China
Africa
Explore chapters and articles related to this topic
Synthesis of Important Chiral Building Blocks for Pharmaceuticals Using Lactobacillus and Rhodococcus Alcohol Dehydrogenases
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
Marion Rauter, Simon Krebs, Gotthard Kunze
Most processes described here gave high conversions of >90% and ee of >99% for the synthesis of 1-phenylethanol and its derivative 1-(S)-[3′,5′-bis(trifluoro-methyl)-phenyl]ethanol, which is necessary for an economic process. Obviously, in many cases additional investigations could increase yields further. Different reactor designs as well as alternative cofactor regeneration procedures can be used for more efficient synthesis processes. The transfer of these process designs to other substrates is possible but has to be deliberated in detail, because substrate solubility and stability of the biocatalysts differ.
Metabolic and Metabolomic Effects of Metformin in Murine Model of Pulmonary Adenoma Formation
Published in Nutrition and Cancer, 2023
Andrew C. Elton, Vannesa Cedarstrom, Arman Quraishi, Beverly Wuertz, Kevin Murray, Todd W. Markowski, Donna Seabloom, Frank G. Ondrey
Branched chain amino acid metabolism had three hits (L-Leucine, L-Isoleucine, L-Valine), and aromatic amino acid metabolism had two (L-Phenylalanine, L-Tyrosine). Glycerophospholipid metabolism had three hits (1-Acyl-sn-glycero-3-phosphocholine, Acetylcholine, sn-Glycero-3-phosphocholine). Lastly, pantothenate and coenzyme A biosynthesis had two hits (Pantothenate, L-Valine). The remaining metabolites were assigned though their associated pathways were not considered significant on ORA or were not assigned. The metabolites included: 3-Hydroxybutyric acid, 3-Hydroxybenzaldehyde, DL-Malic acid, p-Hydroxyphenyllactic acid, Indoxyl sulfate, 1,2-Diamino-2-methylpropane, Betaine, 2-Amino-1-phenylethanol, DL-Octopamine, 2-Aminoadipic acid, L-Citrulline, 8,11-Tridecadienoic acid, 13-(3-pentyl-2-oxiranyl)-, (8Z,11Z)-, LysoPC(14:0/0:0), LysoPC(P-18:0/0:0, LysoPC(18:1(9Z)/0:0), NG,NG-Dimethyl-L-arginine, ç-L-Glutamyl-L-alanine, N-L-ç-Glutamyl-L-leucine, L-Carnitine, L-Propionylcarnitine, 2-Methylbutyryl-L-carnitine, Creatine, and Uric acid. Some of these metabolites, particularly 2-aminoadipic acid and the carnitine derivatives, are associated with lysine degradation though were not included in the pathway hits, which may represent a limitation of the pathway analysis softwares (45, 46). Further studies may also investigate the lysophosphatidylcholine (LPC) derivatives, as they are associated with inflammation and the production of reactive oxygen species (47).
Pharmacokinetic study of Tangwang Mingmu granule for the management of diabetic retinopathy based on network pharmacology
Published in Pharmaceutical Biology, 2021
Yucheng Wang, Beibei Xue, Xiaoli Wang, Qilong Wang, Erwei Liu, Xiaopeng Chen
The extract of TWMM was analyzed using UPLC Q-Orbitrap MS/MS. The total ion current (TIC) chromatograms obtained in both positive and negative modes are shown in Figure 1. The 90 components can be divided into 8 classes: 27 flavonoids, 17 iridoids, 16 alkaloids, 10 triterpenoids, 9 phenols, 9 organic acids, 1 phenylethanol, and 1 anthraquinone. Twenty-six components were identified by matching retention times, quasi-molecular ions, and MS/MS fragments with the standards. The other 64 components were identified by comparing their retention times and MS/MS fragments with those reported in the literature and databases. As shown in Tables 3 and 4, a total of 38 compounds were identified in positive ion mode and 52 compounds in negative ion mode. As an example of the identification process, compound no. 23 with detected ions at m/z 321.0996 and 292.0969 could be identified as berberine by comparison with the standard. The fragment at m/z 321.0996 was generated by the loss of CH3, and m/z 292.0969 was obtained by further loss of HCO.
Recent progress in the development of β2 adrenergic receptor agonists: a patent review (2015-2020)
Published in Expert Opinion on Therapeutic Patents, 2021
Gang Xing, Ce Yi, Peiyuan Dou, Zhengxing Zhi, Bin Lin, Maosheng Cheng
Enormous effects have been invested to discover small-molecule β2AR agonists with novel structures and desirable potency. There are several common structural features for the β2AR agonists. They usually contain three parts in their structures: an aromatic head, an ethanolamine backbone, and an aromatic or aliphatic tail. One or two hydroxyl groups at proper positions of the aromatic head can form hydrogen bonds with the acceptor, which are necessary for β2AR activation. The ethanolamine backbone is indispensable for maintaining the activity so that the charged secondary amine group and the β-hydroxyl group furnish the agonists with the ability of hydrogen bonding and ionic interactions with the receptor. The activity is usually enantioselective: The R-configuration is more active than the S-configuration. The compounds bearing 2-amino-2-phenylethanol scaffold have been developed in contrast to traditional 2-amino-1-phenylethanol scaffold [55,56]. These compounds with 2-amino-2-phenylethanol fragment exhibited the excellent activity and high selectivity in the biological model tested. Novel synthetic β2AR agonists with catecholamine scaffold were reported to stimulate β2AR with high selectivity than β1AR. Several natural product compounds have been isolated and characterized using spectroscopic and chromatographic methods [49,51]. Although the activity and selectivity of the natural product is relatively weak compared with the marketed drugs, they provided novel scaffolds for further modification and optimization. In particular, compounds having both muscarinic receptor antagonist and a β2AR agonist activity represent a new trend in this area because they can act together in a synergistic fashion. As of now, there are few clinical studies available for compounds with dual muscarinic receptor antagonist and β2-AR agonist activities. More research needs to be done to evaluate the safety and effectiveness of such compounds.