Novel l-prolyl-l-leucylglycinamide (PLG) tripeptidomimetics based on a 2-azanorbornane scaffold as positive allosteric modulators of the D2R-Reference-Cited by-同舟云学术

Novel l-prolyl-l-leucylglycinamide (PLG) tripeptidomimetics based on a 2-azanorbornane scaffold as positive allosteric modulators of the D2R

Published:2016 Issue:47 Volume:14 Page:11065-11069
ISSN:1477-0520
Container-title:Organic & Biomolecular Chemistry
language:en
Short-container-title:Org. Biomol. Chem.

Author:

Sampaio-Dias Ivo E.¹²³⁴⁵^ORCID,Sousa Carlos A. D.⁶²³⁴⁵^ORCID,García-Mera Xerardo⁷⁸⁹¹⁰¹¹,Ferreira da Costa Joana¹²¹³¹⁴¹⁵,Caamaño Olga⁷⁸⁹¹⁰¹¹,Rodríguez-Borges José E.¹²³⁴⁵

Affiliation:

1. UCIBIO/REQUIMTE

2. Department of Chemistry and Biochemistry

3. Faculty of Sciences

4. University of Porto

5. 4169-007 Porto

6. LAQV/REQUIMTE

7. Department of Organic Chemistry

8. Faculty of Pharmacy

9. University of Santiago de Compostela

10. E-15782 Santiago de Compostela

11. Spain

12. Instituto de Química

13. Universidade Federal da Bahia

14. Salvador-BA

15. 40170-290 Brazil

Abstract

Replacement of l-prolyl residue in the PLG sequence by an enantiopure (1R,3S,4S)-2-azanorbornane scaffold afforded active peptidomimetics compatible with suppression of the C-terminal carboxamide pharmacophore.

Funder

Fundação para a Ciência e a Tecnologia

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Physical and Theoretical Chemistry,Biochemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2016/OB/C6OB02248K

Reference21 articles.

1. Synthesis and allosteric modulation of the dopamine receptor by peptide analogs of l-prolyl-l-leucyl-glycinamide (PLG) modified in the l-proline or l-proline and l-leucine scaffolds

2. Solid state conformation of the C-terminal tripeptide of oxytocin, L-Pro-L-Leu-Gly-NH2.0.5H2O

3. Design and Synthesis of Photoaffinity-Labeling Ligands of the l-Prolyl-l-leucylglycinamide Binding Site Involved in the Allosteric Modulation of the Dopamine Receptor

4. Synthesis and evaluation of novel pyridine based PLG tripeptidomimetics

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