22126-67-6Relevant articles and documents
Synthesis and antidepressant properties of novel 2-substituted 4,5-dihydro-1H-imidazole derivatives
Wentland,Bailey,Alexander,Castaldi,Ferrari,Haubrich,Luttinger,Perrone
, p. 1482 - 1489 (1987)
A unique combination of α2-adrenoreceptor antagonist and serotonin-selective reuptake inhibitory activities has been identified in a series of 2-substituted 4,5-dihydro-1H-imidazole derivatives. This combination of blocking activities has provided one of these derivatives, napamezole hydrochloride (2), with potential as an antidepressant. A discussion of the syntheses of these compounds includes a convenient method for the conversion of nitriles to imidazolines with ethylenediamine and trimethylaluminum.
Benzylamidine derivatives with serotonin receptor binding activity
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, (2008/06/13)
This invention relates to compounds having serotonin receptor binding activity, to pharmaceutical compositions containing them and to their medical use, particularly in the treatment of CNS conditions. Described herein are compounds which have the general formula: STR1 wherein R 1 is selected from a group of Formula i and ii: STR2 n is 1-3; R 2 is selected from H and C 1-6 alkyl;R 3 is selected from H and C 1-6 alkyl;R 4 is selected from C 1-6 alkyl, halo, phenyl, amino and nitro;R 5 is selected from H, C 1-6 alkyl and arylalkyl;R 6 is selected from H or a alkylene group which is bonded to R 4 to form the naphthalene ring skeleton; and salts, hydrates and solvates thereof.Also described is the use of these compounds as pharmaceuticals to treat indications where stimulation of subtypes of the serotonin receptor is implicated, such as migraine.