Search: onr:"swepub:oai:DiVA.org:uu-225073" >
N-Aryl Isoleucine D...
N-Aryl Isoleucine Derivatives as Angiotensin II AT(2) Receptor Ligands
-
- Behrends, Malte (author)
- Uppsala universitet,Avdelningen för organisk farmaceutisk kemi
-
- Wallinder, Charlotta (author)
- Uppsala universitet,Avdelningen för organisk farmaceutisk kemi
-
- Wieckowska, Anna (author)
- Uppsala universitet,Avdelningen för organisk farmaceutisk kemi
-
show more...
-
Guimond, Marie-Odile (author)
-
- Hallberg, Anders (author)
- Uppsala universitet,Avdelningen för organisk farmaceutisk kemi
-
Gallo-Payet, Nicole (author)
-
- Larhed, Mats (author)
- Uppsala universitet,Avdelningen för organisk farmaceutisk kemi
-
show less...
-
(creator_code:org_t)
- 2014-03-13
- 2014
- English.
-
In: ChemistryOpen. - : Wiley. - 2191-1363. ; 3:2, s. 65-75
- Related links:
-
https://uu.diva-port... (primary) (Raw object)
-
show more...
-
https://doi.org/10.1...
-
https://urn.kb.se/re...
-
https://doi.org/10.1...
-
show less...
Abstract
Subject headings
Close
- A novel series of ligands for the recombinant human AT(2) receptor has been synthesized utilizing a fast and efficient palladium-catalyzed procedure for aminocarbonylation as the key reaction. Molybdenum hexacarbonyl [Mo(CO)(6)] was employed as the carbon monoxide source, and controlled microwave heating was applied. The prepared N-aryl isoleucine derivatives, encompassing a variety of amide groups attached to the aromatic system, exhibit binding affinities at best with K-i values in the low micromolar range versus the recombinant human AT(2) receptor. Some of the new nonpeptidic isoleucine derivatives may serve as starting points for further structural optimization. The presented data emphasize the importance of using human receptors in drug discovery programs.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Läkemedelskemi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Medicinal Chemistry (hsv//eng)
Keyword
- aminocarbonylation
- AT(2) receptor
- medicinal chemistry
- palladium catalysis
- peptide mimics
Publication and Content Type
- ref (subject category)
- art (subject category)
Find in a library
To the university's database