Abstract
Original language | English |
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Pages (from-to) | 928 - 933 |
Number of pages | 6 |
Journal | Australian Journal of Chemistry |
Volume | 60 |
Issue number | 12 |
DOIs | |
Publication status | Published - 2007 |
Cite this
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Synthesis and preliminary pharmacological evaluation of 4'-arylalkyl analogues of clozapine. III. Replacement of the tricyclic nucleus with a bicyclic template. / Capuano, Benny; Crosby, Ian Travers; Lloyd, Edward John; Taylor, David.
In: Australian Journal of Chemistry, Vol. 60, No. 12, 2007, p. 928 - 933.Research output: Contribution to journal › Article › Research › peer-review
TY - JOUR
T1 - Synthesis and preliminary pharmacological evaluation of 4'-arylalkyl analogues of clozapine. III. Replacement of the tricyclic nucleus with a bicyclic template
AU - Capuano, Benny
AU - Crosby, Ian Travers
AU - Lloyd, Edward John
AU - Taylor, David
PY - 2007
Y1 - 2007
N2 - As a continuing part of our research program in search of novel compounds for the treatment of schizophrenia, we report the synthesis and preliminary receptor binding affinity for a series of bicyclic analogues of clozapine derived from a selection of promising tricyclic candidates published previously. These bicyclic compounds investigate some substituent effects and the length and nature of the linker between an ionizable nitrogen atom at physiological pH and the introduced aryl moiety. The chemistry, structural characterization, and in vitro evaluation are described. Preliminary findings on the effects on activity of the nature and length of the linker, degree of unsaturation, and selected substituents coupled to the bicyclic nucleus are discussed in relation to affinity for dopamine D-4 and serotonin 5-HT2A receptors.
AB - As a continuing part of our research program in search of novel compounds for the treatment of schizophrenia, we report the synthesis and preliminary receptor binding affinity for a series of bicyclic analogues of clozapine derived from a selection of promising tricyclic candidates published previously. These bicyclic compounds investigate some substituent effects and the length and nature of the linker between an ionizable nitrogen atom at physiological pH and the introduced aryl moiety. The chemistry, structural characterization, and in vitro evaluation are described. Preliminary findings on the effects on activity of the nature and length of the linker, degree of unsaturation, and selected substituents coupled to the bicyclic nucleus are discussed in relation to affinity for dopamine D-4 and serotonin 5-HT2A receptors.
UR - http://www.scopus.com/record/display.url?eid=2-s2.0-36749034902&origin=inward&txGid=LJA3atyckHuknbWEZfJcUA1%3a16
U2 - 10.1071/CH07201
DO - 10.1071/CH07201
M3 - Article
VL - 60
SP - 928
EP - 933
JO - Australian Journal of Chemistry
JF - Australian Journal of Chemistry
SN - 0004-9425
IS - 12
ER -