Abstract

CCK1 antagonists: Design, Synthesis and Evaluation of N-Substituted Isobuyl-5-Hydroxy-5-Phenyl-Pyrrol-2- Ones as Adjunct to Opiates

Highlights

  • In terms of cholecystokinin-physiology, CCK8 is the most common peptide hormone, which is extensively found throughout the gastrointestinal tract and is widely distributed through the nervous system [1,2]

  • Cholecystokinin antagonists have been extensively investigated as potential drug targets [6]

  • 5-arylated dichloro-2(5H)-furanones A and B were synthesised from mucochloric acid (Figure 2), which is commercially available from furfural under oxidising conditions with hydrochloric acid

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Summary

Introduction

In terms of cholecystokinin-physiology, CCK8 is the most common peptide hormone, which is extensively found throughout the gastrointestinal tract and is widely distributed through the nervous system [1,2]. Cholecystokinin was discovered to cause contractions of the gallbladder [3]. It was rediscovered as pancreozymin, triggering the release of pancreatic enzymes. CCK-ligands, agonists and antagonists have been extensively investigated as potential drug molecules [5]. Cholecystokinin antagonists have been extensively investigated as potential drug targets [6]. They were studied as growth inhibitors in certain forms of cancer, as anxiolytics, in the treatment of schizophrenia and satiety [7,8,9,10]. Cholecystokin in does cause proliferation in colon- and pancreatic cancer cell lines and CCK-antagonists were studied as growth factor inhibitors in certain forms of cancer

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