6398-74-9Relevant academic research and scientific papers
METHOD FOR PREPARING S-Bz-MAG3 AS A PRECURSOR OF CONTRAST MEDIA
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Paragraph 0053; 0054; 0055; 0056; 0057; 0058, (2019/04/25)
The present invention provides a method for preparing S-Bz-MAG3 as a precursor of contrast media. Thioglycolic acid and benzoyl chloride are taken for the thiol protection reaction. Next, N,N′-dicyclohexylcarbodiimide and N-hydroxysuccinimide are converte
Silica-promoted facile synthesis of thioesters and thioethers: A highly efficient, reusable and environmentally safe solid support
Basu, Basudeb,Paul, Susmita,Nanda, Ashis K.
experimental part, p. 767 - 771 (2010/09/05)
An efficient, mild and rapid procedure for the acylation and alkylation of aromatic and aliphatic thiols mediated on a silica gel surface at room temperature is described. The protocol allows the protection of thiols under neutral heterogeneous conditions without requiring any bases or Lewis acids, and the silica gel used as the promoter can be recycled for several runs without any loss of activity.
Synthesis and biological characterization of 99mTc(I) tricarbonyl cysteine complex, a potential diagnostic for assessment of renal function
Park, Sang Hyun,Jang, Beom Su,Park, Kyung Bae
, p. 63 - 73 (2007/10/03)
Cysteine containing three functional groups, i.e. a carboxyl, sulfhydryl, and amino group, has been labelled with 99mTc(I) tricarbonyl precursor (2) in order to study the renal characteristics of the resulting 99mTc(I) tricarbonyl cy
A new convenient preparation of thiol esters utilizing N-acylbenzotriazoles
Katritzky, Alan R.,Shestopalov, Aleksandr A.,Suzuki, Kazuyuki
, p. 1806 - 1813 (2007/10/03)
Diverse thiol esters were synthesized in good to excellent yields (76-99%) by reactions of thiophenol, benzyl mercaptan, ethyl mercaptoacetate, and mercaptoacetic acid with N-acylbenzotriazoles under mild conditions. These results demonstrate the utility of N-acylbenzotriazoles as mild S-acylating agents, especially when the corresponding acid chlorides are not readily available.
Kinetic and structural consequences of the leaving group in substrates of a class C β-lactamase
Ahn, Yong-Mo,Pratt
, p. 1537 - 1542 (2007/10/03)
The class C β-lactamase of Enterobacter cloacae P99 is known to catalyze the hydrolysis of certain acyclic (thio)esters. Previous experiments have employed thioglycolate, m-hydroxybenzoate, and phenylphosphate leaving groups. The relative effectiveness of these leaving groups has now been quantitatively assessed by employment of a series of compounds with common acyl groups, and found to rank in the order phenylphosphate >m-hydroxybenzoate >thioglycolate. Structural models suggest that these leaving groups interact during acylation principally with Tyr 150, Lys 315, and Thr 316 of the β-lactamase active site. The positions of the leaving group carboxylates in these models is compared with those in published crystal structures of complexes of class C β-lactamases with β-lactams. The particular effectiveness of the acyl phosphate indicates the positions of two oxyanions that strongly interact with the active site. This information should be useful in the design of inhibitors of class C β-lactamases.
Convenient synthesis of a new class of N2SO or N2S2 tetradentate ligands suitable for nuclear medicine applications
Fourteau,Benoist,Dartiguenave
, p. 126 - 128 (2007/10/03)
In our search for a 99mTc labelled brain perfusion imaging agent, six new tetradentate acyclic ligands have been synthesised in good yield, through easy and fast syntheses. These compounds possess an aromatic ring bridging a nitrogen and an oxygen or a sulfur and contain two amides (1a, 1b) or an amine and an amide functionalities (2a-2d), which make them good candidates for radiopharmaceuticals.
SYNTHETIC HYDROGEN BONDING RECEPTORS AS MODELS OF TRANSACYLASE ENZYMES
Tecilla, Paolo,Jubian, Vrej,Hamilton, Andrew D.
, p. 435 - 448 (2007/10/02)
A family of synthetic receptors has been prepared containing a barbiturate binding site and an appended thiol nucleophile.These are shown to cause large accelerations in the thiolysis reactions of barbiturate active ester derivatives.The size of the acceleration is shown to depend critically on the length and flexibility of the spacer that links the thiol to the receptor.
Syntheses of some Thiol Esters for Acylation of Proteins
Dalton, John R.,Kirkpatrick, Alan,Maclaren, John A.
, p. 759 - 764 (2007/10/02)
A series of thiol esters and S-esters of thiocarbamic acid, has been prepared by making mercaptoacetic acid or 2-mercaptomethanesulfonic acid react with carboxylic acid chlorides or with isocyanates.Aqueous solutions of these products are stable to hydrolysis but rapidly acylate amines.Azo-dyes that incorporate these reactive groups have been synthesized.
