Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Dean K. Clodfelter"'
Autor:
Dean K. Clodfelter, Anthony Rees
Publikováno v:
Journal of Labelled Compounds and Radiopharmaceuticals. 53:300-314
Autor:
William J. Wheeler, Dean K. Clodfelter
Publikováno v:
Journal of Labelled Compounds and Radiopharmaceuticals. 51:175-181
Enzastaurin (3-(1-methyl-1H-indol-3-yl)-4-[1-[1-(2-pyridinylmethyl)-4-piperidinyl]-1H-indol-3-yl]-1H-pyrrole-2,5-dione, 1), an agent with potential utility in the treatment of solid tumors, is currently in phase II clinical trials. Enzastaurin underg
Publikováno v:
Journal of Labelled Compounds and Radiopharmaceuticals. 50:706-710
Carbon-14-labeled 6-(4-methanesulfonylphenyl)-5-[4-(2-piperidin-1-yl-ethoxy)phenoxy]naphthalen-2-ol, a novel selective estrogen receptor modulator (SERM) was synthesized. The key component, 6-methoxy-1-tetralone-[carbonyl-14C], was synthesized from 3
Publikováno v:
Journal of Labelled Compounds and Radiopharmaceuticals. 50:693-701
Although fenofibrate (1a) is commercially available and clinically effective in lowering serum triglycerides, its activity and sub-type selectivity at the PPARα receptors are only moderate; therefore, there exists a need for more potent and sub-type
Publikováno v:
Journal of Labelled Compounds and Radiopharmaceuticals. 49:663-673
The synthesis of β3-adrenergic receptor agonists A and B with radiolabeled amide fragment, required for drug disposition studies, was accomplished based on initial formation of 2-(4-(2-amino-2-methylpropyl)phenoxy)-5-[14C]-cyanopyridine by the react
Publikováno v:
Journal of Labelled Compounds and Radiopharmaceuticals. 48:85-100
Asymmetric synthesis of AMPA potentiator LY450108-[14C] containing 14C-label attached to the chiral center of the molecule, was accomplished based on Evans' chiral oxazolidinone auxiliary method. Diastereoselective methylation of p-nitrophenylacetic
Publikováno v:
Journal of Labelled Compounds and Radiopharmaceuticals. 47:615-625
Carbon-14 labeled StraterraTM (Atomoxetine HCl, LY139603, (-)-N-methyl-3-(2-methylphenoxy)-benzenepropanamine hydrochloride), a potent inhibitor of the presynaptic norepinephrine transporter, and two of its major metabolites were synthesized. The key
Publikováno v:
Journal of Labelled Compounds and Radiopharmaceuticals. 47:599-608
Human Factor Xa is a trypsin-like serine protease, which serves a critical role in blood coagulation events. LY517717 is currently under clinical investigation as a Factor Xa inhibitor. To support the ADME studies, LY517717 was synthesized using D-ph
Publikováno v:
Journal of Labelled Compounds and Radiopharmaceuticals. 45:1143-1152
Synthesis of 4-hydroxyindole labeled with 14C at the 2-position was accomplished based on the vicarious nucleophilic substitution reaction of benzyl-protected 3-nitrophenol with p-chlorophenoxyacetonitrile-[1-14C]. This was followed by the reductive
Autor:
Kevin A. Destrampe, Dawn Marie Rebhun, Dean K. Clodfelter, Allen H. Pekar, Sharon R. Myers, Henry A. Havel, Mark L. Brader
Publikováno v:
Pharmaceutical Research. 15:254-262
Purpose. To utilize an acylated peptide as a model system to investigate the relationships among solution peptide conformation, non-covalent self-association, subcutaneous absorption and bioavailability under pharmaceutically relevant solution formul