title: Synthesis and preliminary screening of novel N-{2-[4-(substituted)piperazin-1-yl]-2-oxoethyl}acetamides as potential atypical antipsychotic agents.
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. 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.
authors.affiliation: Chemistry Group, Birla Institute of Technology & Science, Pilani, Rajasthan, India. kvgcs@bits-pilani.ac.in
authors.forename: Kondapalli Venkata Gowri
authors.initials: KV
authors.lastname: Chandra Sekhar
authors.forename: Vajja Samabasiva
authors.initials: VS
authors.lastname: Rao
authors.forename: Mutyala Murali
authors.initials: MM
authors.lastname: Krishna
mesh_terms: 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
chemical_list: 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