| Synthesis and evaluation of novel phenylethanolamine derivatives containing acetanilides as potent and selective beta3-adrenergic receptor agonists. | |
| | |
MedLine Citation:
|
PMID: 20410638 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
|
In the search for potent and selective human beta3-adrenergic receptor (AR) agonists as potential pharmacotherapies for the treatment of obesity and non-insulin dependent (type II) diabetes, we prepared a novel series of phenylethanolamine derivatives containing acetanilides and evaluated their biological activities at the human beta3-, beta2-, and beta1-ARs. Among these compounds, the 6-amino-2-pyridylacetanilide (36b), 2-amino-5-methylthiazol-4-ylacetanilide (36g), and 5-amino-1,2,4-thiadiazol-3-ylacetanilide (36h) derivatives showed potent agonistic activity at the beta3-AR with functional selectivity over the beta1- and beta2-ARs. In addition, these compounds exhibited significant hypoglycemic activity in a rodent diabetic model. |
| | |
Authors:
|
Tatsuya Maruyama; Kenichi Onda; Masahiko Hayakawa; Takayuki Suzuki; Tetsuya Kimizuka; Tetsuo Matsui; Toshiyuki Takasu; Itsuro Nagase; Noritaka Hamada; Mitsuaki Ohta |
Related Documents
:
|
3526358 - Insulin-potentiating action of gliclazide (diamicron). 6345588 - Defect in cooperativity in insulin receptors from a patient with a congenital form of e... 20814548 - Insulin-induced electrophysiology changes in human pleura are mediated via its receptor. 2157428 - Insulin-receptor autophosphorylation and kinase activity are constitutively increased i... 3315448 - Guanfacine in the treatment of hypertensives with a pronounced response to exercise and... 10714358 - Insulin resistance and type 2 diabetes mellitus: its relationship with the beta 3-adren... |
Publication Detail:
|
Type: Journal Article |
Journal Detail:
|
Title: Chemical & pharmaceutical bulletin Volume: 58 ISSN: 1347-5223 ISO Abbreviation: Chem. Pharm. Bull. Publication Date: 2010 Apr |
Date Detail:
|
Created Date: 2010-04-22 Completed Date: 2010-07-27 Revised Date: 2011-03-08 |
Medline Journal Info:
|
Nlm Unique ID: 0377775 Medline TA: Chem Pharm Bull (Tokyo) Country: Japan |
Other Details:
|
Languages: eng Pagination: 533-45 Citation Subset: IM |
Affiliation:
|
Drug Discovery Research, Astellas Pharma Inc, Tsukuba, Ibaraki, Japan. tatsuya.maruyama@jp.astellas.com |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
|
Adrenergic Agonists
/
chemical synthesis,
chemistry*,
pharmacology,
therapeutic use* Adrenergic beta-3 Receptor Agonists* Animals Blood Glucose / drug effects Humans Hypoglycemic Agents / chemical synthesis, chemistry*, pharmacology, therapeutic use* Male Mice Models, Molecular Molecular Conformation Phenethylamines / chemical synthesis, chemistry*, pharmacology, therapeutic use* Receptors, Adrenergic, beta-1 / metabolism Receptors, Adrenergic, beta-2 / metabolism Receptors, Adrenergic, beta-3 / metabolism |
| Chemical | |
Reg. No./Substance:
|
0/Adrenergic Agonists; 0/Adrenergic beta-3 Receptor Agonists; 0/Blood Glucose; 0/Hypoglycemic Agents; 0/Phenethylamines; 0/Receptors, Adrenergic, beta-1; 0/Receptors, Adrenergic, beta-2; 0/Receptors, Adrenergic, beta-3 |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
Previous Document: Sulphonamides as inhibitors of protein tyrosine phosphatase 1B: a three-dimensional quantitative str...
Next Document: Two new coumarins from the chloroform extract of Angelica urumiensis from Iran.