Synthesis of isothioureas derived from tetrahydroisoquinoline and NOS inhibitory activity / 药学学报
Acta Pharmaceutica Sinica
;
(12): 988-993, 2005.
Article
in Chinese
| 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>
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Pharmacology
/
Stereoisomerism
/
Thiourea
/
Molecular Structure
/
Chemistry
/
Nitric Oxide Synthase
/
Tetrahydroisoquinolines
/
Metabolism
Language:
Chinese
Journal:
Acta Pharmaceutica Sinica
Year:
2005
Type:
Article
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