title: Disubstituted thiourea derivatives and their activity on CNS: synthesis and biological evaluation.
abstract: A series of new thiourea derivatives of 1,2,4-triazole have been synthesized. The difference in structures of obtained compounds are directly connected with the kind of isothiocyanate (aryl/alkyl). The (1)H NMR, (13)C NMR, MS methods were used to confirm structures of obtained thiourea derivatives. The molecular structure of (1, 17) was determined by an X-ray analysis. Two of the new compounds (8 and 14) were tested for their pharmacological activity on animal central nervous system (CNS) in behavioural animal tests. The results presented in this work indicate the possible involvement of the serotonergic system in the activity of 8 and 14. In the case of 14 is also a possible link between its activity and the endogenous opioid system. All obtained compounds were tested for antibacterial activity against gram-positive cocci, gram-negative rods and antifungal activity. Compounds (1, 2, 5, 7, 9) showed significant inhibition against gram-positive cocci. Microbiological evaluation was carried out over 20 standard strains and 30 hospital strains. Selected compounds (1-13) were examined for cytotoxicity, antitumor, and anti-HIV activity.
authors.affiliation: Department of Pharmaceutical Microbiology, Medical University, 02-007 Warsaw, Poland.
authors.forename: Joanna
authors.initials: J
authors.lastname: Stefanska
authors.forename: Daniel
authors.initials: D
authors.lastname: Szulczyk
authors.forename: Anna E
authors.initials: AE
authors.lastname: Koziol
authors.forename: Barbara
authors.initials: B
authors.lastname: Miroslaw
authors.forename: Ewa
authors.initials: E
authors.lastname: Kedzierska
authors.forename: Sylwia
authors.initials: S
authors.lastname: Fidecka
authors.forename: Bernardetta
authors.initials: B
authors.lastname: Busonera
authors.forename: Giuseppina
authors.initials: G
authors.lastname: Sanna
authors.forename: Gabriele
authors.initials: G
authors.lastname: Giliberti
authors.forename: Paolo
authors.initials: P
authors.lastname: La Colla
authors.forename: Marta
authors.initials: M
authors.lastname: Struga
mesh_terms: D000818:Animals; D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000890:Anti-Infective Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects; D001522:Behavior, Animal / Q000187:drug effects; D045744:Cell Line, Tumor; D002490:Central Nervous System / Q000187:drug effects* / Q000502:physiology; D060326:Chemistry Techniques, Synthetic; D015195:Drug Design; D005658:Fungi / Q000187:drug effects; D006801:Humans; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D013890:Thiourea / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D019380:Anti-HIV Agents; D000890:Anti-Infective Agents; D013890:Thiourea