Screening for antidepressant, sedative and analgesic activities of novel fused thiophene derivatives
Screening for antidepressant, sedative and analgesic activities of novel fused thiophene derivatives
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新型稠合噻吩衍生物抗抑郁、镇静、镇痛活性的筛选
DOI：
10.2478/v10007-007-0041-5
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发表时间：
2008
影响因子：
2.7
通讯作者：
G. Elmegeed
中科院分区：
文献类型：
--
作者：
W. Wardakhan;O. Abdel;G. Elmegeed
新型稠合噻吩衍生物的抗抑郁、镇静和镇痛活性筛选本研究旨在合成含杂环的稠合苯并噻吩衍生物。四氢苯并[B]噻吩衍生物1a、B与异硫氰酸乙氧羰基酯反应得到硫脲衍生物2a、B。后一产物环化得到环化的苯并[B]噻吩并嘧啶衍生物3a、B。化合物2a、B和3a通过与一些化学试剂反应进行一系列杂环化反应，得到新的苯并[B]噻吩并嘧啶衍生物5a、B至8a-c。此外，这项工作被扩展到研究的潜在作用的新合成的硫脲衍生物2a和苯并[B]噻吩并嘧啶衍生物3a，5 B，6 a和8 B作为抗抑郁药，镇静剂或镇痛剂在两个剂量（15或30毫克kg-1体重）。部分化合物（2a、3a和5 b）在强迫游泳实验中显示出轻度的抗抑郁活性。没有化合物显示镇静作用。腹腔注射醋酸引起的小鼠内脏疼痛在高剂量下被所有化合物显著抑制。为了防止经济衰退，我们必须采取新的预防措施，以预防结核病，并采取新的预防措施，以预防结核病的发生。噻托溴铵衍生物2a，B b具有四氢苯并[B]噻托溴铵衍生物1a，B b的结构。本发明公开了一种苯并[B]噻吩并嘧啶3a、B衍生物。Spojevi 2a，B i 3a用于预防苯并[B]噻吩并嘧啶5a，B-8a-c的杂环化反应。抗抑郁、镇静和抗抑郁药的新衍生物2a、苯并[B]噻嘧啶3a、5 B、6 a和8 B b给药一次（15 mg/kg）。第2a、3a和5 b号决议规定了反腐败和预防腐败的措施，但这些措施并没有得到有效执行。Visceralna bol inducirana i.p. injekcijom octene kiseline u miševa značajno je birana sa svim spojevima，ali u visokim dozama.
Screening for antidepressant, sedative and analgesic activities of novel fused thiophene derivatives This study was aimed at the synthesis of fused benzothiophene derivatives containing heterocyclic moiety. The reaction of the tetrahydrobenzo[b]thiophene derivatives 1a,b with ethoxycarbonylisothiocyanate afforded the thiourea derivatives 2a,b. Cyclization of the latter products gave the annulated benzo[b]thienopyrimidine derivatives 3a,b. Compounds 2a,b and 3a underwent a series of heterocyclization reactions through the reaction with some chemical reagents to give the new benzo[b]thienopyrimidine derivatives 5a,b to 8a-c. Also, this work was extended to study the potential role of the novel synthesized thiourea derivative 2a and benzo[b]thienopyrimidine derivatives 3a, 5b, 6a and 8b as antidepressant, sedative or analgesic agents at two doses (15 or 30 mg kg-1 body mass). Some compounds (2a, 3a and 5b) showed mild antidepressant activity in the forced-swimming test. No compound showed sedative effect. Visceral pain evoked by i.p. injection of acetic acid in mice was significantly inhibited by all compounds at a high doses. Ispitivanje antidepresivnog, sedativnog i analgetskog djelovanja novih fuzioniranih derivata tiofena U radu je opisana sinteza fuzioniranih derivata benzotiofena koji sadrže heterociklički ostatak bitan za farmakološko djelovanje. Tiourea derivati 2a,b dobiveni su reakcijom derivata tetrahidrobenzo[b]tiofena 1a,b s etoksikarbonilizotiocijanatom. Iz njih su dalje priređeni anulirani derivati benzo[b]tienopirimidina 3a,b. Spojevi 2a,b i 3a su reakcijama heterociklizacije prevedeni u benzo[b]tienopirimidine 5a,b-8a-c. Ispitivano je antidepresivno, sedativno i analgetsko djelovanje novosintetiziranih derivata tiouree 2a i benzo[b]tienopirimidina 3a, 5b, 6a i 8b u dvije doze (15 ili 30 mg kg-1 tjelesne mase). Spojevi 2a, 3a i 5b pokazali su blago antidepresivno djelovanje u testu forsiranog plivanja, dok sedativni učinak nije pokazao niti jedan ispitivani spoj. Visceralna bol inducirana i.p. injekcijom octene kiseline u miševa značajno je inhibirana sa svim spojevima, ali u visokim dozama.