Abstract
We report that increases in insulin secretion induced by OEA were associated with increased cAMP and a potentiation of glucose-stimulated increases in [Ca(2+)](i). We also demonstrate that ATP-sensitive K(+) and voltage-dependent calcium channels were required for GPR119-mediated increases in glucos...
|
PMID: 18724386
PDF is available here.
Tawfik T Gharbaoui,
Philip J PJ Skinner,
Young-Jun YJ Shin,
Claudia C Averbuj,
Jae-Kyu JK Jung,
Benjamin R BR Johnson,
Tracy T Duong,
Marc M Decaire,
Jane J Uy,
Martin C MC Cherrier,
Peter J PJ Webb,
Susan Y SY Tamura,
Ning N Zou,
Nathalie N Rodriguez,
P Douglas PD Boatman,
Carleton R CR Sage,
Andrew A Lindstrom,
Jerry J Xu,
Thomas O TO Schrader,
Brian M BM Smith,
Ruoping R Chen,
Jeremy G JG Richman,
Daniel T DT Connolly,
Steven L SL Colletti,
James R JR Tata and
Graeme G Semple
Abstract
A strategy for lead identification of new agonists of GPR109a, starting from known compounds shown to activate the receptor, is described. Early compound triage led to the formulation of a binding hypothesis and eventually to our focus on a series of pyrazole acid derivatives. Further elaboration of...
|
PMID: 17588745
PDF is available here.
Abstract
Depending on the single rate constants and on the geometry of the system, lipid bilayer permeation may positively, negatively or not correlate with the bilayer affinity of the permeant....
|
PMID: 17387599
PDF is available here.
Abstract
We have developed a highly regioselective synthesis of heterocycles via palladium-catalyzed annulation reaction of heteroatom-substituted allenes. Various aryl halides were reacted and one regioisomer was observed exclusively in all reactions. In addition, subsequent functionalizations of annulated...
|
PMID: 16272743
PDF is available here.
Abstract
The 1H-pyrazole-3-carboxylic acid 2 was converted in good yield (69%) into the corresponding 1H-pyrazole-3-carboxamide 5 via reaction of the acid chloride 3 with 2,3- diaminopyridine (4). A different product, the 3H-imidazo[4,5-b] pyridine derivative 6, was formed from the reaction of 3 with 4 and b...
|
PMID: 18007329
PDF is available here.
Abstract
Both 25R and 25S 23-oxospirostanes undergo rearrangement to the 22-oxo-23-spiroketal isomers promoted by Lewis acids. An X-ray crystal structure analysis of the rearranged product of 23-oxosarsasapogenin acetate confirmed the R configuration at the new spiro carbon atom.
Copyright 2004 Elsevier Inc....
|
PMID: 15219789
PDF is available here.
Abstract
The reactions of the 2-benzoselenopyrylium (1A) and 2-benzotelluropyrylium cations (1B) with a variety of nucleophiles have been investigated. LiAlH(4), sodium alkoxide (NaOMe, NaOi-Pr and NaOt-Bu), diethylamine, n-butylamine and acetone reacted with 1 to give the 1H-isochromenes (2) and the corresp...
|
PMID: 14709869
PDF is available here.
Abstract
The design, synthesis and in vitro activities of novel alpha-bromoacryloyl pyrazole, imidazole and benzoheterocyclic derivatives of distamycin A, in which the amidino moiety has been replaced by moieties of different physico-chemical features are described, and the structure-activity relationships a...
|
PMID: 12614881
PDF is available here.
Abstract
These results suggest that the L-like conformation is specifically recognized by the active site of the ET(A) receptor. The roles of the L-like conformation in the receptor binding are discussed....
|
PMID: 12413848
PDF is available here.
Abstract
We report the syntheses and biological activities of analogues containing modified biphenyl moieties, bearing heterocyclic proximal rings. Compound 20, the thioacetate ethyl ester prodrug derivative of compound 19a, was found to be an orally active and potent inhibitor of ECE-1 activity in rats....
|
PMID: 12372501
PDF is available here.
Abstract
[structure: see text] Bisbinaphthyl-based macrocycles are found to carry out highly enantioselective fluorescent recognition of alpha-hydroxycarboxylic acids. It is observed that within a certain concentration range, one enantiomer of the chiral acids can increase the fluorescence intensity of the m...
|
PMID: 12227773
PDF is available here.
Abstract
Nine organic acids (formic, pyruvic, lactic, acetic, orotic, citric, uric, propionic, and butyric) were analyzed during ripening of pickled White cheese for 12 mo by high-performance liquid chromatography with a reverse phase C18 (120x 5-mm) column and UV detector. The level oftotal organic acids sh...
|
PMID: 12201516
PDF is available here.
Abstract
The sensitization of the Tb(III) and Eu(III) ions luminescence by drugs, the pyrocatechol, naphthyridine and heterocyclic aromatic acid derivatives, were studied. It was shown that a result of intramolecular energy transfer from the ligand molecule to the lanthanide ion increases the luminescence in...
|
PMID: 9863967
PDF is available here.