Acta Pharm. 58 (2008) 1-14
Original research paper
Screening for antidepressant, sedative and analgesic activities of novel
fused thiophene derivatives
WAGNAT W. WARDAKHAN, OMAR M. E. ABDEL-SALAM and
GAMAL A. ELMEGEED
wagnatward@hotmail.com
National Organization for Drug Control &
Research, P.O. 29,
Pharmacology Department, Hormone
Department, National Research Centre, Dokki,
Accepted February 1, 2008
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.
Keywords: tetrahydrobenzo[b]thiophene, pyrimidine, thiourea, antidepressant,
sedative, analgesic