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NEW CLASS OF POTENT LIGANDS FOR THE HUMAN PERIPHERAL CANNABINOID RECEPTOR
Abstract A new class of potent ligand for the human peripheral cannabinoid (hCB 2 ) receptor is described. Two indole analogs 13 and 17 exhibited nanomolar potencies (K i ) with good selectivity for… Expand
Leukotrienes and Lipoxins: Synthesis and Biosynthesis
A cost-effectiveness analysis of interactive paediatric telecardiology
- C. Sicotte, P. Lehoux, N. van Doesburg, Godefroy Cardinal, Y. Leblanc
- Journal of telemedicine and telecare
- 1 April 2004
We analysed the cost-effectiveness of a teleconsultation service after five years of operation. The service provides diagnostic consultation at a distance for children suffering from cardiac… Expand
Identification of potent, selective KDM5 inhibitors.
- Victor S. Gehling, S. Bellon, +18 authors Brian K. Albrecht
- Chemistry, Medicine
- Bioorganic & medicinal chemistry letters
- 1 September 2016
This communication describes the identification and optimization of a series of pan-KDM5 inhibitors derived from compound 1, a hit initially identified against KDM4C. Compound 1 was optimized to… Expand
Chemical noise reduction via mass spectrometry and ion/ion charge inversion: amino acids.
Charge inversion ion/ion reactions can provide a significant reduction in chemical noise associated with mass spectra derived from complex mixtures for species composed of both acidic and basic… Expand
Cold plasma oxidation of harmful algae and associated metabolite BMAA toxin in aqueous suspension
From indomethacin to a selective COX-2 inhibitor: Development of indolalkanoic acids as potent and selective cyclooxygenase-2 inhibitors
Abstract A series of potent and highly selective cyclooxygenase-2 inhibitors have been prepared by replacing the benzoyl group of indomethacin with a 4-bromobenzyl group, and by extending the acetic… Expand
Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials.
- Brian K. Albrecht, Victor S. Gehling, +24 authors J. Audia
- Medicine, Biology
- Journal of medicinal chemistry
- 4 February 2016
In recent years, inhibition of the interaction between the bromodomain and extra-terminal domain (BET) family of chromatin adaptors and acetyl-lysine residues on chromatin has emerged as a promising… Expand
Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors.
- Victor S. Gehling, M. Hewitt, +21 authors Brian K. Albrecht
- Medicine, Biology
- ACS medicinal chemistry letters
- 26 July 2013
The identification of a novel series of small molecule BET inhibitors is described. Using crystallographic binding modes of an amino-isoxazole fragment and known BET inhibitors, a structure-based… Expand