androstane skeleton with a keto-enol tautomerism at the cyclopentane ring. Wecarried out further isolation for PFTase inhibitors from the cultured broth of strain FO-3929 and found andrastin D (4, Fig. 1). In this paper, fermentation, isolation, structure elucidation, and biological properties of 4 are described. A stock culture of strain FO-3929 was inoculated into six 500-ml Erlenmeyer flasks...

Biologically and pharmaceutically active core structures containing a new class of 4-hydroxy-α-carbolines, dihydropyrido[2,3-b]indoles, pyrimido[4,5-b] and [5,4-b]indoles have been synthesized in good yields via Pd-catalyzed amidation and cyclizations. The keto-enol tautomerism in 4-hydroxy-α-carbolines has been investigated by DFT calculations and spectroscopic techniques. The fluorescence stu...

In this laboratory exercise we will measure the Equilibrium Constant Kc for the keto-enol tautomerism of two -diketones and two -diketoesters. This will be accomplished by measuring the signal strength of key protons in the Nuclear Magnetic Resonance (NMR) spectrum of the equilibrium system. The influence of the solvent on the equilibrium position will be examined by considering the measured ...

Glucagon-like peptide 1 (GLP-1) lowers glycemia by modulating gastric emptying and endocrine pancreatic secretion. Rapidly after its secretion, GLP-1-(7-36) amide is degraded to the metabolite GLP-1-(9-36) amide. The effects of GLP-1-(9-36) amide in humans are less well characterized. Fourteen healthy volunteers were studied with intravenous infusion of GLP-1-(7-36) amide, GLP-1-(9-36) amide, o...

Glucagon-like peptide 1 (GLP-1) is a potent anti-hyperglycemic hormone currently under investigation for its therapeutic potential. However, due to rapid degradation by dipeptidyl peptidase IV (DPP IV), which limits its metabolic stability and eliminates its insulinotropic activity, it has been impossible to assess its true efficacy in vivo. In chloralose-anesthetized pigs given valine-pyrrolid...