Drug Discovery

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 […]

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 […]

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 […]

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 […]

Design and Synthesisof Gramicidin S Analogs with High Antibiotic Activity

Design and Synthesisof Gramicidin S Analogs with High Antibiotic Activity

N-(2,4-Dinitrophenyl)tetrapeptide p-nitroanilides (Dnp-tetra-peptide-pNA) exhibit characteristic CD spectra when they take on β-turn conformation. Exciton coupling of electric transition dipoles of the two chromophores is thought to be the origin of […]

Low-dose ribavirin potentiates the antiviral activity of favipiravir against hemorrhagic fever viruses

Low-dose ribavirin potentiates the antiviral activity of favipiravir against hemorrhagic fever viruses

Favipiravir (T-705) is a nucleoside analog that was recently approved as an anti-influenza drug in Japan, and is in Phase 3 clinical trials in the USA for the same indication. […]