Designing around structural alerts in drug discovery
AS Kalgutkar - Journal of Medicinal Chemistry, 2019 - ACS Publications
Cumulative research over several decades has implicated the involvement of reactive
metabolites in many idiosyncratic adverse drug reactions (IADRs). Consequently,“avoidance …
metabolites in many idiosyncratic adverse drug reactions (IADRs). Consequently,“avoidance …
Determination of cyanide in water and food samples using an efficient naphthalene-based ratiometric fluorescent probe
L Long, X Yuan, S Cao, Y Han, W Liu, Q Chen… - ACS …, 2019 - ACS Publications
Monitoring cyanide levels in water and food samples is crucial. Herein, we rationally
developed a simple and efficient fluorescent probe for cyanide determination. The probe …
developed a simple and efficient fluorescent probe for cyanide determination. The probe …
LC–MS-based metabolomics in the study of drug-induced liver injury
Y Lu, XM Zhao, Z Hu, L Wang, F Li - Current pharmacology reports, 2019 - Springer
Abstract Purpose of Review Metabolomics is the systematic and comparative study of the
levels of small-molecule metabolites in samples under various conditions. In biological …
levels of small-molecule metabolites in samples under various conditions. In biological …
Quantitative Evaluation of Reactivity and Toxicity of Acyl Glucuronides by [35S]Cysteine Trapping
H Harada, Y Toyoda, Y Abe, T Endo… - Chemical Research in …, 2019 - ACS Publications
Acyl glucuronides (AGs) are reactive metabolites of carboxylic acid-containing drugs, which
are associated with idiosyncratic toxicity (IDT) such as anaphylaxis, drug-induced liver …
are associated with idiosyncratic toxicity (IDT) such as anaphylaxis, drug-induced liver …
Time-dependent inhibition (TDI) of CYP1A2 by a CYP3A4-mediated reactive metabolite: proposal for a novel mechanism of irreversible TDI by a non-suicide substrate
H Nishimuta, K Sato, T Watanabe, M Yabuki - Xenobiotica, 2019 - Taylor & Francis
The purpose of this study was to clarify the mechanism of DSP-1053 time-dependent
inhibition (TDI) for CYP1A2. 2. DSP-1053 inhibited time-and concentration-dependently …
inhibition (TDI) for CYP1A2. 2. DSP-1053 inhibited time-and concentration-dependently …
Managing metabolic activation issues in drug discovery
S Kumar, K Mitra, TA Baillie - Handbook of Drug Metabolism, Third …, 2019 - taylorfrancis.com
The main objective of this chapter is to examine the kinetic differences between preformed
and generated metabolites and highlight potential complications associated with the …
and generated metabolites and highlight potential complications associated with the …
Selectivity and Mechanisms of Human Cytochrome P450 Inhibition by Chlormethiazole
RD Pelletier - 2019 - digital.lib.washington.edu
The cytochrome P450 (CYP) superfamily of enzymes are heme containing enzymes that
primarily perform oxidative reactions to a variety of substrates, including small molecule …
primarily perform oxidative reactions to a variety of substrates, including small molecule …
Managing Reactive Metabolites in Drug Discovery and Development
AS Kalgutkar - Handbook of Drug Metabolism, Third Edition, 2019 - taylorfrancis.com
The biotransformation of relatively innocuous chemicals to electrophilic reactive metabolites,
commonly referred to as bioactivation, is viewed as an unfavorable feature in drug …
commonly referred to as bioactivation, is viewed as an unfavorable feature in drug …
[PDF][PDF] 肝障害性薬物ビルダグリプチンのチオール基に対する共有結合性に関する研究
水野克彦 - 2019 - kanazawa-u.repo.nii.ac.jp
第 1 節 緒言 5 第 2 節 実験材料と実験方法 5 I-2-1 実験材料 5 I-2-2 求核試薬存在下における
安定性試験 5 I-2-3 HLM と HLC による M20. 7 生成活性の測定 8 I-2-4 高分解能 MS …
安定性試験 5 I-2-3 HLM と HLC による M20. 7 生成活性の測定 8 I-2-4 高分解能 MS …