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, cilt.26, sa.1, ss.97-103, 2005 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 26 Sayı: 1
  • Basım Tarihi: 2005
  • Doi Numarası: 10.1016/j.ejps.2005.05.005
  • Dergi Adı: EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.97-103
  • Anahtar Kelimeler: anticonvulsant activity, 3,5-dimethylpyrazole, thiourea, urea, ANTICONVULSANT ACTIVITY, THIOUREA, SEIZURE, ANALOGS, UREAS
  • Marmara Üniversitesi Adresli: Evet

Özet

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.