Amides Derived From Hepta- and Octamethyleneimine

Antidepressive Effect of N-3,4,5-Trimethoxybenzoyl Heptamethylenimine

“…The sensitivity, accuracy, precision, and manipulative simplicity of the ferro-citrate color reaction described by Doty (1) have led to its wide use for assay of preparations containing isoproterenol, epinephrine, and other catecholamine drugs. The reaction is selective for the catechol function, and it will therefore be stability indicating where the degradation reaction involves the catechol group.…”

“…Monoamino oxidase has not been inhibited either in vitro or in oivo after premeditation for 1 week The compound has shown no noteworthy harmful effect in subacute toxicity tests. Upon due consideration of the obtained findirlgs, the compound would seem to display an extraordinary likeness in pharmacological properties to tricyclic antidepressants, and as such it may be denoted as a potential antidepressive drug of new chemical type.…”

“…In view of the absence of solution interaction between DCA and reserpine in ethyl acetate, and the lack of change in crystal form, it is concluded that the physical state of reserpine (i.e., an extremely fine particle size attained by co-precipitation with DCA) is responsible for the increased dissolution rates observed with the reserpine-DCA dispersions. As stated by these authors, un-like other amines containing trimethoxybenzoyl group the compodnd is void of depressant and analgesic action; moreover, it exerts a mild stimulating effect.In a series of studies concerned with a large number of derivatives of heptamethylenimine substituted by benzoic acid the above-mentioned compound has also been synthesized and subjected to close pharmacological investigation.Synthesis was carried out principally by the method reported by Luts et al (1). 2-Second-order plot of reserpine dissolution data assuming dissolution was apparent jirst order under nonsink conditions.…”

“…and for various It was Luts et al (1) who reported on the synthesis and preliminary pharmacological investigation of N-3,4,5-trimethoxybenzoyl heptamethylenimine. However, as noted by Levy (8) dissolution in organic solvents does reflect adequately the particle size of the drug.…”

Structure-Activity Studies of New Potential Depressants 3,4,5-TrimethoxybenzamidesI II

“…Keyphrases 0 p-Toluidines, 5-nitrothiazole-synthesis, potentid schistosomicidal agents Schistosomicidal agents, potentialsynthesis of condensed p-toluidines, aminothiazoles Investigations carried out since the discovery of the schistosomicidal activity of 1-(B-diethylaminoethylamino)-4-methylthiaxanthone1 (I) and its analogs showed that the presence of an amino side chain located on C-1 in para-position to the methyl group on C-4 is necessary for the biological activity of these agents (1,2). In the recent schistosomicidal agent, l-(5-nitro-2-thiazoly1)-2-imidazolidin~ne~ (11), the presence of the nitrothiazole group was confirmed to be an essential feature for its activity (3,4).…”