6935-15-5Relevant articles and documents
Synthesis and hybrid sar property modeling of novel cholinesterase inhibitors?
Kos, Jiri,Kozik, Violetta,Pindjakova, Dominika,Jankech, Timotej,Smolinski, Adam,Stepankova, Sarka,Hosek, Jan,Oravec, Michal,Jampilek, Josef,Bak, Andrzej
, (2021)
A library of novel 4‐{[(benzyloxy)carbonyl]amino}‐2‐hydroxybenzoic acid amides was designed and synthesized in order to provide potential acetyl‐ and butyrylcholinesterase (AChE/BChE) inhibitors; the in vitro inhibitory profile and selectivity index were
Salicylic-acid derivatives as antennae for ratiometric luminescent probes based on lanthanide complexes
Terai, Takuya,Ito, Hiroki,Kikuchi, Kazuya,Nagano, Tetsuo
supporting information; experimental part, p. 7377 - 7381 (2012/07/30)
Long-lived ratiometric sensors: Luminescent lanthanide complexes are widely used in time-resolved assays of biomolecules, but most of the sensors with these complexes rely on single-point intensity measurements. Herein, we introduce a simple strategy to create ratiometric probes by using salicylic-acid derivatives as the antenna moiety of Tb3+ complexes. As an example, a probe for alkaline phosphatase (ALP) was developed (see scheme). Copyright
5′-O-[(N-acyl)sulfamoyl]adenosines as antitubercular agents that inhibit MbtA: An adenylation enzyme required for siderophore biosynthesis of the mycobactins
Qiao, Chunhua,Gupte, Amol,Boshoff, Helena I.,Wilson, Daniel J.,Bennett, Eric M.,Somu, Ravindranadh V.,Barry III, Clifton E.,Aldrich, Courtney C.
, p. 6080 - 6094 (2008/09/18)
A study of the structure - activity relationships of 5′-O-[N- (salicyl)sulfamoyl]adenosine (6), a potent inhibitor of the bifunctional enzyme salicyl-AMP ligase (MbtA, encoded by the gene Rv2384) in Mycobacterium tuberculosis, is described, targeting the salicyl moiety. A systematic series of analogues was prepared exploring the importance of substitution at the C-2 position revealing that a hydroxy group is required for optimal activity. Examination of a series of substituted salicyl derivatives indicated that substitution at C-4 was tolerated. Consequently, a series of analogues at this position provided 4-fluoro derivative, which displayed an impressive MIC 99 of 0.098 μM against whole-cell M. tuberculosis under iron-limiting conditions. Examination of other heterocyclic, cycloalkyl, alkyl, and aminoacyl replacements of the salicyl moiety demonstrated that these nonconserative modifications were poorly tolerated, a result consistent with the fairly strict substrate specificities of related non-ribosomal peptide synthetase adenylation enzymes.