76272-53-2Relevant academic research and scientific papers
Novel 3beta-amino azabicyclooctane heteroaromatic amid derivatives preparation method and therapeutic uses thereof
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Page/Page column 11, (2010/02/11)
The invention concerns compounds of general formula 1, wherein: A, B, D and E represent one or two nitrogen atoms, the others being carbon atoms; X represents a S or, a O, thereby forming a bicyclic fused heteroaromatic, such as thieno[2,3-b]pyridine, furo[2,3-b]pyridine, thieno[3,2-b]pyridine, furo[3,2-b]pyridine, thieno[2,3-b]pyrazine, furo[2,3-b]pyrazine, thieno[2,3-c]pyridine, furo[2,3-c]pyridine, thieno[3,2-c]pyridine and furo[3,2-c]pyridine; R1 represents a linear or branched C1-C6 alkoxy group, a linear or branched C1-C6 alkylthio group; R2 represents a linear, branched, cyclic C2-C8 group, a 2- or 3- thienylmethyl group, or a benzyl group optionally substituted by one or several halogens, F, Cl, Br, I, C1-C4 alkyl, C1-C4 alkoxy, CF3, CN, NO2, OH; and their pharmaceutically acceptable salts. Said compounds are anti-dopaminergic agents.
Studies on the neuroleptic benzamides. III - Synthesis and antidopaminergic properties of new 3-nortropane derivatives
Dostert,Imbert,Langlois,et al.
, p. 105 - 110 (2007/10/02)
Various benzamides prepared from 4-alkoxy pyrimidine 5-carboxylic acids and 3-amino nortropane derivatives have been tested for their potential antipsychotic activity. Two compounds exhibited pharamacological activity equivalent to that of haloperidol but had lower toxicity and lower potency to induced catalepsy. Antidopaminergic activity is observed mainly in compounds in which the nortropane ring is substituted in the equatorial position, having a benzyl substituent on the basic nitrogen. The influence of electron attractor or donor substituents carried by the benzyl ring has been evaluated. Some aspects of structure-activity relationships are discussed.
