A5073868581- Peroxisome Proliferator-Activated Receptors
- Chemical synthesis and alkaloids
- Asymmetric Synthesis and Catalysis
- Adipose Tissue and Metabolism
- Metabolism, Diabetes, and Cancer
- Circadian rhythm and melatonin
- Sleep and Wakefulness Research
- Sleep and related disorders
- Receptor Mechanisms and Signaling
- Advanced Synthetic Organic Chemistry
- Alkaloids: synthesis and pharmacology
- Regulation of Appetite and Obesity
- Synthesis and Reactions of Organic Compounds
- Synthesis and Biological Evaluation
- Coordination Chemistry and Organometallics
- Multicomponent Synthesis of Heterocycles
- Eicosanoids and Hypertension Pharmacology
- Synthesis and Reactivity of Heterocycles
- Chemical Synthesis and Analysis
- Synthesis and biological activity
- Neurobiology and Insect Physiology Research
- Pancreatic function and diabetes
- Organophosphorus compounds synthesis
- Signaling Pathways in Disease
- Inflammasome and immune disorders
Stanford University
2021
Reset Therapeutics
2015-2018
Pfizer (United States)
2006-2014
University of Sheffield
1999-2000
In only seven steps a formal synthesis of enantiomerically enriched (+)-anatoxin-a has been achieved. This was accomplished by utilizing highly enantioselective desymmetrization the eight-membered ring ketone 1 to form 2, and novel cascade reaction construct 9-azabicyclo[4.2.1]nonane skeleton.
As part of a strategy to deliver short-acting calcium-sensing receptor (CaSR) antagonists, the metabolically labile thiomethyl functionality was incorporated into zwitterionic amino alcohol derivative 3 with hope increasing human clearance through oxidative metabolism, while delivering pharmacologically inactive sulfoxide metabolite. The effort led identification thioanisoles 22 and 23 as potent orally active CaSR antagonists rapid onset action short pharmacokinetic half-lives, which...
Narcolepsy type 1 (Na-1) and 2 (Na-2) are characterized by an inability to sustain wakefulness likely caused degeneration of orexin neurons. Near complete neurodegeneration depletes orexin-A from the cerebrospinal fluid produces Na-1. The pathophysiology Na-2 is less understood but has been hypothesized be due extensive loss neurotransmission. orexin-tTA; TetO diphtheria toxin A mouse allows conditional control over extent timing neurodegeneration. To evaluate partial ablation field as a...
Conformationally rigid chiral lithium amides based on a tetrahydroisoquinoline motif have been prepared bearing range of substituents at C1 and C3. These bases were tested in the asymmetric deprotonation reaction 4-tert-butylcyclohexanone. Although 1-substituted tetrahydroisoquinolines gave low enantioselectivity, containing nitrogen heterocycle C3 found to induce high enantioselectivity (81% ee) presence HMPA.
Abstract Background Assessment of sleep/wake by electroencephalography (EEG) and electromyography (EMG) is invasive, resource intensive, not amenable to rapid screening at scale for drug discovery. In the preclinical development therapeutics narcolepsy, efficacy tests are hindered lack a non-EEG/EMG based translational test symptom severity. The current methods study offers proof-of-principle that PiezoSleep (noninvasive, unsupervised piezoelectric monitoring gross body movement, together...
A series of pyridine ether PPAR agonists were synthesized through an ADDP and PS-PPh3 modified Mitsunobu protocol, which eliminated significant by-product formation. This method proved to be versatile, efficient amenable parallel synthesis.
In nur sieben Stufen gelang die formale Synthese von enantiomerenangereichertem (+)-Anatoxin-a. Dies wurde erreicht durch eine hoch enantioselektive Desymmetrisierung des Achtringketons 1 unter Bildung 2 und anschließende neuartige Kaskadenreaktion zum Aufbau 9-Azabicyclo[4.2.1]nonan-Gerüsts.