An oxidative photocyclisation of -arylenaminones to indoles is described, that mirrors the Fischer indole synthesis but uses anilines in place of arylhydrazines. Its value is exemplified with new approaches to the WHO-listed APIs ondansetron and alosetron.
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Functional bowel disorders with diarrhoea: Clinical guidelines of the United European Gastroenterology and European Society for Neurogastroenterology and Motility.
United European Gastroenterol J
July 2022
Division of Internal Medicine, IRCCS Azienda Ospedaliero-Universitaria di Bologna, Bologna, Italy.
Irritable bowel syndrome with diarrhoea (IBS-D) and functional diarrhoea (FDr) are the two major functional bowel disorders characterized by diarrhoea. In spite of their high prevalence, IBS-D and FDr are associated with major uncertainties, especially regarding their optimal diagnostic work-up and management. A Delphi consensus was performed with experts from 10 European countries who conducted a literature summary and voting process on 31 statements.
View Article and Find Full Text PDFNew approaches to ondansetron and alosetron inspire a versatile, flow photochemical method for indole synthesis.
Chem Commun (Camb)
January 2022
Chemistry, University of Southampton, Highfield, Southampton, SO17 1BJ, UK.
An oxidative photocyclisation of -arylenaminones to indoles is described, that mirrors the Fischer indole synthesis but uses anilines in place of arylhydrazines. Its value is exemplified with new approaches to the WHO-listed APIs ondansetron and alosetron.
View Article and Find Full Text PDFComparative effectiveness of 5-hydroxytryptamine 3 receptor antagonists in irritable bowel syndrome: a network meta-analysis of randomized controlled studies.
Ann Gastroenterol
April 2021
Tel Aviv University, Ministry of Health, Israel (Yaron Niv).
Background: There is evidence demonstrating the beneficial effects of 5-hydroxytryptamine 3 receptor antagonists (5-HT) for the treatment of non-constipated irritable bowel syndrome (NC-IBS). We aimed to determine the comparative effectiveness of 5-HT antagonists in NC-IBS, as evidenced by the results of a network meta-analysis (NWM) of published relevant randomized controlled trials (RCTs).
Methods: We searched the PubMed/Medline, EMBASE, and Cochrane Library databases for relevant RCTs through September 2020 and data from each selected RCT were extracted.
High-resolution structures of multiple 5-HTR-setron complexes reveal a novel mechanism of competitive inhibition.
Elife
October 2020
Department of Physiology and Biophysics, Case Western Reserve University, Cleveland, United States.
Serotonin receptors (5-HTR) play a crucial role in regulating gut movement, and are the principal target of setrons, a class of high-affinity competitive antagonists, used in the management of nausea and vomiting associated with radiation and chemotherapies. Structural insights into setron-binding poses and their inhibitory mechanisms are just beginning to emerge. Here, we present high-resolution cryo-EM structures of full-length 5-HTR in complex with palonosetron, ondansetron, and alosetron.
View Article and Find Full Text PDFBest management of irritable bowel syndrome.
Frontline Gastroenterol
May 2020
Leeds Gastroenterology Institute, St. James's University Hospital, Leeds, West Yorkshire, UK.
Irritable bowel syndrome (IBS) is a common disorder of gut-brain interaction which can have a considerable impact on quality of life. Following diagnosis, timely and evidence-based management is vital to the care of patients with IBS, aiming to improve outcomes, and enhance patient satisfaction. Good communication is paramount, and clinicians should provide a clear explanation about the disorder, with a focus on exploring the patient's own beliefs about IBS, and a discussion of any concerns they may have.
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