Synthesis and antihypotensive properties of 2-amino-2-thiazoline analogues with enhanced lipophilicity |
| |
| Authors: | Evgeniya V Nurieva Tatyana P Trofimova Alexander A Alexeev Alexey N Proshin Ekaterina A Chesnakova Yuri K Grishin Konstantin A Lyssenko Marina V Filimonova Sergey O Bachurin Olga N Zefirova |
| |
| Institution: | 1. Department of Chemistry, M. V. Lomonosov Moscow State University, 119991 Moscow, Russian Federation;2. D. Rogachev National Research Center of Pediatric Hematology, Oncology and Immunology, 117997 Moscow, Russian Federation;3. Institute of Physiologically Active Compounds, Russian Academy of Sciences, 142432 Chernogolovka, Moscow Region, Russian Federation;4. Medical Radiology Research Center, Russian Academy of Medical Sciences, 249036 Obninsk, Kaluga Region, Russian Federation;5. A. N. Nesmeyanov Institute of Organoelement Compounds, Russian Academy of Sciences, 119991 Moscow, Russian Federation |
| |
| Abstract: | In a search of nitric oxide synthase inhibitors with prolonged vasoconstrictive activity, a series of lipophilic cyclohexafused 2-amino-2-thiazolines was obtained via cyclization of tert-butyl- or benzoyl-substituted N-(cyclohex-2-en-1-yl)thioureas. The crystal structure of intermediate N-(3aRS,7aSR)- 3a,4,5,6,7,7a-hexahydro-1,3-benzothiazol-2-yl]benzamide hydrobromide was determined by X-ray analysis. One compound was found to cause pronounced and prolonged vasoconstrictive effect after single injection to the Wystar rats with lipopolysaccharide induced acute endotoxic (vasodilatation) shock. |
| |
| Keywords: | Corresponding author |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
