当前位置: X-MOL 学术Med. Chem. Res. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Synthesis and analgesic potential of 4-[4–chloro-3- (trifluoromethyl)-phenyl]-4-piperidinol analogues against pain model in mice
Medicinal Chemistry Research ( IF 2.6 ) Pub Date : 2022-02-24 , DOI: 10.1007/s00044-022-02860-8
Shazia Haider 1 , Zafar Saied Saify 1, 2 , Nousheen Mushtaq 1 , Nasreen Begum 2, 3 , Faheema Siddiqui 4 , Toqeer Ahmed Rao 5 , Tabinda Zareen Mallick 6
Affiliation  

In the study of designing pharmacophore models for analgesic, a series of 4-[4–chloro-3- (trifluoromethyl)-phenyl]-4-piperidinol (TFMP) derivatives were synthesized and characterized by physical and spectral method (HR-EIMS, HR-FABMS, 1H-NMR, 13C-NMR, UV, and FT-IR). The analgesic action of the synthesized derivatives was estimated by means of Hot Plate Method. Most of the compounds displayed potent analgesic efficacy and an ultrashort to long duration of action. The results indicate that these compounds are useful as analgesics. In the presence of naloxone they displayed pain reliving effect. In conclusion, among active compounds 3 (188%), 5 (137%), 6 (162%), and 8 (107%) respectively, emerged as most effective analgesic and they depressed peripheral and centrally mediated pain by opioid independent systems.



中文翻译:

4-[4-氯-3-(三氟甲基)-苯基]-4-哌啶醇类似物的合成及其对小鼠疼痛模型的镇痛作用

在设计镇痛药药效团模型的研究中,合成了一系列4-[4-氯-3-(三氟甲基)-苯基]-4-哌啶醇(TFMP)衍生物,并采用物理光谱法(HR-EIMS, HR-FABMS、1 H-NMR、13 C-NMR、UV 和 FT-IR)。采用热板法估计合成衍生物的镇痛作用。大多数化合物显示出有效的镇痛功效和超短至长的作用持续时间。结果表明这些化合物可用作镇痛剂。在纳洛酮存在的情况下,它们表现出缓解疼痛的效果。总之,在活性化合物3 (188%)、5 (137%)、6 (162%) 和8(107%) 分别成为最有效的镇痛剂,它们通过阿片类药物独立系统抑制外周和中枢介导的疼痛。

更新日期:2022-02-24
down
wechat
bug