Glycosylated neuropeptides: a new vista for neuropsychopharmacology?

…, M Dhanasekaran, CM Keyari - Medicinal research …, 2005 - Wiley Online Library
The application of endogenous neuropeptides (eg, enkephalins) as analgesics has been
retarded by their poor stability in vivo and by their inability to effectively penetrate the blood–…

Antinociceptive structure-activity studies with enkephalin-based opioid glycopeptides

…, E Navratilova, M Dhanasekaran, CM Keyari… - … of Pharmacology and …, 2004 - ASPET
Development of opioid peptides as therapeutic agents has historically been limited due to
pharmacokinetic issues including stability and blood-brain barrier (BBB) permeability. …

Glycosylation improves the central effects of DAMGO

JJ Lowery, L Yeomans, CM Keyari… - Chemical Biology & …, 2007 - Wiley Online Library
A series of μ‐agonist DAMGO analogs were synthesized and pharmacologically
characterized to test the ‘biousian’ hypothesis of membrane hopping. DAMGO was altered by …

Synthesis of new quinolinequinone derivatives and preliminary exploration of their cytotoxic properties

CM Keyari, AK Kearns, NS Duncan… - Journal of medicinal …, 2013 - ACS Publications
A series of 7-amino- and 7-acetamidoquinoline-5,8-diones with aryl substituents at the 2-position
were synthesized, characterized, and evaluated as potential NAD(P)H:quinone …

Biousian glycopeptides penetrate the blood–brain barrier

…, F Porreca, HI Yamamura, L Yeomans, CM Keyari… - Tetrahedron …, 2005 - Elsevier
Clinicians have long desired the ability to introduce either exogenous or endogenous
neuropeptides directly into the brain in order to alter brain chemistry, but have been thwarted by …

Glycopeptides related to β-endorphin adopt helical amphipathic conformations in the presence of lipid bilayers

…, I Alves, L Yeomans, CM Keyari… - Journal of the …, 2005 - ACS Publications
A series of glycosylated endorphin analogues designed to penetrate the blood−brain barrier
(BBB) have been studied by circular dichroism and by 2D-NMR in the presence of water; …

Serine and Threonine Schiff Base Esters React with β-Anomeric Peracetates in the Presence of BF3·Et2O to Produce β-Glycosides

CM Keyari, R Polt - Journal of Carbohydrate Chemistry, 2010 - Taylor & Francis
Improved procedures are reported for the glycosylation of L-serine and L-threonine utilizing
activated Schiff base glycosyl acceptors, which are less expensive and more efficient …

Asymmetric [C+ NC+ CC] coupling entry to the naphthyridinomycin natural product family: formal total synthesis of cyanocycline A and bioxalomycin β2

P Garner, HU Kaniskan, CM Keyari… - The Journal of Organic …, 2011 - ACS Publications
A full account of our [C + NC + CC] coupling approach to the naphthyridinomycin family of
natural products is presented, culminating in formal total syntheses of cyanocycline A and …

Development and characterization of novel and selective inhibitors of cytochrome P450 CYP26A1, the human liver retinoic acid hydroxylase

P Diaz, W Huang, CM Keyari, B Buttrick… - Journal of medicinal …, 2016 - ACS Publications
Cytochrome P450 CYP26 enzymes are responsible for all-trans-retinoic acid (atRA) clearance.
Inhibition of CYP26 enzymes will increase endogenous atRA concentrations and is an …

Suzuki–Miyaura cross-coupling of benzylic bromides under microwave conditions

SW McDaniel, CM Keyari, KC Rider, NR Natale… - Tetrahedron letters, 2011 - Elsevier
A procedure for benzylic Suzuki–Miyaura cross-coupling under microwave conditions has
been developed. These conditions allowed for heterocyclic compounds to be coupled. …