A5021774563- Chemokine receptors and signaling
- Immune Cell Function and Interaction
- Cytokine Signaling Pathways and Interactions
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Traumatic Brain Injury Research
- Trauma and Emergency Care Studies
- Immunotherapy and Immune Responses
- Asymmetric Synthesis and Catalysis
- Oxidative Organic Chemistry Reactions
- Chronic Disease Management Strategies
- Synthesis and Catalytic Reactions
- Click Chemistry and Applications
- Advanced Photocatalysis Techniques
- Pharmacogenetics and Drug Metabolism
- Biotechnology and Related Fields
- Synthesis and biological activity
- Geriatric Care and Nursing Homes
- Rheumatoid Arthritis Research and Therapies
- Antimicrobial Peptides and Activities
- Pharmacological Receptor Mechanisms and Effects
- Radical Photochemical Reactions
- Pharmacological Effects of Natural Compounds
- Electroconvulsive Therapy Studies
- Eicosanoids and Hypertension Pharmacology
Shepherd Center
2024
Bristol-Myers Squibb (United States)
2003-2022
Duke University Health System
2016-2022
Duke University
2022
Duke University Hospital
2016
Campbell University
2016
Pathways Behavioral Services
2013
GlaxoSmithKline (United States)
2013
GlaxoSmithKline (United Kingdom)
2008
University of Missouri
2006
BMS-813160 (compound 3) was identified as a potent and selective CCR2/5 dual antagonist. Compound 3 displayed good permeability at pH = 7.4 in PAMPA experiments demonstrated excellent human liver microsome stability. Pharmacokinetic studies established that had oral bioavailability exhibited low clearance dog cyno. also studied the mouse thioglycollate-induced peritonitis model, which confirmed its ability to inhibit migration of inflammatory monocytes macrophages. As result this profile,...
Primary objective To gain an understanding of current evaluation practices, post-injury recommendations, and referrals to allied healthcare professions (AHP) by first-line professionals (FHPs) providing care for people with mild traumatic brain injury (mTBI).
We describe the hybridization of our previously reported acyclic and cyclic CC chemokine receptor 2 (CCR2) antagonists to lead a new series dual CCR2 CCR5. Installation γ-lactam as spacer group quinazoline benzamide mimetic improved oral bioavailability markedly. These efforts led identification 13d, potent orally bioavailable antagonist suitable for use in both murine monkey models inflammation.
We encountered a dilemma in the course of studying series antagonists G-protein coupled receptor CC chemokine receptor-2 (CCR2): compounds with polar C3 side chains exhibited good ion channel selectivity but poor oral bioavailability, whereas lipophilic bioavailability preclinical species selectivity. Attempts to solve this through direct modulation physicochemical properties failed. However, installation protonation-dependent conformational switching mechanism resolved problem because it...
We report here the BMS-PR460: a photoreactor designed for multi-reaction arrays at various scales and temperatures with irradiation 460 nm. Transformations of interest to pharmaceutical research have been performed demonstrate reactor utility.
Purpose: Speech-language pathologists provide important services to people recovering from mild traumatic brain injury (mTBI), also called concussion, although they may be underutilized in outpatient care. Because health care providers face challenges selecting assessments efficiently describe patient needs, the purpose of this study was factors related patients receiving speech-language pathology after mTBI, as well how predict amount received. Method: In retrospective chart review study,...
To improve the metabolic stability profile of BMS-741672 (1a), we undertook a structure–activity relationship study in our trisubstituted cyclohexylamine series. This ultimately led to identification 2d (BMS-753426) as potent and orally bioavailable antagonist CCR2. Compared previous clinical candidate 1a, tert-butyl amine showed significant improvements pharmacokinetic properties, with lower clearance higher oral bioavailability. Furthermore, compound exhibited improved affinity for CCR5...
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This article describes the Highly Individualized Dedicated Onsite Care (HIDOC) intensive primary care program implemented at a university clinic, comprising (a) by an interprofessional team, (b) new logistical capacity, and (c) clinician skills training. Measured outcomes include Emergency Department (ED) visits hospitalizations community hospital over 2 years, using within-subjects design. We demonstrate decreased University Hospital, decrease in ED both sites. Team-based strategies to...