Warning: Undefined array key "mm" in /www/wwwroot/www.ai-bt.com/si.php on line 10 Deprecated: trim(): Passing null to parameter #1 ($string) of type string is deprecated in /www/wwwroot/www.ai-bt.com/si.php on line 10 Synthesis and evaluation of ligands for D2-like receptors: the role of common pharmacophoric groups.

Literature DB >> 19155177

Synthesis and evaluation of ligands for D2-like receptors: the role of common pharmacophoric groups.

Donald M N Sikazwe¹, Nancy T Nkansah, Ramazan Altundas, Xue Y Zhu, Bryan L Roth, Vincent Setola, Seth Y Ablordeppey.

Abstract

Arylcycloalkylamines, such as n class="Chemical">phenyl piperidines and piperazines and their arylalkyl substituents, constitute pharmacophoric groups exemplified in several antipsychotic agents. A review of previous reports indicates that arylalkyl substituents can improve the potency and selectivity of the binding affinity at D(2)-like receptors. In this paper, we explored the contributions of two key pharmacophoric groups, that is, 4'-fluorobutyrophenones and 3-methyl-7-azaindoles, to the potency and selectivity of synthesized agents at D(2)-like receptors. Preliminary observation of binding affinities indicates that there is little predictability of specific effects of the arylalkyl moieties but the composite structure is responsible for selectivity and potency at these receptors.

Entities: CellLine Chemical Disease Gene Species

Mesh：

Substances：

Year: 2008 PMID： 19155177 PMCID： PMC2719767 DOI： 10.1016/j.bmc.2008.12.054

Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641

27 in total

1. Design, synthesis, and evaluation of metabolism-based analogues of haloperidol incapable of forming MPP+-like species.

Authors: M Lyles-Eggleston; R Altundas; J Xia; D M N Sikazwe; P Fan; Q Yang; S Li; W Zhang; X Zhu; A W Schmidt; M Vanase-Frawley; A Shrihkande; A Villalobos; R F Borne; S Y Ablordeppey
Journal: J Med Chem Date: 2004-01-29 Impact factor: 7.446

Review 2. Role of dopamine D3 receptors in the addictive properties of ethanol.

Authors: Christian A Heidbreder; Michela Andreoli; Clara Marcon; Panayotis K Thanos; Charles R Ashby; Eliot L Gardner
Journal: Drugs Today (Barc) Date: 2004-04 Impact factor: 2.245

Review 3. Magic shotguns versus magic bullets: selectively non-selective drugs for mood disorders and schizophrenia.

Authors: Bryan L Roth; Douglas J Sheffler; Wesley K Kroeze
Journal: Nat Rev Drug Discov Date: 2004-04 Impact factor: 84.694

4. Dopamine D4 ligands and models of receptor activation: 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole and related heteroarylmethylarylpiperazines exhibit a substituent effect responsible for additional efficacy tuning.

Authors: Andrew O Stewart; Marlon D Cowart; Robert B Moreland; Steve P Latshaw; Mark A Matulenko; Pramila A Bhatia; Xueqing Wang; Jerome F Daanen; Sherry L Nelson; Marc A Terranova; Marian T Namovic; Diana L Donnelly-Roberts; Loan N Miller; Masaki Nakane; James P Sullivan; Jorge D Brioni
Journal: J Med Chem Date: 2004-04-22 Impact factor: 7.446

5. Activation of dopamine D4 receptors by ABT-724 induces penile erection in rats.

Authors: Jorge D Brioni; Robert B Moreland; Marlon Cowart; Gin C Hsieh; Andrew O Stewart; Petter Hedlund; Diana L Donnelly-Roberts; Masaki Nakane; James J Lynch; Teodozyi Kolasa; James S Polakowski; Mark A Osinski; Kennan Marsh; Karl-Erik Andersson; James P Sullivan
Journal: Proc Natl Acad Sci U S A Date: 2004-04-15 Impact factor: 11.205

6. The acute EPS of haloperidol may be unrelated to its metabolic transformation to BCPP+.

Authors: Donald M N Sikazwe; Shouming Li; Margaret Lyles-Eggleston; Seth Y Ablordeppey
Journal: Bioorg Med Chem Lett Date: 2003-11-03 Impact factor: 2.823

7. Central mechanisms regulating penile erection in conscious rats: the dopaminergic systems related to the proerectile effect of apomorphine.

Authors: Gin C Hsieh; Peter R Hollingsworth; Brenda Martino; Renjie Chang; Marc A Terranova; Alyssa B O'Neill; James J Lynch; Robert B Moreland; Diana L Donnelly-Roberts; Teodozyi Kolasa; Joseph P Mikusa; Jill M McVey; Kennan C Marsh; James P Sullivan; Jorge D Brioni
Journal: J Pharmacol Exp Ther Date: 2003-10-20 Impact factor: 4.030

8. Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.

Authors: Seth Y Ablordeppey; Ramazan Altundas; Barbara Bricker; Xue Y Zhu; Eyunni V K Suresh Kumar; Tanise Jackson; Abdul Khan; Bryan L Roth
Journal: Bioorg Med Chem Date: 2008-06-20 Impact factor: 3.641

9. The novel dopamine D4 receptor agonist (PD 168,077 maleate): doses with different effects on locomotor activity are without effect in classical conditioning.

Authors: Sahana Nayak; Helen J Cassaday
Journal: Prog Neuropsychopharmacol Biol Psychiatry Date: 2003-05 Impact factor: 5.067

10. The dopamine D4 receptor is essential for hyperactivity and impaired behavioral inhibition in a mouse model of attention deficit/hyperactivity disorder.

Authors: M E Avale; T L Falzone; D M Gelman; M J Low; D K Grandy; M Rubinstein
Journal: Mol Psychiatry Date: 2004-07 Impact factor: 15.992

6 in total

Synthesis and evaluation of ligands for D2-like receptors: the role of common pharmacophoric groups.

1. Design, synthesis, and evaluation of metabolism-based analogues of haloperidol incapable of forming MPP+-like species.

Review 2. Role of dopamine D3 receptors in the addictive properties of ethanol.

Review 3. Magic shotguns versus magic bullets: selectively non-selective drugs for mood disorders and schizophrenia.

4. Dopamine D4 ligands and models of receptor activation: 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole and related heteroarylmethylarylpiperazines exhibit a substituent effect responsible for additional efficacy tuning.

5. Activation of dopamine D4 receptors by ABT-724 induces penile erection in rats.

6. The acute EPS of haloperidol may be unrelated to its metabolic transformation to BCPP+.

7. Central mechanisms regulating penile erection in conscious rats: the dopaminergic systems related to the proerectile effect of apomorphine.

8. Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.

9. The novel dopamine D4 receptor agonist (PD 168,077 maleate): doses with different effects on locomotor activity are without effect in classical conditioning.

10. The dopamine D4 receptor is essential for hyperactivity and impaired behavioral inhibition in a mouse model of attention deficit/hyperactivity disorder.

1. Multi-receptor drug design: Haloperidol as a scaffold for the design and synthesis of atypical antipsychotic agents.

2. Enhancing a CH-π Interaction to Increase the Affinity for 5-HT1A Receptors.

3. Structure-activity relationship studies of SYA 013, a homopiperazine analog of haloperidol.

4. Identification of a new selective dopamine D4 receptor ligand.

5. Further evaluation of the tropane analogs of haloperidol.

Review 6. Mannich bases in medicinal chemistry and drug design.