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The menopause
Published in Michael J. O’Dowd, The History of Medications for Women, 2020
Mrs Garrett Anderson (1907) held the opinion that ‘There seems to be no clear evidence that the ovaries form any internal secretion of great nutritive value. The disturbance seen at the menopause is nervous rather than nutritional or chemical’. The patient was advised that the organs of elimination must be kept well up to their work’. Warm bathing, flesh-glove rubbing, mild laxatives, an occasional blue pill (mercury) ‘and a little patience, are in ordinary cases all that is wanted ... When a stimulant is really indicated, quinine and strychnia with hydrobromic acid answer the purpose adequately. In cases of more severity ... mild purgation followed by a short course of Bromides and a fairly long one of Liq. Ferri. Perchlor., combined with Liq. Amm. Acet., will usually give quick relief. In climacteric melancholy good results seem to follow... from pil. Hydrar... a month at Buxton or any similar place, under conditions of absolute rest, is of the greatest value’.
Reactivities of Amino Acids and Proteins with Iodine
Published in Erwin Regoeczi, Iodine-Labeled Plasma Proteins, 2019
The reaction of tryptophan-containing peptides with iodine has been extensively studied by Alexander125,126 using a variety of iodinating agents, including lactoperoxidase, horse-radish peroxidase, IC1, chloramine-T, I2, and triiodide. He found that all these agents oxidize tryptophan over the pH range of 2 to 11. Moreover, peptide bonds involving the tryptophanyl carboxyl group are split too in acid media with a maximum at pH 5, though not in alkaline media. Chloramine-T also oxidizes tryptophan in the absence of iodide. The mechanism proposed by Alexander for these oxidative changes is similar to the one suggested by others to explain the action of brominating agents, such as N-bromosuccinimide,127,128 N-bromo- acetamide,127,128 2,4,6-tribromo-4-methyl-cyclohexadienone,129 or hydrobromic acid-di- methyl sulfoxide.130 The sequence of events is summarized in Figure 46, and it involves the action of three I equivalents (IC1 or I2). The first one forms an intermediate with C-2 and C-3 that is analogous to the hypothetical bromonium intermediate of Patchomik and colleagues127 (Structure C). The intermediate is hydrolyzed by H2O yielding HI and 2- hydroxytryptophan (Structure D). The second I equivalent oxidizes C-2 to yield oxindolyl- alanine (Structure E), and the third forms 5-iodooxindolylalanine (Structure F).
Technetium-Labeled Compounds
Published in Garimella V. S. Rayudu, Lelio G. Colombetti, Radiotracers for Medical Applications, 2019
Suresh C. Srivastava, Powell Richards
Tin metal can be dissolved in hydrochloric acid. Pure tin dissolves slowly in the dilute acid and much more rapidly in hot concentrated acid. Solution can also be effected using a 4:1 mixture of hydrobromic acid and bromine, hot concentrated sulfuric acid, hot concentrated hydrochloric acid plus 30% hydrogen peroxide, and aqua regia. In nitric acid, tin gets converted into β-stannic acid. Losses by volatilization occur when acid solutions are subjected to prolonged heating, especially if stannic halides are formed or present.
What is the gold standard model for Alzheimer’s disease drug discovery and development?
Published in Expert Opinion on Drug Discovery, 2021
Ramón Cacabelos, Iván Carrera, Olaia Martínez-Iglesias, Natalia Cacabelos, Vinogran Naidoo
Under the epigraph of mechanistic and procedural models (MPPs) we include a series of artificial models which attempt to mimic important aspects of the AD phenotype or are able to generate partial features of the AD-related pathogenic cascade. These models result from the neurotoxic, pharmacological, surgical or genetic manipulation of different animals or TMMs/TRMs. Some of them are age-related and/or reversible. The most important MPPs in AD research and drug development are the following: (i) neurotoxic models: cholinergic (chemical lesions of cholinergic nuclei with kainic acid, anisodine, hemicholine hydrobromic acid, ibotenic acid or immunotoxins; pharmacological inhibition of the cholinergic system with scopolamine and/or muscarinic or nicotinic inhibitors), amyloidogenic, formaldehyde, environmental toxicants and metals, Streptozotocin, and other pharmacological models (γ-Fluoromethylhistidine, 6-hydroxydopamine (6-OHDA), 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), 1-Methyl-4-phenylpyridinium (MPP+), paraquat, rotenone, and permethrin); (ii) neuroinflammation models; (iii) neurovascular models; (iv) neurometabolic models; (v) lipidomic models; (vi) Blood-Brain Barrier models; (vii) traumatic brain injury models; (viii) memory and behavioral models; (ix) Circadian and Sleep models; (x) microbiome models; (xi) senescence models; (xii) Autophagy models; and (xiii) Epigenetic models [10,16,43,92] (Table 3).
Structure activity evaluation and computational analysis identify potent, novel 3-benzylidene chroman-4-one analogs with anti-fungal, anti-oxidant, and anti-cancer activities
Published in Drug Development and Industrial Pharmacy, 2021
Gaffar Sarwar Zaman, Hossam Kamli, Suresh Radhakrishnan, Irfan Ahmad, Hassan Otifi, Mohamad Y. Alshahrani, Prasanna Rajagopalan
The series of 3-benzylidene chroman-4-ones (45e–64e) as shown in Figure 1 were synthesized in the laboratory. Synthesis of 3-benzylidene-6-(prop-2-enyl)-8-methoxy chroman-4-one was achieved starting from benzaldehyde and methyl acrylate. The synthesis of methyl-α-methylene-β-hydroxy-b-phenyl propanoate was achieved starting from benzaldehyde and methyl acrylate. Baylis-Hillman reaction, with DABCO as a catalyst, was carried out in solid phase using silica gel, in absence of any solvent. In general, Baylis-Hillman reaction was a slow reaction, requiring several days/weeks for completion, depending upon the reactivity or both activated alkenes and electrophile. The application of silica gel on solid phase medium was used for performing the Baylis-Hillman reaction particularly between tertiary-butyl acrylate and aromatic aldehydes under the influence of catalytic amount of DABCO (15 mol%) at increased the rates. The hydroxy propanoate was treated with hydrobromic acid with a catalytic amount of concentrated sulfuric acid at room temperature to give bromomethyl propionate. The bromomethyl propionate was treated with eugenol in presence of potassium carbonate in acetone to give methyl 3-aryl-2-(2-methoxy-4-prop-2-enyl) phenoxy ethyl prop-2-enoate. The ester was hydrolyzed by potassium hydroxide in an aqueous 1,4-dioxane at room temperature. The acid obtained by acidification of the compound is 3-aryl-2 [2-methoxy-4(prop-2-enyl)] phenoxy methyl prop-2-enoic acid. The propenoic acid was subjected to intra molecular Friedel–Crafts acylation by the action of TFAA in methylene dichloride to desired product.
Design, synthesis, and apoptosis-promoting effect evaluation of novel pyrazole with benzo[d]thiazole derivatives containing aminoguanidine units
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2019
Da Chuan Liu, Mei Jia Gao, Qiang Huo, Tao Ma, Ying Wang, Cheng Zhu Wu
A mixture of 6-methoxy-2, 3-dihydrobenzo[d]thiazol-2-amine (1) (10 g, 55.56 mmol) and 40 ml of hydrobromic acid (48% water solution) was refluxed at 126 °C for 20 h. The mixture was allowed to cool to room temperature and neutralised with NaOH solution to pH 7–8. Then, the precipitate was filtered and washed with water. The filtrate was stirred with 100 ml hot water for 0.5 h and the remaining precipitate was filtered to yield a brown solid, compound 2.