Development of liquid chromatography tandem mass spectrometry method to quantify cyclobutane pyrimidine dimer photolyase activity by detection of 15mer oligonucleotide as reaction product

Development of liquid chromatography tandem mass spectrometry method to quantify cyclobutane pyrimidine dimer photolyase activity by detection of 15mer oligonucleotide as reaction product

Publication: J Chromatogr A
Software: ADMET Predictor®

Ultraviolet radiation from sunlight causes DNA damage in skin cells by formation of photoproducts, mainly cyclobutane pyrimidine dimers (CPD), which are reverted by exogenous CPD-photolyase, preventing photoaging and skin cancer.

A novel five‐step synthetic route to 1,3,4‐oxadiazole derivatives with potent α‐glucosidase inhibitory potential and their in silico studies

A novel five‐step synthetic route to 1,3,4‐oxadiazole derivatives with potent α‐glucosidase inhibitory potential and their in silico studies

Publication: Arch Pharm
Software: ADMET Predictor®

A series of new N‐aryl/aralkyl derivatives of 2‐methyl‐2‐{5‐(4‐chlorophenyl)‐1,3,4‐oxadiazole‐2ylthiol}acetamide were synthesized by successive conversions of ...

Utilizing the Combination of Binding Kinetics and Micro-Pharmacokinetics Link in Vitro α-Glucosidase Inhibition to in Vivo Target Occupancy

Utilizing the Combination of Binding Kinetics and Micro-Pharmacokinetics Link in Vitro α-Glucosidase Inhibition to in Vivo Target Occupancy

Publication: Biomolecules

Many compounds with good inhibitory activity (i.e., high affinity) within in vitro experiments failed in vivo studies due to a lack of efficacy from limited target occupancy (TO) in the drug discovery process.

Biopredictive in vitro testing methods to assess intestinal drug absorption from supersaturating dosage forms

Biopredictive in vitro testing methods to assess intestinal drug absorption from supersaturating dosage forms

Publication: J Drug Deliv Sci Technol
Software: GastroPlus®

The discovery pipelines in pharmaceutical companies are highly populated with poorly soluble compounds, demanding for an appropriate solution to overcome this problem.

Food ingredient safety evaluation: Utility and relevance of toxicokinetic methods

Food ingredient safety evaluation: Utility and relevance of toxicokinetic methods

Publication: Toxicol Appl Pharmacol
Software: GastroPlus®

The use of toxicokinetic (TK) data is becoming more prevalent in the evaluation of food ingredient safety as more TK information is being incorporated in safety data packages.

Prediction of pharmacokinetic drug-drug interactions causing atorvastatin-induced rhabdomyolysis using physiologically based pharmacokinetic modelling

Prediction of pharmacokinetic drug-drug interactions causing atorvastatin-induced rhabdomyolysis using physiologically based pharmacokinetic modelling

Publication: Biomed Pharmacother
Software: ADMET Predictor®

Atorvastatin and its lactone form metabolite are reported to be associated with statin-induced myopathy (SIM) such as myalgia and life-threatening rhabdomyolysis.

The solubility-absorption trade-off in using solubilizers: mechanistic PK simulations of progesterone with explicit cyclodextrin

The solubility-absorption trade-off in using solubilizers: mechanistic PK simulations of progesterone with explicit cyclodextrin

Conference: World Conference on Physico Chemical Methods in Drug Discovery and Development
Software: GastroPlus®
Division: PBPK

Cyclodextrins improve solubility of poorly soluble lipophilic drugs due to 1:1 complexation in their nonpolar interior cavity.

Design, synthesis, and biological activity of Plastoquinone analogs as a new class of anticancer agents

Design, synthesis, and biological activity of Plastoquinone analogs as a new class of anticancer agents

Publication: Bioorg Chem
Software: ADMET Predictor®

In this paper, based on Plastoquinone (PQ) analogs possessing substituted aniline containing alkoxy group(s), new 2,3-dimethyl-5-amino-1,4-benzoquinones (PQ1-15) were designed and synthesized in either two steps or one-pot reaction.

Phytochemicals as Lead Compounds for New Drug Discovery

Phytochemicals as Lead Compounds for New Drug Discovery

Publication: Elsevier
Software: ADMET Predictor®

Phytochemicals as Lead Compounds for New Drug Discovery presents complete coverage of the recent advances in the discovery of phytochemicals from medicinal plants as models to the development of new drugs and chemical entities.