Synthesis and biological evaluation of new N-substituted-N '-(3,5-di/1,3,5-trimethylpyrazole-4-yl)thiourea/urea derivatives


Kaymakcioglu B. , Rollas S., Korcegez E., Aricioglu F.

EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, vol.26, no.1, pp.97-103, 2005 (Journal Indexed in SCI) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 26 Issue: 1
  • Publication Date: 2005
  • Doi Number: 10.1016/j.ejps.2005.05.005
  • Title of Journal : EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
  • Page Numbers: pp.97-103

Abstract

Several thiourea and urea derivatives were prepared by the reaction of 4-aminopyrazoles with substituted isothiocyanates or isocyanates. The novel compounds were tested anticonvulsant activity using by pentylenetetrazole-induced seizure (PTZ) and maximal electroshock seizure (MES) tests. Among the tested compounds, thiourea derivatives of 4b were afforded 90 and 100% protection in PTZ and MES tests at 50 mg/kg, respectively. Urea derivatives of 5a and 5b were afforded 82 and 100% protection both at 25 and 50 mg/kg. Also synthesized compounds were screened for antituberculosis activity against Mycobacterium tuberculosis H(37)Rv at 6.25 mu g/mL concentration but they were not found active at these concentration. In addition, some selected compounds were evaluated for in vitro anti-HIV activity and they were all negative. (c) 2005 Elsevier B.V. All rights reserved.