DBS sampling can be used to stabilize prodrugs in drug discovery rodent studies without the addition of esterase inhibitors
CJ D'Arienzo, QC Ji, L Discenza, G Cornelius… - Bioanalysis, 2010 - Future Science
Background: Prodrugs that exhibit ex vivo instability owing to high levels of esterases in
rodent blood, plasma and serum present challenges in the accurate determination of drug …
rodent blood, plasma and serum present challenges in the accurate determination of drug …
Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2, 4-dioxo-1, 2-dihydroquinazolin-3 (4 H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2, 3, 4, 9-tetrahydro-1 …
…, R Vickery, LN Discenza, CJ D'Arienzo… - Journal of medicinal …, 2016 - ACS Publications
Bruton's tyrosine kinase (BTK), a nonreceptor tyrosine kinase, is a member of the Tec family
of kinases. BTK plays an essential role in B cell receptor (BCR)-mediated signaling as well …
of kinases. BTK plays an essential role in B cell receptor (BCR)-mediated signaling as well …
Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl) …
…, Z Yang, LM Zadjura, CJ D'Arienzo… - Journal of medicinal …, 2009 - ACS Publications
Azaindole derivatives derived from the screening lead 1-(4-benzoylpiperazin-1-yl)-2-(1H-indol-3-yl)ethane-1,2-dione
(1) were prepared and characterized to assess their potential as …
(1) were prepared and characterized to assess their potential as …
Tandem optimization of target activity and elimination of mutagenic potential in a potent series of N-aryl bicyclic hydantoin-based selective androgen receptor …
…, R Golla, JE Kuhns, JA Lupisella, CJ Darienzo… - Bioorganic & medicinal …, 2007 - Elsevier
Pharmacokinetic studies in cynomolgus monkeys with a novel prototype selective androgen
receptor modulator revealed trace amounts of an aniline fragment released through …
receptor modulator revealed trace amounts of an aniline fragment released through …
Inhibitors of HIV-1 attachment. Part 7: indole-7-carboxamides as potent and orally bioavailable antiviral agents
…, H Fang, Z Yang, L Zadjura, CJ D'Arienzo… - Bioorganic & medicinal …, 2013 - Elsevier
A series of substituted carboxamides at the indole C7 position of the previously described 4-fluoro-substituted
indole HIV-1 attachment inhibitor 1 was synthesized and the SAR …
indole HIV-1 attachment inhibitor 1 was synthesized and the SAR …
(3R,5S,E)-7-(4-(4-Fluorophenyl)-6-isopropyl-2-(methyl(1-methyl-1H-1,2,4-triazol-5-yl)amino)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoic Acid (BMS-644950): A …
…, CA Cuff, T Harrity, CJ Darienzo… - Journal of medicinal …, 2008 - ACS Publications
3-Hydroxy-3-methylglutaryl coenzyme-A reductase (HMGR) inhibitors, more commonly known
as statins, represent the gold standard in treating hypercholesterolemia. Although statins …
as statins, represent the gold standard in treating hypercholesterolemia. Although statins …
Integrated quantitative and qualitative workflow for in vivo bioanalytical support in drug discovery using hybrid Q-TOF-MS
…, R Ramanathan, M Jemal, CJ D'Arienzo… - Bioanalysis, 2012 - Future Science
Background: UHPLC coupled with orthogonal acceleration hybrid quadrupole-TOF (Q-TOF)-MS
is an emerging technique offering new strategies for the efficient screening of new …
is an emerging technique offering new strategies for the efficient screening of new …
Periodic, partial inhibition of IκB kinase β-mediated signaling yields therapeutic benefit in preclinical models of rheumatoid arthritis
…, DW Kukral, J Strnad, KW McIntyre, CJ Darienzo… - … of Pharmacology and …, 2009 - ASPET
We have previously shown that inhibitors of IκB kinase β (IKKβ), including 4(2′-aminoethyl)amino-1,8-dimethylimidazo(1,2-a)quinoxaline
(BMS-345541), are efficacious against …
(BMS-345541), are efficacious against …
Inhibitors of HIV-1 attachment. Part 8: the effect of C7-heteroaryl substitution on the potency, and in vitro and in vivo profiles of indole-based inhibitors
…, B Pearce, Z Yang, L Zadjura, CJ D'Arienzo… - Bioorganic & medicinal …, 2013 - Elsevier
As part of the SAR profiling of the indole-oxoacetic piperazinyl benzamide class of HIV-1
attachment inhibitors, substitution at the C7 position of the lead 4-fluoroindole 2 with various 5- …
attachment inhibitors, substitution at the C7 position of the lead 4-fluoroindole 2 with various 5- …
Quantitation of therapeutic proteins following direct trypsin digestion of dried blood spot samples and detection by LC–MS-based bioanalytical methods in drug …
BG Sleczka, CJ D'Arienzo, AA Tymiak, TV Olah - Bioanalysis, 2012 - Future Science
Background: There is considerable interest in the pharmaceutical industry today in both
development of therapeutic proteins as viable biopharmaceutical agents as well as the …
development of therapeutic proteins as viable biopharmaceutical agents as well as the …