title: Screening for antidepressant, sedative and analgesic activities of novel fused thiophene derivatives.
abstract: 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.
authors.affiliation: National Organization for Drug Control and Research, P.O. 29 Cairo, Egypt. wagnatward@hotmail.com
authors.forename: Wagnat W
authors.initials: WW
authors.lastname: Wardakhan
authors.forename: Omar M E
authors.initials: OM
authors.lastname: Abdel-Salam
authors.forename: Gamal A
authors.initials: GA
authors.lastname: Elmegeed
mesh_terms: D000700:Analgesics / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000928:Antidepressive Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D003863:Depression / Q000188:drug therapy; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D005260:Female; D006993:Hypnotics and Sedatives / Q000138:chemical synthesis* / Q000494:pharmacology; D008297:Male; D051379:Mice; D015394:Molecular Structure; D009043:Motor Activity; D010146:Pain / Q000139:chemically induced / Q000517:prevention & control; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000700:Analgesics; D000928:Antidepressive Agents; D006993:Hypnotics and Sedatives; D013876:Thiophenes