Search results: Found 2

Listing 1 - 2 of 2
Sort by
Carbonic Anhydrases and Metabolism

Author:
ISBN: 9783038978008 9783038978015 Year: Pages: 184 DOI: 10.3390/books978-3-03897-801-5 Language: eng
Publisher: MDPI - Multidisciplinary Digital Publishing Institute
Subject: Science (General) --- Biology
Added to DOAB on : 2019-04-25 16:37:17
License:

Loading...
Export citation

Choose an application

Abstract

Carbonic anhydrases (CAs; EC 4.2.1.1) are metalloenzymes present in all kingdoms of life, as they equilibrate the reaction between three simple but essential chemical species: CO2, bicarbonate, and protons. Discovered more than 80 years ago, in 1933, these enzymes have been extensively investigated due to the biomedical application of their inhibitors, but also because they are an extraordinary example of convergent evolution, with seven genetically distinct CA families that evolved independently in Bacteria, Archaea, and Eukarya. CAs are also among the most efficient enzymes known in nature, due to the fact that the uncatalyzed hydration of CO2 is a very slow process and the physiological demands for its conversion to ionic, soluble species is very high. Inhibition of the CAs has pharmacological applications in many fields, such as antiglaucoma, anticonvulsant, antiobesity, and anticancer agents/diagnostic tools, but is also emerging for designing anti-infectives, i.e., antifungal, antibacterial, and antiprotozoan agents with a novel mechanism of action. Mitochondrial CAs are implicated in de novo lipogenesis, and thus selective inhibitors of such enzymes may be useful for the development of new antiobesity drugs. As tumor metabolism is diverse compared to that of normal cells, ultimately, relevant contributions on the role of the tumor-associated isoforms CA IX and XII in these phenomena have been published and the two isoforms have been validated as novel antitumor/antimetastatic drug targets, with antibodies and small-molecule inhibitors in various stages of clinical development. CAs also play a crucial role in other metabolic processes connected with urea biosynthesis, gluconeogenesis, and so on, since many carboxylation reactions catalyzed by acetyl-coenzyme A carboxylase or pyruvate carboxylase use bicarbonate, not CO2, as a substrate. In organisms other than mammals, e.g., plants, algae, and cyanobacteria, CAs are involved in photosynthesis, whereas in many parasites (fungi, protozoa), they are involved in the de novo synthesis of important metabolites (lipids, nucleic acids, etc.). The metabolic effects related to interference with CA activity, however, have been scarcely investigated. The present Special Issue of Metabolites aims to fill this gap by presenting the latest developments in the field of CAs and their role in metabolism.

Amide Bond Activation

Author:
ISBN: 9783039212033 / 9783039212040 Year: Pages: 466 DOI: 10.3390/books978-3-03921-204-0 Language: eng
Publisher: MDPI - Multidisciplinary Digital Publishing Institute
Subject: Science (General) --- Chemistry (General)
Added to DOAB on : 2019-08-28 11:21:27
License:

Loading...
Export citation

Choose an application

Abstract

The amide bond represents a privileged motif in chemistry. The recent years have witnessed an explosion of interest in the development of new chemical transformations of amides. These developments cover an impressive range of catalytic N–C bond activation in electrophilic, Lewis acid, radical, and nucleophilic reaction pathways, among other transformations. Equally relevant are structural and theoretical studies that provide the basis for chemoselective manipulation of amidic resonance. This monograph on amide bonds offers a broad survey of recent advances in activation of amides and addresses various approaches in the field.

Keywords

fumardiamide --- primaquine --- succindiamide --- Michael acceptor --- biofilm eradication --- antibacterial screening --- antiviral activity --- cytostatic activity --- N,N-dimethylformamide --- DMF --- N,N-dimethylacetamide --- DMAc --- amination --- amidation --- thioamidation --- formylation --- carbonylation --- cyanation --- insertion --- cyclization --- amide --- arynes --- insertion --- activation --- heterocycles --- organic synthesis --- multi-component coupling reaction --- aryl thioamides --- thiourea --- C-H/C-N activation --- C-S formation --- transition-metal-free --- rotational barrier energy --- amide bond --- nuclear magnetic resonance --- kinetic --- density functional theory --- non planar amide --- base-catalyed hydrolysis --- water solvation --- entropy --- transamidation --- amide --- amine --- catalyst --- catalysis --- acylative cross-coupling --- trialkylborane --- amide activation --- palladium --- N-heterocyclic carbene --- ruthenium (Ru) --- N-heterocyclic carbenes (NHCs) --- homogeneous catalysis --- in situ --- amide bonds --- synthesis --- density functional theory --- cis/trans isomerization --- secondary amides --- dipeptides --- steric effects --- tert-butyl --- additivity principle --- amino acid transporters --- amide bond --- gemcitabine prodrug --- metabolic stability --- pancreatic cancer cells --- pharmacokinetics --- peptide bond cleavage --- amide bond resonance --- twisted amides --- enzymes --- metal complexes --- catalysts --- amide C–N bond activation --- nickel catalysis --- amidation --- DFT study --- reaction thermodynamics --- amide resonance --- anomeric effect --- HERON reaction --- pyramidal amides --- physical organic chemistry --- reaction mechanism --- amide --- activation --- amidicity --- carbonylicity --- transamidation --- acyl transfer --- excited state --- Suzuki-Miyaura --- cross-coupling --- aryl esters --- C–O activation --- Pd-catalysis --- amides --- carbanions --- C–H acidity --- nitro-aci tautomerism --- molecular dynamics --- density-functional theory --- alkynes --- C–H bond cleavage --- C–N bond cleavage --- cyclopentadienyl complexes --- N-(1-naphthyl)acetamide --- rhodium --- [2+2+2] annulation --- amide bond --- sulfonamide bond --- alkynes --- addition reaction --- aminoacylation --- aminosulfonylation --- pre-catalysts --- palladium catalysis --- amide bond activation --- ester bond activation --- cross-coupling --- amide bond --- bridged lactams --- twisted amides --- amides --- Winkler-Dunitz parameters --- N–C activation --- hypersensitivity --- nitrogen heterocycles --- distortion --- bridged sultams --- amides --- C-N ? bond cleavage --- sodium --- crown ether --- amide hydrolysis --- model compound --- intramolecular catalysis --- twisted amide --- protease --- intein --- C-H functionalization --- directing groups --- amides --- transition metals --- catalysis

Listing 1 - 2 of 2
Sort by
Narrow your search

Publisher

MDPI - Multidisciplinary Digital Publishing Institute (2)


License

CC by-nc-nd (2)


Language

eng (2)


Year
From To Submit

2019 (2)

-->