Rodger F. Henry

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PCR has many applications in the isolation and analysis of plant DNA. The influence of salt and EDTA concentration, pH, incubation time and temperature on the preparation of plant material for PCR was evaluated. A general single-step method was developed in which a small amount of plant tissue was heated in a simple solution. The DNA in the supernatant was(More)
Purpose. In the summer of 1998, Norvir semi-solid capsules supplies were threatened as a result of a new much less soluble crystal form of ritonavir. This report provides characterization of the two polymorphs and the structures and hydrogen bonding network for each form. Methods. Ritonavir polymorphism was investigated using solid state spectroscopy and(More)
We have extended the established physical stability treatment for hydrates/solvates to co-crystals with solid co-crystal formers. Based on the proposed treatment, a suspension/slurry screening technique is developed and tested in sixteen pharmaceutical co-crystal systems with success. The theoretical treatment and the practical screening technique should(More)
A stereoselective synthesis of the hydroxyethylene dipeptide isostere 1 is described. The route employs a substrate-directed kinetic protonation of an alpha/gamma-substituted lactone to afford the desired stereochemistry. A method for converting the diastereomerically enriched intermediate lactone to the ring-open form with retention of stereochemistry is(More)
One of the primary objectives in the design of protein inhibitors is to shape the three-dimensional structures of small molecules to be complementary to the binding site of a target protein. In the course of our efforts to discover potent inhibitors of Bcl-2 family proteins, we found a unique folded conformation adopted by tethered aromatic groups in the(More)
Structure-activity relationships were investigated on a novel series of tricyclic dihydropyridine-containing K(ATP) openers. This diverse group of analogues, comprising a variety of heterocyclic rings fused to the dihydropyridine nucleus, was designed to determine the influence on activity of hydrogen-bond-donating and -accepting groups and their(More)
(3R)-1-[4,4-bis(3-methyl-2-thienyl)-3-butenyl]-3-piperidinecarboxylic acid 1 (tiagabine, Gabitril) is a potent and selective gamma-aminobutyric acid (GABA) uptake inhibitor with proven anticonvulsant efficacy in humans. This drug, which has a unique mechanism of action among marketed anticonvulsant agents, has been launched for add-on treatment of partial(More)
Four solvates of erythromycin have been crystallographically characterized. The solvates of THF and dioxane are very similar but differ in notable ways. The isopropanol solvate exhibits uncommon modes of hydrogen bonding, which have previously been seen only in the erythomycin B hydrate. The methanol solvate is strikingly similar to the methanol solvate of(More)
Herein we report a concise protocol for the diastereoselective synthesis of novel bridged bicyclic lactams from commercially available components by the sequence of Ugi, ring-closing metathesis (RCM), and Heck reactions. X-ray diffraction studies revealed that the bicyclic products contain varying degrees of pyramidalization of the bridgehead nitrogen atom.
Starting from a rapidly metabolized adamantane 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) inhibitor 22a, a series of E-5-hydroxy-2-adamantamine inhibitors, exemplified by 22d and (+/-)-22f, was discovered. Many of these compounds are potent inhibitors of 11beta-HSD1 and are selective over 11beta-HSD2 for multiple species (human, mouse, and(More)