M. Wood

发表

Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor.

Brian A. Chauder, Bruce J. Melancon, D. Sheffler, 2012, Bioorganic & medicinal chemistry letters.

Discovery and development of a second highly selective M1 Positive Allosteric Modulator (PAM)

C. Lindsley, C. Weaver, E. Dawson, 2010 .

Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator (PAM) Series with Greatly Improved Human Receptor Activity

C. Lindsley, P. Conn, C. Niswender, 2010 .

Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism.

D. Sheffler, C. Lindsley, C. Hopkins, 2013, Bioorganic & medicinal chemistry letters.

Chemical modification of the M(1) agonist VU0364572 reveals molecular switches in pharmacology and a bitopic binding mode.

D. Sheffler, C. Lindsley, E. Lebois, 2012, ACS chemical neuroscience.

Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia.

Bruce J. Melancon, Anna L. Blobaum, D. Sheffler, 2013, Bioorganic & medicinal chemistry letters.

Further optimization of the M5 NAM MLPCN probe ML375: tactics and challenges.

C. Lindsley, Hyekyung P. Cho, P. Conn, 2015, Bioorganic & medicinal chemistry letters.

Discovery, Synthesis and Characterization of a Highly Muscarinic Acetylcholine Receptor (mAChR)‐Selective M5‐Orthosteric Antagonist, VU0488130 (ML381): A Novel Molecular Probe

C. Lindsley, Hyekyung P. Cho, P. Conn, 2014, ChemMedChem.

Discovery and optimization of a novel, selective and brain penetrant M1 positive allosteric modulator (PAM): the development of ML169, an MLPCN probe.

D. Sheffler, C. Lindsley, Hyekyung P. Cho, 2011, Bioorganic & medicinal chemistry letters.

Identification of Positive Allosteric Modulators VU0155094 (ML397) and VU0422288 (ML396) Reveals New Insights into the Biology of Metabotropic Glutamate Receptor 7

Bruce J. Melancon, K. Gregory, Z. Xiang, 2014, ACS chemical neuroscience.

Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes

Tudor I. Oprea, Jennifer E. Golden, Joshua A. Bittker, 2015, Cell.

Development and characterization of a highly selective M5 PAM probe molecule with improved potency

Julie L. Engers, C. Lindsley, P. Conn, 2013 .

Extended Probe Characterization: Development of an M4 PAM with Improved Activity and Brain Exposure, while Avoiding Species Bias

Julie L. Engers, Bruce J. Melancon, D. Sheffler, 2013 .

Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides.

Bruce J. Melancon, N. Brandon, C. Lindsley, 2017, Bioorganic & medicinal chemistry letters.

Discovery and SAR of a novel series of potent, CNS penetrant M4 PAMs based on a non-enolizable ketone core: Challenges in disposition.

N. Brandon, C. Lindsley, P. Conn, 2016, Bioorganic & medicinal chemistry letters.

Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core.

Alison R. Gregro, Julie L. Engers, Bruce J. Melancon, 2016, Bioorganic & medicinal chemistry letters.

5-Piperazinyl pyridine carboxamide bradykinin B1 antagonists.

M. Bock, S. Kuduk, T. Prueksaritanont, 2006, Bioorganic & medicinal chemistry letters.

Benzodiazepines as potent and selective bradykinin B1 antagonists.

Tsing-Bau Chen, M. Bock, R. M. Dipardo, 2003, Journal of medicinal chemistry.

Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia.

Bruce J. Melancon, Anna L. Blobaum, N. Brandon, 2017, ACS medicinal chemistry letters.

Novel CGRP receptor antagonists from central amide replacements causing a reversal of preferred chirality.

J. Vacca, H. Selnick, R. Bednar, 2010, Bioorganic & medicinal chemistry letters.

The antipsychotic potential of muscarinic allosteric modulation.

C. Lindsley, C. Hopkins, E. Lebois, 2010, Drug news & perspectives.

Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and in vivo characterization of a series of 3-aminoazetidine-derived amides.

N. Brandon, C. Lindsley, Hyekyung P. Cho, 2017, Bioorganic & medicinal chemistry letters.

Total Syntheses of Vancomycin and Eremomycin Aglycons.

J. Barrow, T. I. Richardson, Davidr . Evans, 1998, Angewandte Chemie.

Cyanocuprate-catalyzed 1,4-additions of vinylic zirconocenes using a zincate as an organolithium shuttle. A new and potentially practical approach to 3-component couplings

B. Lipshutz, M. Wood, 1993 .

Michael Additions of Functionalized Organozinc Reagents Mediated by Catalytic Quantities of Copper(I)

B. Lipshutz, M. Wood, R. Tirado, 1995 .

Total Syntheses of Vancomycin and Eremomycin Aglycons.

J. Barrow, T. I. Richardson, Davidr . Evans, 1998, Angewandte Chemie.

Copper‐Catalyzed Conjugate Addition of Functionalized Organozinc Reagents to α,β‐Unsaturated Ketones: Ethyl 5‐(3‐Oxocyclohexyl)Pentanoate

B. Lipshutz, M. Wood, R. Tirado, 2003 .

Synthesis and biological activity of novel cephalosporins containing a (Z)-vinyl dimethylphosphonate group.

P. Smith, P. Howes, K. Cobley, 1995, The Journal of antibiotics.

Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery.

Bruce J. Melancon, A. Christopoulos, C. Lindsley, 2012, Journal of medicinal chemistry.

Nonconventional Stereochemical Issues in the Design of the Synthesis of the Vancomycin Antibiotics: Challenges Imposed by Axial and Nonplanar Chiral Elements in the Heptapeptide Aglycons.

T. I. Richardson, Davidr . Evans, C. Dinsmore, 1998, Angewandte Chemie.

"Molecular switches" on mGluR allosteric ligands that modulate modes of pharmacology.

P Jeffrey Conn, Craig W Lindsley, C. Lindsley, 2011, Biochemistry.

An Efficient Procedure for Preparation of C‐ and N‐Protected 1‐Aminocyclobutane Carboxylic Acid

M. Wood, J. J. Kim, 2004 .

Substituted indoles as selective protease activated receptor 4 (PAR-4) antagonists: Discovery and SAR of ML354.

Julie L. Engers, Bruce J. Melancon, H. Hamm, 2014, Bioorganic & medicinal chemistry letters.

Cyclopropylamino acid amide as a pharmacophoric replacement for 2,3-diaminopyridine. Application to the design of novel bradykinin B1 receptor antagonists.

M. Bock, R. Freidinger, R. Chang, 2006, Journal of medicinal chemistry.

Alpha-hydroxy amides as a novel class of bradykinin B1 selective antagonists.

M. Bock, R. M. Dipardo, R. Freidinger, 2008, Bioorganic & medicinal chemistry letters.

Allosteric modulation of the M1 muscarinic acetylcholine receptor: improving cognition and a potential treatment for schizophrenia and Alzheimer's disease.

Craig W Lindsley, Bruce J. Melancon, Bruce J Melancon, 2013, Drug discovery today.

State-dependent alterations in sleep/wake architecture elicited by the M4 PAM VU0467154 – Relation to antipsychotic-like drug effects

N. Brandon, C. Lindsley, M. Ivarsson, 2016, Neuropharmacology.

Phosphodiesterase 10 A Regulates Alcohol and Saccharin Self-Administration in Rats

Robert L Barry, John C Gore, P Jeffrey Conn, 2014 .

Discovery of ML326: The first sub-micromolar, selective M5 PAM.

Julie L. Engers, C. Lindsley, P. Conn, 2013, Bioorganic & medicinal chemistry letters.

Synthesis and biological characterization of a series of novel diaryl amide M₁ antagonists.

D. Sheffler, C. Lindsley, P. Conn, 2012, Bioorganic & medicinal chemistry letters.

Development of novel M1 antagonist scaffolds through the continued optimization of the MLPCN probe ML012.

Bruce J. Melancon, D. Sheffler, C. Lindsley, 2012, Bioorganic & medicinal chemistry letters.

Development of a more highly selective M(1) antagonist from the continued optimization of the MLPCN Probe ML012.

Bruce J. Melancon, D. Sheffler, C. Lindsley, 2012, Bioorganic & medicinal chemistry letters.

Development of orally bioavailable and CNS penetrant biphenylaminocyclopropane carboxamide bradykinin B1 receptor antagonists.

M. Bock, R. M. Dipardo, D. Reiss, 2007, Journal of medicinal chemistry.

COVID-19 and autoinflammatory diseases: prevalence and outcomes of infection and early experience of vaccination in patients on biologics

C. Papadopoulou, H. Lachmann, Claire J Peet, 2021, Rheumatology advances in practice.

Targeting selective activation of M(1) for the treatment of Alzheimer's disease: further chemical optimization and pharmacological characterization of the M(1) positive allosteric modulator ML169.

Anna L. Blobaum, D. Sheffler, C. Lindsley, 2012, ACS chemical neuroscience.

Allosteric modulation of the M 1 muscarinic acetylcholine receptor : improving cognition and a potential treatment for schizophrenia and Alzheimer ’ s disease

Bruce J. Melancon, C. Lindsley, Joseph D. Panarese, 2013 .

Spectroscopic experiments on the role of Me3SiCl in lithium dialkylamide deprotonations

C. Lindsley, B. Lipshutz, M. Wood, 1995 .

Muscarinic receptor pharmacology and circuitry for the modulation of cognition.

N. Byun, M. Bubser, Michael Bubser, 2012, Handbook of experimental pharmacology.

Application of Parallel Multiparametric Cell-Based FLIPR Detection Assays for the Identification of Modulators of the Muscarinic Acetylcholine Receptor 4 (M4)

Peter Hodder, Louis Scampavia, Franck Madoux, 2015, Journal of biomolecular screening.

Allosteric activation of M4 muscarinic receptors improve behavioral and physiological alterations in early symptomatic YAC128 mice

Z. Xiang, C. Lindsley, P. Conn, 2015, Proceedings of the National Academy of Sciences.

Challenges in the development of an M4 PAM in vivo tool compound: The discovery of VU0467154 and unexpected DMPK profiles of close analogs.

Bruce J. Melancon, N. Brandon, C. Lindsley, 2017, Bioorganic & medicinal chemistry letters.

Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor.

Anna L. Blobaum, D. Sheffler, C. Lindsley, 2012, Bioorganic & medicinal chemistry letters.

Preview : Published ahead of advance online publication

C. Lindsley, P. Conn, C. Niswender, 2015 .

Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071.

D. Sheffler, Z. Xiang, C. Lindsley, 2011, Bioorganic & medicinal chemistry letters.

Discovery of the first M5-selective and CNS penetrant negative allosteric modulator (NAM) of a muscarinic acetylcholine receptor: (S)-9b-(4-chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-one (ML375).

Peter Chase, P Jeffrey Conn, Craig W Lindsley, 2013, Journal of medicinal chemistry.

M5 Receptor Activation Produces Opposing Physiological Outcomes in Dopamine Neurons Depending on the Receptor's Location

D. Sulzer, Z. Xiang, C. Lindsley, 2014, The Journal of Neuroscience.

Development of a Novel, Orthosteric M5 Antagonist Possessing a High Degree of Muscarinic Subtype Selectivity

Julie L. Engers, C. Lindsley, P. Conn, 2015 .

Development of a Highly Potent, Novel M5 Positive Allosteric Modulator (PAM) Demonstrating CNS Exposure: 1-((1H-Indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide (ML380)

C. Lindsley, Hyekyung P. Cho, P. Conn, 2014, Journal of medicinal chemistry.

SAR inspired by aldehyde oxidase (AO) metabolism: Discovery of novel, CNS penetrant tricyclic M4 PAMs.

Alison R. Gregro, Andrew S. Felts, N. Schnetz-Boutaud, 2019, Bioorganic & medicinal chemistry letters.

Novel M4 positive allosteric modulators derived from questioning the role and impact of a presumed intramolecular hydrogen-bonding motif in β-amino carboxamide-harboring ligands.

C. Lindsley, P. Conn, C. Niswender, 2019, Bioorganic & medicinal chemistry letters.

Influence of M1 muscarinic acetylcholine receptor activation on arousal and cognitive performance using electroencephalography and novel touchscreen cognition assessment (845.5)

J. Wess, Z. Xiang, C. Lindsley, 2014 .

Novel CGRP receptor antagonists through a design strategy of target simplification with addition of molecular flexibility.

J. Vacca, H. Selnick, I. M. Bell, 2009, Bioorganic & medicinal chemistry letters.

Spirocyclic replacements for the isatin in the highly selective, muscarinic M1 PAM ML137: the continued optimization of an MLPCN probe molecule.

D. Sheffler, C. Lindsley, P. Conn, 2013, Bioorganic & medicinal chemistry letters.

Discovery of MK-3207: A Highly Potent, Orally Bioavailable CGRP Receptor Antagonist.

J. Vacca, C. Regan, T. Prueksaritanont, 2010, ACS medicinal chemistry letters.

Potentiation of M1 Muscarinic Receptor Reverses Plasticity Deficits and Negative and Cognitive Symptoms in a Schizophrenia Mouse Model

C. Lindsley, P. Conn, C. Niswender, 2016, Neuropsychopharmacology.

Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia.

N. Brandon, C. Lindsley, P. Conn, 2017, ACS medicinal chemistry letters.

Antipsychotic Drug-Like Effects of the Selective M4 Muscarinic Acetylcholine Receptor Positive Allosteric Modulator VU0152100

Stephen M. Damon, A. Deutch, J. Wess, 2014, Neuropsychopharmacology.

Scheme 1, Reagents and conditions

C. Lindsley, P. Conn, C. Weaver, 2013 .

VU6005806/AZN-00016130, an advanced M4 positive allosteric modulator (PAM) profiled as a potential preclinical development candidate.

Alison R. Gregro, Andrew S. Felts, N. Brandon, 2019, Bioorganic & medicinal chemistry letters.

Optimization of M4 positive allosteric modulators (PAMs): The discovery of VU0476406, a non-human primate in vivo tool compound for translational pharmacology.

Bruce J. Melancon, N. Brandon, C. Lindsley, 2017, Bioorganic & medicinal chemistry letters.

Isatin replacements applied to the highly selective, muscarinic M1 PAM ML137: continued optimization of an MLPCN probe molecule.

D. Sheffler, C. Lindsley, Margrith E. Mattmann, 2013, Bioorganic & medicinal chemistry letters.