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Cationic Surfactants and Quaternary Derivatives for Hair and Skin Care
Published in Randy Schueller, Perry Romanowski, Conditioning Agents for Hair and Skin, 2020
Matthew F. Jurczyk, David T. Floyd, Burghard H. Grüning
The number of radicals combined with the nitrogen atom determines the order of substitution. These designations are known as primary (mono-substituted), secondary (di-substituted), and tertiary (tri-substituted). Primary amines are also used as intermediates in the preparation of diamines (4).
Xenobiotic Biotransformation
Published in Robert G. Meeks, Steadman D. Harrison, Richard J. Bull, Hepatotoxicology, 2020
Xenobiotics or endogenous compounds containing amino, hydroxyl, or sulfhydryl groups are substrates for acetyltransferases [reviewed by King and Glowinski (1983) and Weber and Hein (1985)]. Amines, including aromatic and aliphatic primary amines, hydrazines, hydrazides, and sulfonamides, have been the most widely studied substrates. Endogenous substrates are 5-hydroxy-tryptamine and histamine. The enzymes are cytosolic and are present in several tissues; liver has the highest activity. Acetyl coenzyme A is the co-factor. The enzymes have been designated acetyl CoA: amine acetyl transferases. Sulfamethazine N-acetyltransferase is another term for the enzyme activity; sulfamethazine is the prototype substrate. The activity is characterized by polymorphism across many species, and individuals (or species and strains) are characterized as “slow” or “fast” acetylators. This polymorphism is determined by a single gene locus containing two co-dominant alleles: R = rapid, and r = slow. This polymorphism is an important determinant of susceptibility to toxicity and carcinogenicity of drugs (e.g., isoniazid) or xenobiotics, particularly aromatic amines, which are bioactivated or detoxified by acetylation.
Detection And Identification of Drugs of Dependence
Published in S.J. Mulé, Henry Brill, Chemical and Biological Aspects of Drug Dependence, 2019
Color reactions for this group of compounds primarily concern reactions associated with primary, secondary, and tertiary amines. It is possible through reaction of sympathomimetic amines44 with benzoyl chloride, p-nitrobenzoyl chloride, benzenesulphonyl chloride, picric acid, and ammonium reineckate to differentiate dexam-phetamine, amphetamine, methamphetamine, and ephedrine by color and microcrystal tests. A dark red color may be obtained45 when a sample solution in CC14 is treated with ethanolic quinhydrone, indicating a diamine. Primary amines give a gold color; secondary and tertiary amines do not react.
PDE1 inhibitors: a review of the recent patent literature (2008-present)
Published in Expert Opinion on Therapeutic Patents, 2022
Mei-Ling Le, Mei-Yan Jiang, Chuan Han, Yi-Yi Yang, Yinuo Wu
In 2015, Kehler and coworkers disclosed a series of PDE1 inhibitors with quinazoline scaffold (Figure 27). The X group on the quinazoline was a halogen atom in the first patent. The IC50 values of these compounds against PDE1 ranged from 7 nM to 2800 nM. Most compounds in this patent had two or more stereoisomers and one showed better inhibitory activities than others [79]. For the representative compound 86, stereoisomer 1 gave the IC50 value of 9.9 nM, while stereoisomer 2 gave the IC50 value of 65 nM against PDE1B. However, no configuration was provided for each stereoisomer. In another patent by Kehler, the X group on the quinazoline was instead by the methoxy group. The amine can be primary amine, secondary amine, or cyclic aliphatic amine [80]. The configuration had a significant impact on the inhibitory activities. For example, the (S)-87 was 30-fold more potent against PDE1B than (R)-87 [81].
Design, synthesis, HER2 inhibition and anticancer evaluation of new substituted 1,5-dihydro-4,1-benzoxazepines
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2021
Olga Cruz-López, Matilde Ner, Francho Nerín-Fonz, Yaiza Jiménez-Martínez, David Araripe, Juan A. Marchal, Houria Boulaiz, Hugo Gutiérrez-de-Terán, Joaquín M. Campos, Ana Conejo-García
Thus, we present here a new series of substituted 1,5-dihydro-4,1-benzoxazepines with the aim to develop antitumour agents. First, the methyl group was chosen to replace the nitro one of bozepinib in the present study. The different steps of the biotransformations that produce a primary amine from an aromatic nitro compound involve the nitro radical ion, the nitroso derivative, the nitroxyl radical, the hydroxylamine and then the primary amine. Each of these different intermediates could contribute to the toxicity14. Then, the substitution of the nitro (3, Figure 1) by a methyl group (7, Figure 1) eliminates the above-mentioned toxic metabolites. In addition, this methyl group may be oxidised to an alcohol and further to a carboxylic acid, favouring its elimination from the body.
Curcumin loaded poly (amidoamine) dendrimer-plamitic acid core-shell nanoparticles as anti-stress therapeutics
Published in Drug Development and Industrial Pharmacy, 2020
Pushpendra Kumar Tripathi, Shraddha Gupta, Suruchi Rai, Ankur Shrivatava, Shalini Tripathi, Sima Singh, Ajay J. Khopade, Prashant Kesharwani
The in vitro drug release estimation is essential for drug delivery, as the restricted release of a drug from its encapsulated materials will interfere with the drug bioavailability [46]. The drug release profile of sample batches was presented in Table 3. Figure 5 explains that initial burst release in the first 6 h followed by delayed-release after 24 h in all formulations. The formulations DCP 1 initially releases above 50% of drug and the later half-slowed up to 60% in 24 h shows retard the release of the hydrophobic drug. Drug attachment to the primary amines causes an early release of drug and the tertiary nitrogen within the dendritic cavities, which delayed the drug release. In formulation DCP 2, addition of fatty acid (palmitic acid) causes the increase in release of drug up to 60% in 6th hr and delayed-release for about 68% till 24 h. As the concentration of fatty acids increases the release decreases up to 53% in DCP 4 and 57% DCP 3.