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Synthetic Approaches to Inhibitors of Isoprenoid Biosynthesis
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
Pedro Merino, Loredana Maiuolo, Ignacio Delso, Vincenzo Algieri, Antonio De Nino, Tomas Tejero
Pamidronate (5), Alendronate (6), and neridronate (7) were prepared as mono- and diesters, starting from protected substrates on the amino group. Further deprotection was performed by using an excess of hydrazine in water at physiological pH (Guenin et al., 2007).
Molecular Aspects of the Activity and Inhibition of the FAD-Containing Monoamine Oxidases
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
The original discovery of the antidepressant effect of hydrazines came from the observation of mood elevation in tuberculosis patients treated with isoniazid. Hydrazines were then characterized as effective MAO inhibitors (Zeller et al., 1955). Both phenelzine and isocarboxazid carry the risk of liver toxicity but remain useful for treatment-resistant depression. The reversible inhibition of MAO by phenelzine is poor (Ki is 47 μM for MAO A, 15 μM for MAO B (Binda et al., 2008), as it is in rat and pig brain (Tipton and Spires, 1971). Inactivation requires that the hydrazine act first as a substrate. The normal product from the oxidation of the hydrazine is an imine that is hydrolysed to the aldehyde and released as usual with concomitant H2O2 production. Alternatively, the product could be a diazene that reacts with oxygen giving a radical that could alkylate the flavin. Inactivation of MAO A and of MAO B follows the same O2-dependent mechanism with some turnover for each inactivation event (the partition ratio). The kinetics of inactivation give kinact/Kinact equal to 18 min−1M−1 for MAO A and 3 min−1M−1 for MAO, B both with a partition ratio of turnover to inactivation of about 40 (Binda et al., 2008). The crystal structure shows that the adduct formed is at N5 of the FAD (Fig. 10.4).
Cancer
Published in Spyridon E. Kintzios, Maria G. Barberaki, Evangelia A. Flampouri, Plants That Fight Cancer, 2019
These include diverse, mostly controversial methods for treating cancer while avoiding the debilitating effects of conventional methods. The alternative treatment of cancer will probably gain in significance in the future, since it has been estimated that roughly half of all cancer patients currently turn to alternative medicine. The most prominent alternative cancer treatments include: The delivery of antineoplastons, peptides considered to inhibit tumor growth and first identified by Stanislaw Burzynski in blood and urine. According to the Food and Drug Administration (FDA) the drug can be applied only in experimental trials monitored by the agency and only on patients who have exhausted conventional therapies. However, the therapy has found a significant amount of political support, while attracting wide publicity.Hydrazine sulfate, a compound reversing cachexia of cancer patients, thus improving survival.Various herbal extracts, some of which are dealt with in this book.
Discovery of novel enasidenib analogues targeting inhibition of mutant isocitrate dehydrogenase 2 as antileukaemic agents
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
Ahmed F. Khalil, Tarek F. El-Moselhy, Eman A. El-Bastawissy, Rasha Abdelhady, Nancy S. Younis, Mervat H. El-Hamamsy
Target compounds, of series (I), 6a–l, and series (II), 7a–l were prepared as displayed in Scheme 1. The three chlorine atoms of cyanuric chloride, 1 disclosed diverse reactivity and can be substituted gradually at different temperatures38. Compounds 3a,b were prepared from cyanuric chloride 1via nucleophilic substitution of the first chlorine atom with morpholine, 2a or piperidine, 2b at 0–5 °C to afford analogues, 3a and 3b, respectively. Compounds 3a,b underwent nucleophilic substitution of the remaining two chlorine atoms with two hydrazine groups through heating under reflux with excess amount of hydrazine hydrate to provide the trisubstituted s-triazine derivatives, 4a,b, respectively. Condensation of hydrazine derivatives, 4a,b with various aldehydes yielded the corresponding hydrazones, 6a–l and 7a–l, respectively.
Bimetallic nickel-ferrite nanorod particles: greener synthesis using rosemary and its biomedical efficiency
Published in Artificial Cells, Nanomedicine, and Biotechnology, 2020
Hajar Q. Alijani, Shahram Pourseyedi, Masoud Torkzadeh-Mahani, Alexander Seifalian, Mehrdad Khatami
Nejati and Zabihi [34] were synthesised NiFe2O4 bimetallic NP by the hydrothermal method using Hydrazine hydrate. Hydrazine hydrate is toxic to humans [35]. Current mentioned chemical methods usually have disadvantages such as dependence on expensive equipment, high energy consumption and dependence on chemical compounds toxic to the environment and humans [36–43]. Therefore, finding simple, economical, inexpensive, non-toxic and environmentally friendly methods are very important and necessary for the synthesis of these types of NP. A method that can eliminate the need to use any harmful chemicals is shown in [44]. The methods that recently attracted the attention of scientists are synthesis of nanostructures using natural resources such as herbal, bacterial, fungal or their derivative (green methods). Compared with chemical synthesis methods, green methods have various important advantages, including facility, low external energy consumption, affordable, rapid synthesis process, non-toxicity, convenient one-step process and eco-friendly [45–49].
HPLC–UV assay for the evaluation of inhibitors of plasma amine oxidase using crude bovine plasma
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2019
Kira Mergemeier, Florian Galster, Matthias Lehr
2-(3-Phenylphenyl)acetohydrazide (18). Hydrazine monohydrate (273 mg, 5.45 mmol, 265 µL) was added to a solution of ethyl 2-(3-phenylphenyl)acetate34 (140 mg, 0.58 mmol) in ethanol (7 mL) and the mixture was heated to reflux for 42 h. Further amounts of hydrazine monohydrate were added after 19 h (273 mg, 5.45 mmol, 265 µL) and 27 h (273 mg, 5.45 mmol, 265 µL). After cooling the mixture to ambient temperature, the solvent was removed under reduced pressure. The crude product was treated with a small amount of ice-cold ethanol. The precipitate obtained was filtered off by suction and washed twice with ice-cold ethanol to give 18 as a white solid (39 mg, 29%). C14H14N2O (226.3); mp 126 °C; 1H-NMR (600 MHz, DMSO-d6): δ (ppm) 3.42 (s, 2H), 4.24 (s, 2H), 7.25 (dt, J = 7.7 Hz and 1.4 Hz, 1H), 7.35–7.40 (m, 2H), 7.45–7.49 (m, 2H), 7.51 (ddd, J = 7.7 Hz, 1.9 Hz and 1.1 Hz, 1H), 7.55 (t, J = 1.8 Hz, 1H), 7.61–7.64 (m, 2H), 9.23 (s, 1H); 13C-NMR (151 MHz, DMSO-d6): δ (ppm) 40.55, 124.78, 126.66, 127.42, 127.43, 128.03, 128.80, 128.92, 136.93, 140.14, 140.17, 169.51; HRMS (APCI, direct probe) m/z [M + H]+ calculated: 227,1179, found: 227,1163. Purity (HPLC) 99%.