Results 151 to 160 of about 110,887 (393)

Discovery of novel 1,3-diaryltriazene sulfonamides as carbonic anhydrase I, II, VII, and IX inhibitors

open access: yesJournal of Enzyme Inhibition and Medicinal Chemistry, 2018
A series of new 1,3-diaryltriazene sulfonamides was synthesised by reaction of diazonium salt of metanilamide (3-aminobenzene sulfonamide) with substituted aromatic amines. The obtained new compounds were assayed as inhibitors of four physiologically and
Suleyman Akocak   +3 more
semanticscholar   +1 more source

Small‐Molecule KRAS Inhibitors by Tyrosine Covalent Bond Formation

open access: yesChemMedChem, Accepted Article.
The development of the KRAS G12C inhibitor sotorasib was a major advance towards drugging KRAS. However, the G12C mutation is only found in about 10% of tumors with a KRAS mutation. KRAS tyrosine amino acids could provide alternative sites for covalent drug development.
Alexander Landgraf   +5 more
wiley   +1 more source

Peptide‐based covalent inhibitors of protein–protein interactions

open access: yesJournal of Peptide Science, Volume 29, Issue 1, January 2023., 2023
Peptide interaction motifs derived from a protein–protein interaction interface can serve as starting points for the development of inhibitors. However, for certain proteins when applying competitive inhibitors, peptide‐based ligands with an irreversible binding mode may be more active. This review summarizes examples of covalent inhibitors that employ
Felix M. Paulussen, Tom N. Grossmann
wiley   +1 more source

Designing Cyclic Nitrogen‐Bridged Sulfonamides with Anti‐Cancer Activity

open access: yesChemMedChem, EarlyView.
Nitrogen bridgehead compounds, especially cyclic sulfonamides, are an abundant motif in bioactive compounds. simple methods for the synthesis of nitrogen bridgehead sulfonamides is developed and their activity against cancer cell lines is explored. The N‐bridgehead heterocyclic structure is an abundant motif in a multitude of natural products.
Benedikt W. Grau   +4 more
wiley   +1 more source

Sulfa Allergy and Therapeutic Decisions

open access: yesSouthwest Respiratory and Critical Care Chronicles, 2013
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Kristen K Fuhrmann   +1 more
doaj  

A Novel Inhibitor against the Bromodomain Protein 1 of the Malaria Pathogen Plasmodium Falciparum

open access: yesChemMedChem, EarlyView.
This article presents the development of a first‐in‐class inhibitor targeting the bromodomain protein PfBDP1 in Plasmodium falciparum, the deadliest variant of the malaria‐causing Plasmodium parasites. Through structure‐based drug design, the inhibitor interactions were characterized via X‐ray crystallography and isothermal titration calorimetry ...
Marius Amann   +10 more
wiley   +1 more source

Emerg. Infect. Dis [PDF]

open access: yes, 2008
The multidrug-resistant (MDR) Salmonella enterica serotype Newport strain that produces CMY-2 β-lactamase(Newport MDR-AmpC) was the source of sporadic cases and outbreaks in humans in France during 2000–2005.
Achtman, M.   +13 more
core   +1 more source

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