Synthesis of isothioureas derived from tetrahydroisoquinoline and NOS inhibitory activity / 药学学报
Acta Pharmaceutica Sinica
;
(12): 988-993, 2005.
Artículo
en Chino
| WPRIM
| ID: wpr-253507
ABSTRACT
<p><b>AIM</b>To get some novel potent compounds with NOS inhibitory activity, a series of new compounds of isothioureas derived from 1,2,3,4-tetrahydroisoquinoline were synthesized.</p><p><b>METHODS</b>1,2, 3,4-Tetrahydroisoquinol-2-yl was introduced into the structure of isothioureas, the NOS inhibitory activity of the new compounds synthesized were measured.</p><p><b>RESULTS AND CONCLUSION</b>Twenty-two isothiourea derivatives of [alkyl(or aryl) imino] (1,2,3,4-tetrahydroisoquinol-2-yl) methyl alkyl thioethers (I) and S-alkyl-1-phenyl-3-[4-(1,2,3,4-tetrahydroisoquinol-2-yl) methane] phenyl isothioureas (II) were synthesized from thioureas by S-alkylation with alkyl halides, and their structures were identified by IR, 1H NMR, MS and elemental analysis. The preliminary biological test showed that the part of type I (1-9 and 1-13) had higher NOS inhibitory activity than that the control aminoguanidine (AG), but the type II had weak ability to inhibit NOS.</p>
Texto completo:
Disponible
Índice:
WPRIM (Pacífico Occidental)
Asunto principal:
Farmacología
/
Estereoisomerismo
/
Tiourea
/
Estructura Molecular
/
Química
/
Óxido Nítrico Sintasa
/
Tetrahidroisoquinolinas
/
Metabolismo
Idioma:
Chino
Revista:
Acta Pharmaceutica Sinica
Año:
2005
Tipo del documento:
Artículo
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