As part of an on-going lead optimisation effort, a cross screening exercise identified an aryl sulphonyl amide hit that was optimised to afford a highly potent series of ghrelin receptor agonists.
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http://dx.doi.org/10.1016/j.bmcl.2008.12.042 | DOI Listing |
Eur J Med Chem
December 2024
Department of Natural Products and Medicinal Chemistry, CSIR-IICT Hyderabad, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, 201002, India. Electronic address:
Investigations into fruit and vegetable processing residues (FVPRs) offer huge opportunities to discover novel therapeutics against many diseases. In this study, detailed investigation of Garcinia mangostana fruit peel extract led to the isolation and identification of ten known compounds (1-10). Further, a new series of α-mangostin derived sulphonyl piperzines, aryl alkynes and 1,2,3-triazole derivatives were synthesized using Huisgen 1,3-dipolar cyclo-addition reaction ("click" chemistry).
View Article and Find Full Text PDFJ Enzyme Inhib Med Chem
December 2024
Faculty of Pharmacy, Universiti Teknologi MARA (UiTM), Kampus, Malaysia.
Quinoxalines are benzopyrazine derivatives with significant therapeutic impact in the pharmaceutical industry. They proved to be useful against inflammation, bacterial, fungal, viral infection, diabetes and other applications. Very recently, in January 2024, the FDA approved new quinoxaline containing drug, erdafitinib for treatment of certain carcinomas.
View Article and Find Full Text PDFSAR QSAR Environ Res
August 2024
Natural Science Laboratory, Division of Medicinal and Pharmaceutical Chemistry, Department of Pharmaceutical Technology, Jadavpur University, Kolkata, India.
MMP-2 overexpression is strongly related to several diseases including cancer. However, none of the MMP-2 inhibitors have been marketed as drug candidates due to various adverse effects. Here, a set of sulphonyl pyrrolidines was subjected to validation of molecular modelling followed by binding mode analysis to explore the crucial structural features required for the discovery of promising MMP-2 inhibitors.
View Article and Find Full Text PDFOrg Lett
March 2023
College of Science, China Agricultural University, 2 West Yuanmingyuan Road, Beijing 100193, China.
N-Functionalized C-fluoroalkyl amidines are attracting great attention due to their potential in pharmaceuticals. Herein, we report a Pd-catalyzed tandem reaction of azide with isonitrile and fluoroalkylsilane via a carbodiimide intermediate, providing facile access to N-functionalized C-fluoroalkyl amidines. This protocol offers an approach toward not only N-sulphonyl, N-phosphoryl, N-acyl, and N-aryl but also C-CF, CF, and CFH amidines with a broad substrate scope.
View Article and Find Full Text PDFPolymers (Basel)
July 2022
Faculty of Medical Dentistry, "Apollonia" University of Iasi, 700511 Iasi, Romania.
Bacterial oral diseases are chronic, and, therefore, require appropriate treatment, which involves various forms of administration and dosing of the drug. However, multimicrobial resistance is an increasing issue, which affects the global health system. In the present study, a commercial amphiphilic copolymer, Pluronic F127, was used for the encapsulation of 1-(5'-nitrobenzimidazole-2'-yl-sulphonyl-acetyl)-4-aryl-thiosemicarbazide, which is an original active pharmaceutical ingredient (API) previously synthesized and characterized by our group, at different copolymer/API weight ratios.
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