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Published in Anton Sebastian, A Dictionary of the History of Medicine, 2018
Anaphrodisiacs [Greek: a, without + phrodesia, venus] Medications and methods used to diminish sexual passion. Some used in the past include cold baths, ice, flagellation and warm underclothes. Bromide of potassium and ammonium, iodide of potassium, camphor, digitalis, purgatives, nauseates and bleeding were tried in the 19th century.
Novel 4-arylaminoquinazolines bearing N,N-diethyl(aminoethyl)amino moiety with antitumour activity as EGFRwt-TK inhibitor
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2019
Yaling Zhang, Li Chen, Xiabing Li, Li Gao, Yunxia Hao, Baolin Li, Yaping Yan
A mixture of 2-aminobenzonitrile (1) (0.02 mol) and ammonium iodide (0.02 mol) was dissolved in acetic acid (50 mL), stirred for 30 min at room temperature (r.t.), then 30% aqueous hydrogen peroxide solution (0.13 mol) was slowly added at r.t. and stirred for 12 h. After reaction completed, the reaction solution was treated with aqueous sodium thiosulphate solution 40 ml (0.03 mol) and basified to about pH to 8 by the addition of 20% sodium hydroxide. The reaction mixture was stirred at r.t. for 30 min. The desired product, which was partially precipitated during this step, was isolated by vacuum filtration to afford 2 as silvery white flake solid in 92.6% yield.
Benzimidazole derivatives endowed with potent antileishmanial activity
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2018
Michele Tonelli, Elena Gabriele, Francesca Piazza, Nicoletta Basilico, Silvia Parapini, Bruno Tasso, Roberta Loddo, Fabio Sparatore, Anna Sparatore
The mono-methylated benzimidazoles 2 and 7 were converted into the quaternary salts 4, 12 and 14 (Scheme 1), by heating them with propyl iodide or with benzyl chloride for the latter. As suggested by Howarth and Hanlon35 for analogous compounds, by treating the 2-pentadecyl benzimidazole with (ferrocenylmethyl)trimethyl ammonium iodide at r.t., the 1-ferrocenylmethylbenzimidazole 16 was obtained in high yield, the latter was then quaternised with methyl iodide to 17 (Scheme 3).