Synthesis and biological evaluation of new N-substituted-N′-(3,5-di/1,3,5-trimethylpyrazole-4-yl)thiourea/urea derivatives
| Autor: | Eylem Korcegez, S. Rollas, Feyza Aricioglu, Bedia Koçyiğit Kaymakçıoğlu |
|---|---|
| Rok vydání: | 2005 |
| Předmět: |
Male
Electroshock Chemistry medicine.medical_treatment Thiourea Pharmaceutical Science In vitro Mice Structure-Activity Relationship chemistry.chemical_compound Maximal electroshock Anticonvulsant Pharmaceutical technology Seizures medicine Urea Animals Pentylenetetrazole Organic chemistry Anticonvulsants Female Urea derivatives Biological evaluation Nuclear chemistry |
| Zdroj: | European Journal of Pharmaceutical Sciences. 26:97-103 |
| ISSN: | 0928-0987 |
| DOI: | 10.1016/j.ejps.2005.05.005 |
| Popis: | 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 μg/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. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect