 3-chloroquinoxaline-2-carboxamides as serotonin3 (5-HT3) receptor antagonist
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DOI：
10.1248/bpb.27.1403
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发表时间：
2004-09-01
影响因子：
2
通讯作者：
Pandi, PV
中科院分区：
文献类型：
--
作者：
Mahesh, R;Perumal, RV;Pandi, PV
以3-氯-2-喹喔啉酰氯为原料，与对氨基苯酚的Mannich碱在微波条件下缩合，合成了一系列3-氯喹喔啉-2-甲酰胺类化合物。在豚鼠回肠纵行肌间神经丛（LMMP）中，用5-羟色胺（5-HT 3）受体激动剂2-甲基-5-HT对合成的化合物进行拮抗活性评价。化合物3g表现出与标准拮抗剂昂丹司琼（PA（2）6.9）相当的5-HT 3拮抗活性（PA（2）6.4），而其他化合物表现出轻度至中度的5-HT 3拮抗活性。
A series of 3-chloroquinoxaline-2-carboxamides were designed and prepared by the condensation of 3-chloro-2-quinoxaloylchloride with appropriate Mannich bases of the p-aminophenol in the microwave environment. The synthesized compounds were evaluated for serotonin(3) (5-HT3) receptor antagonistic activities in longitudinal muscle-myenteric plexus (LMMP) preparation from guinea pig ileum against the 5-HT3 agonist, 2-methyl-5-HT. Compound 3g exhibited comparable 5-HT3 antagonistic activity (pA(2) 6.4) to that of standard antagonist Ondansetron (pA(2) 6.9), while the other compounds exhibited mild to moderate 5-HT3 antagonistic activities.