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Bioorg Med Chem Lett ; 18(23): 6054-7, 2008 12 01.
Article in English | MEDLINE | ID: mdl-18948000

ABSTRACT

A series of N-2-(4-(4-(2-substitutedthiazol-4-yl) piperazin-1-yl)-2-oxoethyl)acetamides were synthesized in an effort to prepare novel atypical antipsychotic agents. The compounds were synthesized by either microwave irradiation technique or by conventional synthesis and were characterized by spectral data (IR, (1)H NMR, and MS) and the purity was ascertained by microanalysis. All the synthesized compounds were screened for their in vivo pharmacological activity in Swiss albino mice. D(2) antagonism studies were performed using climbing mouse assay model and 5-HT(2A) antagonism studies were performed using quipazine induced head twitches in mice. It was observed that none of the new chemical entities exhibited catalepsy. AG 3 was found to be the most active compound.


Subject(s)
Acetamides/chemical synthesis , Acetamides/pharmacology , Antipsychotic Agents/chemical synthesis , Antipsychotic Agents/pharmacology , Piperazines/chemical synthesis , Piperazines/pharmacology , Serotonin 5-HT2 Receptor Antagonists , Acetamides/chemistry , Animals , Antipsychotic Agents/chemistry , Combinatorial Chemistry Techniques , Disease Models, Animal , Head Movements/drug effects , Mice , Molecular Structure , Motor Activity/drug effects , Piperazines/isolation & purification , Quipazine/pharmacology
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