77505-83-0Relevant articles and documents
Design, synthesis and antimalarial evaluation of novel thiazole derivatives
Bueno, José María,Carda, Miguel,Crespo, Benigno,Cu?at, Ana Carmen,de Cozar, Cristina,León, María Luisa,Marco, J. Alberto,Roda, Nuria,Sanz-Cervera, Juan F.
supporting information, p. 3938 - 3944 (2016/08/01)
As part of our medicinal chemistry program's ongoing search for compounds with antimalarial activity, we prepared a series of thiazole analogs and conducted a SAR study analyzing their in vitro activities against the chloroquine-sensitive Plasmodium falciparum 3D7 strain. The results indicate that modifications of the N-aryl amide group linked to the thiazole ring are the most significant in terms of in vitro antimalarial activity, leading to compounds with high antimalarial potency and low cytotoxicity in HepG2 cell lines. Furthermore, the observed SAR implies that non-bulky, electron-withdrawing groups are preferred at ortho position on the phenyl ring, whereas small atoms such as H or F are preferred at para position. Finally, replacement of the phenyl ring by a pyridine affords a compound with similar potency, but with potentially better physicochemical properties which could constitute a new line of research for further studies.
GLUCAGON-LIKE PEPTIDE 1 (GLP-1) RECEPTOR AGONISTS AND THEIR PHARMACOLOGICAL METHODS OF USE
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, (2010/11/24)
This invention provides peptides with novel modifications that provide suitable derivatization sites to improve the pharmacokinetic properties of the peptides. These GLP-1 modified peptides function in vivo as agonists of the GLP-1 receptor. The peptides of the present invention provide a new therapy for patients with decreased endogenous insulin secretion, for example, type 2 diabetics.
NEUROPEPTIDE Y4 RECEPTOR AGONISTS
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Page/Page column 54, (2008/06/13)
This invention provides peptides that act as selective NPY4 receptor agonists in vitro and are efficacious in vivo to reduce food intake. The invention is a peptide selected from a specific group of derivatized PP-related peptides, or functional equivalents thereof. The invention is also directed to a method of treating a metabolic disease in a mammal comprising administering a therapeutically effective amount of the peptides to said mammal to reduce food intake and body weight.