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Biotransformation of Xenobiotics in Living Systems—Metabolism of Drugs: Partnership of Liver and Gut Microflora
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2020
The intestinal microfora plays a role in the reduction of some drugs which contain the sulfoxide groups such as non-steroidal anti-inflammatory drugs, sulindac and sulfinpyrazone, catalyzing their conversion to respective sulfite metabolites with increased activity compared to parent drugs (Strong et al., 1987). The activation of sulindac (sulfoxide) to a non-selective COX inhibitor sulindac sulfide, which is responsible for the anti-inflammatory properties of sulindac, by anaerobic intestinal bacteria (Gurpinar et al., 2013), is presented in Fig. 6.23.Bacterial reduction of sulindac to active metabolite sulindac oxide.
Composition of Proprietary Products Approved in the United States
Published in Sarfaraz K. Niazi, Handbook of Pharmaceutical Manufacturing Formulations, Third Edition, 2019
CLINORIL (Sulindac) is available in 150 and 200 mg tablets for oral administration. Each tablet contains the following inactive ingredients: cellulose, magnesium stearate, and starch. Sulindac is a nonsteroidal, anti-inflammatory indene derivative.
The generation and reactions of sulfenate anions. An update
Published in Journal of Sulfur Chemistry, 2022
Adam B. Riddell, Matthew R. A. Smith, Adrian L. Schwan
Contained within the 96 alkyl aryl sulfoxides synthesized are a vast array of well tolerated functional groups and aryl groups derived from chiral sources such as menthol, cholesterol and glucose [56]. In addition to these, Zhang and coworkers [56] synthesized enantioenriched aryl alkyl sulfoxides from the aryl chloride pharmaceuticals fenofibrate and clofibrate as well as sulfoxide 39, a precursor to (R)-Sulindac, a nonsteroidal anti-inflammatory drug, in a 93% e.e (Scheme 24c) [56]. This contribution is, to date, the premier example of palladium catalyzed arylation of sulfenates due to the extensive product list, high yields and e.e.’s, universal nature in terms of function group tolerance, and applicability to both alkyl or aryl sulfenate anions [56].