This article is cited in 12 papers

Communications

Synthesis and antihypotensive properties of 2-amino-2-thiazoline analogues with enhanced lipophilicity

E. V. Nurieva^a, T. P. Trofimova^ab, A. A. Alexeev^a, A. N. Proshin^c, E. A. Chesnakova^d, Yu. K. Grishin^a, K. A. Lyssenko^e, M. V. Filimonova^d, S. O. Bachurin^c, O. N. Zefirova<sup>ac

a</sup> Department of Chemistry, M.V. Lomonosov Moscow State University, Moscow, Russian Federation
^b Dmitry Rogachev National Medical Research Center of Pediatric Hematology, Oncology and Immunology, Moscow, Russian Federation
^c Institute of Physiologically Active Compounds, Federal Research Center of Problems of Chemical Physics and Medicinal Chemistry, Russian Academy of Sciences, Chernogolovka, Moscow Region, Russian Federation
^d Medical Radiology Research Center, Russian Academy of Medical Sciences, Obninsk, Kaluga Region, Russian Federation
^e A.N. Nesmeyanov Institute of Organoelement Compounds of Russian Academy of Sciences, 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.

Language: English

DOI: 10.1016/j.mencom.2018.07.016

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