CNT-Based Nano Medicine From Synthesis to Therapeutic Application

Carbon nanotubes (CNTs) are allotropes of carbon consisting of cylindrical tubes, made up of graphite with a diameter of several nm to a length of several mm. They had extraordinary structural, mechanical, and electronic properties due to their small size and mass, high mechanical resilience, and high electrical and thermal conductivity. Their large surface area made them applicable in pharmacy and medicine and adsorb or conjugate a broad variety of medical and diagnostic agents (drugs, genes, vaccines, antibodies, biosensors, etc.). They are often used to deliver drugs directly into the cells without going through the metabolic process of body. In addition to drug delivery and gene therapy, CNTs are also used for tissue regeneration, diagnostic biosensors, chiral drug enantiomer separation, drug extraction, and drug or pollutant analysis. CNTs have recently been discovered as effective antioxidants. The ADME and toxicity of different types of CNTs have also been documented here, as well as the prospects, advantages, and challenges of this promising bio-nano technology.

Transaminase Catalysis for Enantiopure Saturated Heterocycles as Potential Drug Scaffolds

As efforts in rational drug design are driving the pharmaceutical industry towards more complex molecules, the synthesis and production of these new drugs can benefit from new reaction routes. In addition to the introduction of new centers of asymmetry, complexity can be also increased by ring saturation, which also provides improved developability measures. Therefore, in this report, our aim was to develop transaminase (TA)-catalyzed asymmetric synthesis of a new group of potential chiral drug scaffolds comprising a saturated amine heterocycle backbone and an asymmetric primary amine sidechain (55a–g). We screened the Codex® Amine Transaminase Kit of 24 transaminases with the morpholine containing ketone 57a, resulting in one (R)-selective TA and three (S)-selective TAs operating at 100 mM substrate concentration and 25 v/v% isopropylamine (IPA) content. The optimized reaction conditions were than applied for asymmetric transamination of further six ketones (57b–g) containing various amine heterocycles, in which a strong effect of the substitution pattern of the γ-position relative to the substituted N-atom could be observed. Mediated by the most enantiotope selective (S)-TAs in scaled-up process, the (S)-amines [(S)-55a–g] were isolated with moderate-to-excellent yields (47–94%) in enantiopure form (>99% ee).

Recent advances in chiral analysis for biosamples in clinical research and forensic toxicology

This article covers current methods and applications in chiral analysis from 2010 to 2020 for biosamples in clinical research and forensic toxicology. Sample preparation for aqueous and solid biological samples prior to instrumental analysis were discussed in the article. GC, HPLC, capillary electrophoresis and sub/supercritical fluid chromatography provide the efficient tools for chiral drug analysis coupled to fluorescence, UV and MS detectors. The application of chiral analysis is discussed in the article, which involves differentiation between clinical use and drug abuse, pharmacokinetic studies, pharmacology/toxicology evaluations and chiral inversion. Typical chiral analytes, including amphetamines and their analogs, anesthetics, psychotropic drugs, β-blockers and some other chiral compounds, are also reviewed.