Synthesis and preliminary screening of novel N-{2-[4-(substituted)piperazin-1-yl]-2-oxoethyl}acetamides as potential atypical antipsychotic agents.
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. D(2) antagonism studies were performed using the climbing mouse assay model and 5-HT(2A) antagonism studies were performed using quipazine induced head twitches in mice. Among the synthesized compounds P4 was found to be the most active compound.
Chandra Sekhar
Kondapalli Venkata Gowri
KV
Chemistry Group, Birla Institute of Technology & Science, Pilani, Rajasthan, India. kvgcs@bits-pilani.ac.in
Rao
Vajja Samabasiva
VS
Krishna
Mutyala Murali
MM
D000081:Acetamides / Q000737:chemistry* / Q000494:pharmacology*; D000818:Animals; D014150:Antipsychotic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D065127:Dopamine D2 Receptor Antagonists; D004353:Drug Evaluation, Preclinical; D005260:Female; D019416:Head Movements / Q000187:drug effects; D008297:Male; D051379:Mice; D008872:Microwaves; D010879:Piperazines / Q000737:chemistry* / Q000494:pharmacology*; D011814:Quipazine / Q000494:pharmacology; D051381:Rats; D044405:Receptor, Serotonin, 5-HT2C / Q000378:metabolism; D017448:Receptors, Dopamine D2 / Q000378:metabolism; D058830:Serotonin 5-HT2 Receptor Antagonists
D000081:Acetamides; D014150:Antipsychotic Agents; D065127:Dopamine D2 Receptor Antagonists; D010879:Piperazines; D044405:Receptor, Serotonin, 5-HT2C; D017448:Receptors, Dopamine D2; D058830:Serotonin 5-HT2 Receptor Antagonists; D011814:Quipazine