Phenyloxazoles and phenylthiazoles as benzamide bioisosteres: synthesis and dopamine receptor binding profiles.
Conformationally restricted benzamide bioisosteres were investigated when the aminomethylpyrrolidine derivative 4o proved D3 as well as D4 binding properties which were comparable to those of the atypical neuroleptics sulpiride and clozapine, respectively.
Einsiedel
J
J
Department of Medicinal Chemistry, Emil Fischer Center, Friedrich-Alexander University, Erlangen, Germany.
Thomas
C
C
Hübner
H
H
Gmeiner
P
P
D014150:Antipsychotic Agents / Q000138:chemical synthesis*; D001549:Benzamides / Q000138:chemical synthesis* / Q000378:metabolism; D006801:Humans; D010080:Oxazoles / Q000138:chemical synthesis* / Q000378:metabolism; D011954:Receptors, Dopamine / Q000378:metabolism*; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis* / Q000378:metabolism
D014150:Antipsychotic Agents; D001549:Benzamides; D010080:Oxazoles; D011954:Receptors, Dopamine; D013844:Thiazoles