title: Structure-activity relationship studies of SYA 013, a homopiperazine analog of haloperidol.
abstract: Structure-activity relationship studies on 4-(4-(4-chlorophenyl)-1,4-diazepan-1-yl)-1-(4-fluorophenyl)butan-1-one (SYA 013), a homopiperazine analog of haloperidol has resulted in an understanding of the effect of structural modifications on binding affinity at dopamine and serotonin receptor subtypes. Further exploration, using bioisosteric replacement strategies has led to the identification of several new agents including compounds 7, 8, 11 and 12 which satisfy the initial criteria for further exploration as new antipsychotic agents. In addition, compound 18, a D(3) selective tropanol, has been identified as having the potential for further optimization into a useful drug which may combat neuropsychiatric diseases.
authors.affiliation: Division of Basic Pharmaceutical Sciences, Florida A&M University, College of Pharmacy and Pharmaceutical Sciences, Tallahassee, FL 32307, USA.
authors.forename: Kwakye
authors.initials: K
authors.lastname: Peprah
authors.forename: Xue Y
authors.initials: XY
authors.lastname: Zhu
authors.forename: Suresh V K
authors.initials: SV
authors.lastname: Eyunni
authors.forename: Jagan R
authors.initials: JR
authors.lastname: Etukala
authors.forename: Vincent
authors.initials: V
authors.lastname: Setola
authors.forename: Bryan L
authors.initials: BL
authors.lastname: Roth
authors.forename: Seth Y
authors.initials: SY
authors.lastname: Ablordeppey
mesh_terms: D014150:Antipsychotic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001381:Azepines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006220:Haloperidol / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: C576224:4-(4-(4-chlorophenyl)-1,4-diazepan-1-yl)-1-(4-fluorophenyl)butan-1-one; D014150:Antipsychotic Agents; D001381:Azepines; D006220:Haloperidol