Synthesis and preliminary screening of novel N-{2-[4-(substituted)piperazin-1-yl]-2-oxoethyl}acetamides as potential atypical antipsychotic agents |
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| Authors: | Kondapalli Venkata Gowri Chandra Sekhar Vajja Samabasiva Rao Mutyala Murali Krishna |
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| Institution: | 1. Chemistry Group, Birla Institute of Technology &2. Science, Pilani, Rajasthan, Indiakvgcs@bits-pilani.ac.in;4. Science, Pilani, Rajasthan, India |
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| Abstract: | A series of N-{2-4-(substituted)piperazin-1-yl]-2-oxoethyl}acetamides were synthesized as prospective novel atypical antipsychotic agents. Microwave irradiation of acetyl glycine (I) with substituted piperazines in the presence of DCC in DMF for about 3-5 min gave the titled compounds (P:1-7). All the synthesized compounds were screened for their in vivo pharmacological activity in Swiss albino mice. D2 antagonism studies were performed using the climbing mouse assay model and 5-HT2A antagonism studies were performed using quipazine induced head twitches in mice. Among the synthesized compounds P4 was found to be the most active compound. |
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| Keywords: | Schizophrenia atypical antipsychotics D2 antagonists 5-HT2A antagonists |
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