Discovery of non-peptidergic MrgX1 and MrgX2 receptor agonists and exploration of an initial SAR using solid-phase synthesis
Malik, Leila ; Kelly, Nicholas M. ; Ma, Jian Nong ; Currier, Erika A. ; Burstein, Ethan S. and Olsson, Roger LU
(2009)
In Bioorganic and Medicinal Chemistry Letters
19(6).
p.1729-1732
- Abstract
A class of small molecules displaying comparable activities with peptide ligands BAM22 and corticostatin-14 at both the human and rhesus monkey MrgX1 and MrgX2 receptors, respectively, was discovered. A comparative study to compare solid-phase and solution-phase chemistries for the efficient synthesis of the active class, tetracyclic benzimidazoles, was undertaken. The solid-phase chemistry was found to be superior both for the synthesis of analogs and for the synthesis of gram quantities.
Please use this url to cite or link to this publication:
https://lup.lub.lu.se/record/71266977-5302-4550-93e5-725fc21272bc
- author
- Malik, Leila
; Kelly, Nicholas M.
; Ma, Jian Nong
; Currier, Erika A.
; Burstein, Ethan S.
and Olsson, Roger
LU
- publishing date
- 2009-03-15
- type
- Contribution to journal
- publication status
- published
- keywords
- Agonist, Mas related, MrgX1, MrgX2, Nociception, Non-peptidergic, R-SAT, Sensory-neuron specific receptors, Small molecule, SNSR, Solid-phase
- in
- Bioorganic and Medicinal Chemistry Letters
- volume
- 19
- issue
- 6
- pages
- 4 pages
- publisher
- Elsevier
- external identifiers
-
- scopus:61349141397
- pmid:19230660
- ISSN
- 0960-894X
- DOI
- 10.1016/j.bmcl.2009.01.085
- language
- English
- LU publication?
- no
- id
- 71266977-5302-4550-93e5-725fc21272bc
- date added to LUP
- 2019-10-02 10:01:16
- date last changed
- 2024-01-01 21:24:22
@article{71266977-5302-4550-93e5-725fc21272bc,
abstract = {{<p>A class of small molecules displaying comparable activities with peptide ligands BAM22 and corticostatin-14 at both the human and rhesus monkey MrgX1 and MrgX2 receptors, respectively, was discovered. A comparative study to compare solid-phase and solution-phase chemistries for the efficient synthesis of the active class, tetracyclic benzimidazoles, was undertaken. The solid-phase chemistry was found to be superior both for the synthesis of analogs and for the synthesis of gram quantities.</p>}},
author = {{Malik, Leila and Kelly, Nicholas M. and Ma, Jian Nong and Currier, Erika A. and Burstein, Ethan S. and Olsson, Roger}},
issn = {{0960-894X}},
keywords = {{Agonist; Mas related; MrgX1; MrgX2; Nociception; Non-peptidergic; R-SAT; Sensory-neuron specific receptors; Small molecule; SNSR; Solid-phase}},
language = {{eng}},
month = {{03}},
number = {{6}},
pages = {{1729--1732}},
publisher = {{Elsevier}},
series = {{Bioorganic and Medicinal Chemistry Letters}},
title = {{Discovery of non-peptidergic MrgX1 and MrgX2 receptor agonists and exploration of an initial SAR using solid-phase synthesis}},
url = {{http://dx.doi.org/10.1016/j.bmcl.2009.01.085}},
doi = {{10.1016/j.bmcl.2009.01.085}},
volume = {{19}},
year = {{2009}},
}