1513-45-7Relevant academic research and scientific papers
Electrochemically generatedN-iodoaminium species as key intermediates for selective methyl sulphonylimination of tertiary amines
Huang, Binbin,Yang, Chao,Zhou, Jia,Xia, Wujiong
, p. 5010 - 5013 (2020)
Reported herein is a straightforward protocol for approachingN-sulphonylamidinesviaan electricity-driven, iodine-mediated cross dehydrogenative condensation (CDC) between sulphonamides and tertiary amines, which features exclusive N-CH3selectivity for the amine partners. Mechanistic studies indicate that anin situgeneratedN-iodoaminium species serves as the key intermediate.
Rationally Designed Polypharmacology: α-Helix Mimetics as Dual Inhibitors of the Oncoproteins Mcl-1 and HDM2
Conlon, Ivie L.,Drennen, Brandon,Lanning, Maryanna E.,Hughes, Samuel,Rothhaas, Rebecca,Wilder, Paul T.,MacKerell, Alexander D.,Fletcher, Steven
supporting information, p. 1691 - 1698 (2020/07/04)
Protein–protein interactions (PPIs), many of which are dominated by α-helical recognition domains, play key roles in many essential cellular processes, and the dysregulation of these interactions can cause detrimental effects. For instance, aberrant PPIs involving the Bcl-2 protein family can lead to several diseases including cancer, neurodegenerative diseases, and diabetes. Interactions between Bcl-2 pro-life proteins, such as Mcl-1, and pro-death proteins, such as Bim, regulate the intrinsic pathway of apoptosis. p53, a tumor-suppressor protein, also has a pivotal role in apoptosis and is negatively regulated by its E3 ubiquitin ligase HDM2. Both Mcl-1 and HDM2 are upregulated in numerous cancers, and, interestingly, there is crosstalk between both protein pathways. Recently, synergy has been observed between Mcl-1 and HDM2 inhibitors. Towards the development of new anticancer drugs, we herein describe a polypharmacology approach for the dual inhibition of Mcl-1 and HDM2 by employing three densely functionalized isoxazoles, pyrazoles, and thiazoles as mimetics of key α-helical domains of their partner proteins.
N-acyl sulfamide FBPase inhibitor, preparation method thereof, drug composition and application
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Paragraph 2501; 2503; 2504, (2017/09/08)
The invention discloses an N-acryl sulfamide FBPase inhibitor of a novel structure, and a preparation method thereof, a drug composition and an application, and particularly relates to an N-acryl sulfamide FBPase inhibitor shown in the formula I, a salt thereof for medicine, a preparation method, a composition comprising one or more compounds, an application of the compound in preparing the FBPase inhibitor or a drug for treating FBPase-related diseases, and an application in preparing a drug for preventing and/or treating diabetes. The formula is shown in the description.
Design and synthesis of triazolopyrimidine acylsulfonamides as novel anti-mycobacterial leads acting through inhibition of acetohydroxyacid synthase
Patil, Vikas,Kale, Manoj,Raichurkar, Anandkumar,Bhaskar, Brahatheeswaran,Prahlad, Dwarakanath,Balganesh, Meenakshi,Nandan, Santosh,Shahul Hameed
supporting information, p. 2222 - 2225 (2014/05/06)
Novel triazolopyrimidine acylsulfonamides class of antimycobacterial agents, which are mycobacterial acetohydroxyacid synthase (AHAS) inhibitors were designed by hybridization of known AHAS inhibitors such as sulfonyl urea and triazolopyrimidine sulfonamides. This Letter describes the synthesis and SAR studies of this class of molecules by variation of two parts of the molecule, the phenyl and triazolopyrimidine rings. SAR study describes optimisation of enzyme potency, whole cell potency and evidence of mechanism of action.
Sulfonamido- and sulfonamidocarbonylpyridine-2-carboxamides and their pyridine-n-oxides, process for their preparation and their use as pharmaceuticals
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, (2008/06/13)
The invention relates to sulfonamido- and sulfonamido-carbonylpyridine-2-carboxa of the formula I STR1 and their use as pharmaceuticals, in particular against fibrotic diseases.
Acylsulfonamido- and sulfonamidopyridine-2-carboxylic acid esters and their pyridine N-oxides, processes for their preparation and their use as medicaments
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, (2008/06/13)
The invention relates to acylsulfonamido- and sulfonamidopyridine-2-carboxylic acid esters and their pyridine N-oxides of the formula I STR1 in which ______________________________________A = R3 and B = X--NR5 R6 orB = R3 and A = X--NR5 R6.______________________________________ The compounds are suitable as medicaments against fibrotic diseases.
