Lawrence Joseph Heinz

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Featured researches published by Lawrence Joseph Heinz.

Bioorganic & Medicinal Chemistry Letters | 1996

Synthesis and structure-activity relationships of benzophenones as inhibitors of cathepsin D

Celia A. Whitesitt; Richard Lee Simon; Jon K. Reel; Sandra Kay Sigmund; Michael Leroy Phillips; J. Kevin Shadle; Lawrence Joseph Heinz; Gary A. Koppel; David C. Hunden; Sherryl Lynn Lifer; Dennis R. Berry; Judy Ray; Sheila P. Little; Xiadong Liu; Winston S. Marshall; Jill Ann Panetta

Abstract Non peptide inhibitors of cathepsin D, an aspartyl protease that has been implicated in many disease states including Alzheimers disease, were prepared and evaluated. The most potent inhibitor of cathepsin D in this series was found to be (Z)-5-[[4-(4-benzoyl-3-hydroxy-2-propylphenoxy) methylphenyl]methylene]-2-thioxo-4-thiazolidinone ( 3f , IC 50 = 210 nM).

Bioorganic & Medicinal Chemistry Letters | 1998

Heteroatom-substitution as a strategy for increasing the potency of competitive NMDA antagonists

Paul L. Ornstein; M. Brian Arnold; William Henry Walker Lunn; Lawrence Joseph Heinz; J. David Leander; David Lodge; Darryle D. Schoepp

We report the synthesis and characterization of compounds that are competitive NMDA receptor antagonists. Significant increases in affinity and potency were obtained by incorporation of a heteroatom into the substructure of the tetrazole-substituted amino acid LY233053.

Archive | 2003

Multicyclic compounds for use as melanin concentrating hormone antagonists in the treatment of obesity and diabetes

Jochen Ammenn; James Ronald Gillig; Lawrence Joseph Heinz; Philip Arthur Hipskind; Michael Dean Kinnick; Yen-Shi Lai; John Michael Morin; James Arthur Nixon; Carsten Ott; Kenneth Allen Savin; Theo Schotten; Lawrence J. Slieker; Nancy June Snyder; Michael Alan Robertson

Archive | 1995

Inhibitors of amyloid beta-protein production

Lawrence Joseph Heinz; Jill Ann Panetta; Michael Leroy Phillips; Jon K. Reel; John Kevin Shadle; Richard Lee Simon; Celia A. Whitesitt

Journal of Medicinal Chemistry | 1992

DL-Tetrazol-5-ylglycine, a highly potent NMDA agonist: its synthesis and NMDA receptor efficacy

William Henry Walker Lunn; Darryle D. Schoepp; David O. Calligaro; R. T. Vasileff; Lawrence Joseph Heinz; Craig R. Salhoff; Patrick J. O'Malley

Archive | 2002

Benzenesulfonic acid indol-5-yl esters as antagonists of the 5-ht6 receptor

Sandra Ann Filla; Michael Edward Flaugh; James Ronald Gillig; Lawrence Joseph Heinz; Joseph H. Krushinski; Bin Liu; Marta Maria Pineiro-Nunez; John Mehnert Schaus; John S. Ward

Archive | 1997

Novel compounds useful as neuro-protective agents

Lawrence Joseph Heinz; Jill Ann Panetta; Michael Leroy Phillips; John Kevin Shadle

Journal of Organic Chemistry | 1996

An Efficient Synthesis of cis- and trans-Methyl-3-hydroxy-2-pyrrolidone- 5-carboxylates, Key Intermediates for the Synthesis of gamma-Substituted Glutamic Acid Analogs.

Lawrence Joseph Heinz; William Henry Walker Lunn; R. E. Murff; Jonathan W. Paschal; Larry A. Spangle

Analytical Biochemistry | 2004

Europium-labeled melanin-concentrating hormone analogues: ligands for measuring binding to melanin-concentrating hormone receptors 1 and 2

Xiaoying Gao; Chiun-King Hsu; Lawrence Joseph Heinz; John Michael Morin; Yuguang Shi; Nikhil K Shukla; David L. Smiley; Jie Xu; Boyu Zhong; Lawrence J. Slieker

Archive | 1997