2016 April

Validation of a HPLC-MS/MS assay for the determination of total and unbound concentration of temocillin in human serum

Validation of a HPLC-MS/MS assay for the determination of total and unbound concentration of temocillin in human serum

Temocillin is a β-lactam antibiotic active against gram-negative bacteria, including β-lactamase producers. It is currently indicated for the treatment of septicemia, urinary tract infections, and lower respiratory tract infections. In […]

Enantioselective Synthesis of Janus Kinase Inhibitor INCB018424 via an Organocatalytic Aza-Michael Reaction

Enantioselective Synthesis of Janus Kinase Inhibitor INCB018424 via an Organocatalytic Aza-Michael Reaction

Janus kinases (JAKs) are crucial signal transducers for a variety of cytokines, growth factors, and interferons. Inhibition of JAKs has advanced the basic and clinical studies of tyrosine kinase inhibitors […]

Peri- and Postnatal Developmental Toxicity of Salcaprozate Sodium (SNAC) in Sprague-Dawley Rats

Peri- and Postnatal Developmental Toxicity of Salcaprozate Sodium (SNAC) in Sprague-Dawley Rats

Salcaprozate sodium (SNAC) (sodium 8-((2-hydroxybenzoyl)amino) octanoate, CAS RN 203787-91-1) is classified as an oral absorption promoter. Although several clinical investigations have explored the potential therapeutic applications of Salcaprozate sodium (SNAC) as […]

Comparison of the Effects of Omapatrilat and Lisinopril on Circulating Neurohormones and Cytokines in Patients With Chronic Heart Failure

Comparison of the Effects of Omapatrilat and Lisinopril on Circulating Neurohormones and Cytokines in Patients With Chronic Heart Failure

A number of endogenous systems exist to counter the effects of vasoconstricting neurohormones that are increased in congestive heart failure (CHF). These include natriuretic peptides, nitric oxide, and prostaglandins. A […]

Labeled oxazaphosphorines for applications in mass spectrometry studies. 2. Synthesis of deuterium-labeled 2-dechloroethylcyclo-phosphamides and 2- and 3-dechloroethylifosfamides

Labeled oxazaphosphorines for applications in mass spectrometry studies. 2. Synthesis of deuterium-labeled 2-dechloroethylcyclo-phosphamides and 2- and 3-dechloroethylifosfamides

The prodrugs cyclophosphamide (CP) and ifosfamide (IF) each metabolize to an active alkylating agent through a cytochrome P450-mediated oxidation at the C-4 position. Competing with this activation pathway are enzymatic […]

Celastrol supports survival of retinal ganglion cells injured by optic nerve crush

Celastrol supports survival of retinal ganglion cells injured by optic nerve crush

Celastrol, a quinine methide triterpene extracted from the perennial vine Tripterygium wilfordii (Celastraceae), has been used in traditional Chinese medicine as a natural remedy for inflammation and a variety of […]

Total Synthesis of Distamycin A and 2640 Analogues: A Solution-Phase Combinatorial Approach to the Discovery of New, Bioactive DNA Binding Agents and Development of a Rapid, High-Throughput Screen for Determining Relative DNA Binding Affinity or DNA Binding Sequence Selectivity

Total Synthesis of Distamycin A and 2640 Analogues: A Solution-Phase Combinatorial Approach to the Discovery of New, Bioactive DNA Binding Agents and Development of a Rapid, High-Throughput Screen for Determining Relative DNA Binding Affinity or DNA Binding Sequence Selectivity

The regulation of gene expression is based on the sequence selective recognition of nucleic acids by a host of repressor, activator, and enhancer proteins. Selective external disruption or control of […]

Stereoselective synthesis of nicotinamide β-riboside and nucleoside analogs

Stereoselective synthesis of nicotinamide β-riboside and nucleoside analogs

Nicotinamide riboside (β-NAR) is an intermediate in one biosynthetic pathway by which nicotinamide is converted into NAD. In fact, nicotinamide or nicotinamide riboside derived from degradation of NAD can be […]

Application of a coupled enzyme assay to characterize nicotinamide riboside kinases

Application of a coupled enzyme assay to characterize nicotinamide riboside kinases

Nicotinamide adenine dinucleotide (NAD) has versatile functions in all cells. Besides its involvement in energy metabolism it serves important functions as substrate in a variety of cellular signaling reactions.  Although […]

Electroanalytical  and  isothermal  calorimetric  study  of  As(III) complexation  by the metal  poisoning  remediators,  2,3-dimercapto-1-propanesulfonate  and meso-2,3-dimercaptosuccinic acid

Electroanalytical and isothermal calorimetric study of As(III) complexation by the metal poisoning remediators, 2,3-dimercapto-1-propanesulfonate and meso-2,3-dimercaptosuccinic acid

Arsenic toxicity and its association with human diseases such as blackfoot disease, diabetes, hypertension and some kinds of cancers have been widely considered in the literature.  It  is  well known […]