Efficient Syntheses of Benzothiazepines as Antagonists for the Mitochondrial Sodium-Calcium Exchanger: Potential Therapeutics for Type II Diabetes was written by Pei, Yazhong;Lilly, Michael J.;Owen, David J.;D’Souza, Lawrence J.;Tang, Xiao-Qing;Yu, Jinghua;Nazarbaghi, Ramina;Hunter, Andrew;Anderson, Christen M.;Glasco, Susan;Ede, Nicholas J.;James, Ian W.;Maitra, Uday;Chandrasekaran, S.;Moos, Walter H.;Ghosh, Soumitra S.. And the article was included in Journal of Organic Chemistry in 2003.Computed Properties of C11H14ClNO2 This article mentions the following:
Type II diabetes mellitus is a chronic metabolic disorder that can lead to serious cardiovascular, renal, neurol., and retinal complications. While several drugs are currently prescribed to treat type II diabetes, their efficacy is limited by mechanism-related side effects (weight gain, hypoglycemia, gastrointestinal distress), inadequate efficacy for use as monotherapy, and the development of tolerance to the agents. Consequently, combination therapies are frequently employed to effectively regulate blood glucose levels. We have focused on the mitochondrial sodium-calcium exchanger (mNCE) as a novel target for diabetes drug discovery. We have proposed that inhibition of the mNCE can be used to regulate calcium flux across the mitochondrial membrane, thereby enhancing mitochondrial oxidative metabolism, which in turn enhances glucose-stimulated insulin secretion (GSIS) in the pancreatic 尾-cell. In this paper, we report the facile synthesis of benzothiazepines, e.g., I, and derivatives by S-alkylation using 2-aminobenzhydrols. The syntheses of other bicyclic analogs based on benzothiazepine, benzothiazecine, benzodiazecine, and benzodiazepine templates are also described. These compounds have been evaluated for their inhibition of mNCE activity, and the results from the structure-activity relationship (SAR) studies are discussed. In the experiment, the researchers used many compounds, for example, tert-Butyl (4-chlorophenyl)carbamate (cas: 18437-66-6Computed Properties of C11H14ClNO2).
tert-Butyl (4-chlorophenyl)carbamate (cas: 18437-66-6) belongs to organic chlorides. Organochlorines are organic compounds having multiple chlorine atoms. They were the first synthetic pesticides that were used in agriculture. They are resistant to most microbial and chemical degradations.While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available. Alkyl chlorides readily undergo attack by nucleophiles.Computed Properties of C11H14ClNO2
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics