A5028325803- Synthesis and biological activity
- Cholinesterase and Neurodegenerative Diseases
- Bone health and osteoporosis research
- Lanthanide and Transition Metal Complexes
- Multicomponent Synthesis of Heterocycles
- Advanced MRI Techniques and Applications
- Computational Drug Discovery Methods
- Diet, Metabolism, and Disease
- Diet and metabolism studies
- Synthesis of Organic Compounds
- Medical Imaging Techniques and Applications
- Cardiovascular Disease and Adiposity
- Alzheimer's disease research and treatments
- Obesity, Physical Activity, Diet
- Vitamin D Research Studies
- Liver Disease Diagnosis and Treatment
- Adipokines, Inflammation, and Metabolic Diseases
- Organic Chemistry Cycloaddition Reactions
- Adrenal Hormones and Disorders
- Chemical Synthesis and Analysis
- Hormonal Regulation and Hypertension
- Free Radicals and Antioxidants
- Pituitary Gland Disorders and Treatments
- Synthesis and Characterization of Heterocyclic Compounds
- Adrenal and Paraganglionic Tumors
Université de franche-comté
2022-2025
Inserm
2024-2025
Laboratoire de Neurosciences Cognitives
2024
Laboratoire de recherches Intégratives en Neurosciences et psychologie Cognitive
2024
Université Bourgogne Franche-Comté
2022
GI Specialists of Georgia (United States)
2015-2019
Augusta University
2010-2011
National Institutes of Health
2006
Rogers (United States)
1998-2002
Epix Pharmaceuticals (United States)
1998-1999
Abstract Childhood studies of the fat-bone relationship are conflicting, possibly reflecting influence metabolic abnormalities in some but not all obese children. Bone mass was compared between prepubertal overweight children with (n = 41) and without 99) prediabetes. Associations bone measures total central adiposity, glucose intolerance, insulin sensitivity, lipid profile, systemic inflammation, osteocalcin also were determined. In 140 aged 7 to 11 years, an oral tolerance test used...
Although animal studies suggest that it is the uncarboxylated rather than carboxylated form of osteocalcin affects glucose homeostasis, human data are scant and equivocal.
Amphiphilic gadolinium complexes were investigated as potential magnetic resonance imaging (MRI) contrast agents. A series of was synthesized in order to study the effect hydrophilic phosphodiester groups on albumin binding, relaxivity, and blood half-life rats. Thus, compound 11a, a diethylenetriaminepentaacetato aquo gadolinium(III) (Gd-DTPA) derivative with an octyl substituent, compared 5b, analogous containing linkage between chelate alkyl chain. Likewise, 11b, naphthyl Gd-DTPA...
Abstract Herein, we describe the high yielding synthesis of spiropyrimido[4,5‐ d ]pyrimidines by Friedländer‐type reaction substituted 4‐aminopyrimidine‐5‐carbonitriles with cyclohexanone, using sodium ethoxide as catalyst. The biological activity new compounds anti‐inflammatory agents was evaluated and to predict their pharmacological properties a comprehensive in silico analysis conducted. Among tested compound, three exhibited potent lipoxygenase inhibitory comparing very well reference...
Islet neogenesis associated protein (INGAP) is a factor that can stimulate new islet mass from adult pancreatic progenitor cells. In models of neogenesis, INGAP expression elevated in acinar Using transgenic model to drive sustained cells, we have identified protection chemical-induced hyperglycemia. A during development did not perturb or basal blood glucose homeostasis, although β-cell and insulin content were significantly increased the mice. When challenged with diabetogenic dose...
Excess fat within bone marrow is associated with lower density. Metabolic stressors such as chronic caloric restriction (CR) can exacerbate adiposity, and increased glucocorticoid signaling adrenergic are implicated in this phenotype. The current study tested the role of CR-induced stress by conditionally deleting receptor (GR) osteoprogenitors (Osx1-Cre) mice subjected to CR ad libitum diets. Conditional knockout GR (GR-CKO) reduced cortical trabecular mass compared wildtype (WT) under both...
Alzheimer's disease (AD) is a multifactorial neurodegenerative that has heavy social and economic impact on all societies for which there still no cure. Multitarget-directed ligands (MTDLs) seem to be promising therapeutic strategy finding an effective treatment this disease. For purpose, new MTDLs were designed synthesized in three steps by simple cost-efficient procedures targeting calcium channel blockade, cholinesterase inhibition, antioxidant activity. The biological physicochemical...
ABSTRACTIntroduction Alzheimer’s disease (AD) is a progressive, irreversible, and multifactorial brain disorder that gradually insidiously destroys individual’s memory, thinking, other cognitive abilities.Areas covered In this perspective, the authors examine complex nature of believe best approach to develop new drugs MTDL strategy, which obviously faces several challenges. These challenges include identifying key combination targets their suitability for coordinated actions, as well...
Abstract Herein we report the synthesis of ten newly substituted 3‐phenyl‐5‐aryl‐3,5‐dihydro‐4 H ‐benzo[6,7]chromeno[2,3‐ d ]pyrimidin‐4,6,11‐triones (“benzochromenopyrimidines”) in a one‐step reaction, by reacting ethyl 2‐amino‐4‐aryl‐5,10‐dioxo‐5,10‐dihydro‐4 ‐benzo[ g ]chromene‐3‐carboxylates with aniline, and triethyl orthoformate, under acidic catalyst solvent‐free conditions. These benzochromenopyrimidines were submitted to biological evaluation for vitro anti‐cancer activity, several...
This work relates to the design and synthesis of a series novel multi-target directed ligands (MTDLs), i.e., compounds 4a–l, via convenient one-pot three-component Hantzsch reaction. approach targeted calcium channel antagonism, antioxidant capacity, cathepsin S inhibition, interference with Nrf2 transcriptional activation. Of these MTDLs, 4i emerged as promising compound, demonstrating robust activity, ability activate Nrf2-ARE pathways, well blockade inhibition. Dihydropyridine represents...
Novel multitarget-directed ligands BIGI 4a-d and 5a-d were designed synthesized with a simple cost-efficient procedure via one-pot three-component Biginelli reaction targeting acetyl-/butyrylcholinesterases inhibition, calcium channel antagonism, antioxidant ability. Among these ligands, 4b, 4d, 5b identified as promising new hit compounds showing in vitro balanced activities toward the recognized AD targets. In addition, showed suitable physicochemical properties good druglikeness score...
Ten new differently substituted 3-benzyl-5-aryl-3,5-dihydro-4H-benzo[6,7]chromeno[2,3-d]pyrimidin-4,6,11-triones 3 were synthesized by a simple and cost-efficient procedure in one-pot, three-component reaction from readily available ethyl 2-amino-4-aryl-5,10-dioxo-5,10-dihydro-4H-benzo[g]chromene-3-carboxylates, benzylamine triethyl orthoformate under solvent- catalyst-free conditions. All the compounds screened for their antiproliferative activity against two colorectal-cancer-cell lines....
Abstract An efficient synthesis of alcohol 2 is described from L-Serine (OMe) in four synthetic steps. The process uses readily available reagents and suitable for manufacturing.
Abstract A preparation of 4,4-diphenylcyclohexanol 2 is described from benzoin in five synthetic steps. The process uses readily available reagents and suitable for manufacturing.
Eleven new differently substituted N,7-diphenylpyrimido [4,5-d]pyrimidin-4-amines 4a–k were synthesized from readily available reagents in a simple and inexpensive two-step procedure with yields up to 57%. Neuroprotective analysis against H2O2 using ORAC assays identified compounds 4g, 4i 4j as promising antioxidant compounds. These also showed potent inhibition of Aβ1–42 self-aggregation, suitable physicochemical properties predicted by Datawarior software V6.1.0, this biological activity...