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Chlorquinaldol
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Results of patch testing chlorquinaldol in consecutive patients (routine testing) and in groups of selected patients are shown in table 3.66.1. Routine testing in the USA yielded low prevalences of 0.3% and 0.4% of sensitization (2,3) and somewhat higher (1.1%) in Germany in the period 1972-1983 (19). Higher rates were – as expected – observed in patients patch tested for leg ulcers: 2.8% in 1970-1973 in Italy (5) and even 17% in 1976-1978 in Finland. In those days, hydroxyquinolines were widely used on leg ulcers and stasis dermatitis. Very likely, many of the observed reactions represent cross-reactions to clioquinol, which was far more used than chlorquinaldol.
HIV Integrase Inhibitors
Published in Satya Prakash Gupta, Cancer-Causing Viruses and Their Inhibitors, 2014
Serrao et al. (2013) used a fragment-based drug design approach to develop a series of 8-hydroxyquinoline derivatives that are the part of several FDA-approved drugs. Over the past decade, several quinoline-related scaffolds have been explored for the development of IN inhibitors. Modifications at the C-5 position yielded potent inhibitors with high potency and low cytotoxicity. The lead compounds of this series were reported to be drug-like, have low molecular weights, and were suitable for substituent modifications to enhance the potency and selectivity.
Synthesis and evaluation of a large library of nitroxoline derivatives as pancreatic cancer antiproliferative agents
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
Serena Veschi, Simone Carradori, Laura De Lellis, Rosalba Florio, Davide Brocco, Daniela Secci, Paolo Guglielmi, Mattia Spano, Anatoly P. Sobolev, Alessandro Cama
For these reasons, nitroxoline structure has prompted the Medicinal chemists to explore the structural requirements suitable to improve antitumor effects. In previous papers, taking advantage of the reactivity of the quinoline nucleus, most authors studied the introduction of halogens and additional side chains as well as modifications of the nitro group17,18. A limitation of most previous efforts was that they were directed towards the cathepsin B inhibitory activity, disregarding the other mechanisms of action demonstrated for nitroxoline as an anticancer compound so far. The aim of our study was the hitherto unexplored modification of the OH group. This could lead to a strong alteration of the chemical–physical characteristics of this 8-hydroxyquinoline. Indeed, this functional group endowed the chemical structure with a discrete acidity (reinforced by the p-NO2 moiety) and chelating ability. Furthermore, this phenolic compound is characterised by proton and electron-donating capacity and, as a consequence, antioxidant properties which can occur during several important biological processes19.
Efficacy and safety of intravenous belimumab in Japanese patients with systemic lupus erythematosus: A subgroup analysis of a phase 3 randomized placebo-controlled trial
Published in Modern Rheumatology, 2019
Yoshiya Tanaka, Damon Bass, Myron Chu, Sally Egginton, Beulah Ji, Herbert Struemper, David Roth
Of the 707 patients randomized to treatment in the overall trial, 60 patients were enrolled and randomized (belimumab, n = 39; placebo, n = 21) from study centers in Japan. The PK population comprised the 39 patients in the belimumab group. Overall, 48/60 (80.0%) patients completed the 52-week study (Figure 1(b)). Reasons for withdrawals were: AEs, n = 4 (6.7%); withdrawal by patient, n = 4 (6.7%); lack of efficacy, n = 3 (5%); and withdrawal by investigator decision, n = 1 (1.7%). Demographic and baseline disease characteristics were similar between treatment groups (Table 1). Patients across both groups were all taking concomitant steroid medication and the majority was taking concomitant immunosuppressive/immunomodulatory agents (belimumab, 69.2%; placebo, 90.5%). It should be noted that hydroxyquinoline was not available in Japan at the time of the study.
Tetralone derivatives are MIF tautomerase inhibitors and attenuate macrophage activation and amplify the hypothermic response in endotoxemic mice
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2021
János Garai, Marcell Krekó, László Őrfi, Péter Balázs Jakus, Zoltán Rumbus, Patrik Kéringer, András Garami, Eszter Vámos, Dominika Kovács, Viola Bagóné Vántus, Balázs Radnai, Tamás Lóránd
As regards the mechanism of action of the test compounds, we suppose, similarly to other authors, the importance of the N-terminal proline. The role of this basic amino acid in the mechanism of MIF was discussed by some researchers75. Mc Lean et al. studied hydroxyquinoline derivatives as efficient MIF inhibitors76. Applying crystallographic methods they were able to detect the covalent adduct formed in the reaction of Pro1 and an intermediate unsaturated ketone (“quinone methide”). Similar observations were made by Orita et al. also using hydroxyquinolines25.