Drug Discovery

Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Pyrazinamide

Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Pyrazinamide

A biowaiver monograph of pyrazinamide based on literature data together with some additional experimental data is presented. The risks of basing a bioequivalence (BE) assessment on in vitro rather than […]

Screening strategies based on solubility and solution composition generate pharmaceutically acceptable cocrystals of carbamazepine

Screening strategies based on solubility and solution composition generate pharmaceutically acceptable cocrystals of carbamazepine

The study of carbamazepine solid forms continues to be a forum for advancing fundamental knowledge about polymorphism, hydrate formation, crystal engineering of pharmaceuticals, and structure–property relationships of pharmaceutical relevance. The […]

Progress in The Development of New Drugs in Alzheimer’s Disease

Progress in The Development of New Drugs in Alzheimer’s Disease

Alzheimer’s disease (AD) is an age-related neurodegenerative disease that is characterized by a progressive loss of memory associated with other cognitive sphere deficits interfering with social and occupational functioning. The […]

Roquinimex inhibits dextran sodium sulfate-induced murine colitis

Roquinimex inhibits dextran sodium sulfate-induced murine colitis

The majority of inflammatory bowel disease (IBD) consists of two related but clinically and histologically distinct conditions, ulcerative colitis and Crohn’s disease. Both conditions are characterized by chronically relapsing inflammation […]

Optimized Rhodamine B labeled mesoporous silica nanoparticles as fluorescent scaffolds for the immobilization of photosensitizers: a theranostic platform for optical imaging and photodynamic therapy

Optimized Rhodamine B labeled mesoporous silica nanoparticles as fluorescent scaffolds for the immobilization of photosensitizers: a theranostic platform for optical imaging and photodynamic therapy

Nanomaterials with easy surface functionalization and high biocompatibility have emerged as good candidates for theranostic applications. In particular the integration of multiple smart functions such as contrast agents (CA) and […]

Design, characterization and cellular uptake studies of fluorescence-labeled prototypic cathepsin inhibitors

Design, characterization and cellular uptake studies of fluorescence-labeled prototypic cathepsin inhibitors

The cathepsins comprise a family of lysosomal proteolytic enzymes. Eleven human cathepsins are cysteine proteases of the papain-like subfamily C1A and represent the best characterized group of cathepsins. Cysteine cathepsins […]

Perspectives on natural product epigenetic modulators in chemical biology and medicine

Perspectives on natural product epigenetic modulators in chemical biology and medicine

Epigenetic therapies from natural products in the clinic 1. Clinically approved natural product epigenetic modulators Despite an increasing number of synthetically-derived epigenetic modulators being taken into preclinical and clinical studies, […]

Synthesis, anticancer evaluation and docking study of vadimezan derivatives with carboxyl substitution

Synthesis, anticancer evaluation and docking study of vadimezan derivatives with carboxyl substitution

Xanthones with various substituents on the three-membered heterocyclic ring skeleton exhibit diverse biological activities, such as antihypertensive, antioxidative, antithrombotic and anticancer activities. Naturally existing xanthone analogues, including gentiakochianin, α-mangostin and […]

The use of environmental metrics to evaluate green chemistry improvements to the synthesis of (S,S)-reboxetine succinate

The use of environmental metrics to evaluate green chemistry improvements to the synthesis of (S,S)-reboxetine succinate

(±)-Reboxetine mesylate is a selective norepinephrine uptake (NRI) inhibitor which is marketed as the racemate, under the trade name EdronaxTM, for the treatment of depression, in more than 60 countries. […]

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 […]