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Relevant academic research and scientific papers

Design, synthesis and antimalarial evaluation of novel thiazole derivatives

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.

NEUROPEPTIDE Y4 RECEPTOR AGONISTS

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.

SELECTIVE NEUROPEPTIDE Y2 RECEPTOR AGONISTS

This invention provides peptides that act as selective NPY2 receptor agonists and may be used to reduce food intake. The invention includes a peptide selected from a specific group of derivatized NPY-related peptides, or functional equivalents thereof. The invention is also directed to a method of treating obesity or related diseases in a mammal comprising administering a therapeutically effective amount of the peptide to said mammal to reduce food intake and body weight.

PITUITARY ADENYLATE CYCLASE ACTIVATING PEPTIDE (PACAP) RECEPTOR (VPAC2) AGONISTS AND THEIR PHARMACOLOGICAL METHODS OF USE

This invention provides peptides with novel modifications that provide suitable derivatization sites to improve the pharmacokinetic properties of the peptides. These modified peptides function in vivo as agonists of the VPAC2 receptor. The peptides of the present invention provide a new therapy for patients with decreased endogenous insulin secretion, for example, type 2 diabetics.

GLUCAGON-LIKE PEPTIDE 1 (GLP-1) RECEPTOR AGONISTS AND THEIR PHARMACOLOGICAL METHODS OF USE

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.

GLUCOSE-DEPENDENT INSULINOTROPIC POLYPEPTIDE (GIP) RECEPTOR AGONISTS AND THEIR PHARMACOLOGICAL METHODS OF USE

This invention provides peptides with novel modifications that provide suitable derivatization sites to improve the pharmacokinetic properties of the peptides. These modified peptides function in vivo as agonists of the GIP receptor. The peptides of the present invention provide a new therapy for patients with decreased endogenous insulin secretion, for example, type 2 diabetics.

The Preparation of Thiazole-4- and -5-carboxylates, and an Infrared Study of their Rotational Isomers

Convenient general procedures have been developed for preparing series of thiazole-4- and -5-carboxylates containing alkyl and halogeno substituents.While both series of esters show i.r. carbonyl doublets caused by rotational isomerism, the more intense absorptions of the 4-carboxylates are the lower wavenumber components, whereas those of the 5-carboxylates are the higher wavenumber components.In both series the stronger bands arise from the thermochemically more stable forms; identification of these forms as the carbonyl O,S-syn-s-trans rotamers is more certain with the 4-carboxylates than with the 5-carboxylates.