85301-93-5Relevant academic research and scientific papers
Synthesis of Boronocysteine
Gibson, Samantha M.,Macmillan, Derek,Sheppard, Tom D.
, p. 314 - 317 (2017/10/30)
Herein we report the first synthesis of protected boronocysteine. The target compound was prepared via copper-catalysed diastereoselective nucleophilic borylation of a sulfinimine. After deprotection to give the amine as the hydrochloride salt, four boron
Bioresponsive small molecule polyamines as noncytotoxic alternative to polyethylenimine
Drake, Christopher R.,Aissaoui, Abderrahim,Argyros, Orestis,Serginson, James M.,Monnery, Bryn D.,Thanou, Maya,Steinke, Joachim H. G.,Miller, Andrew D.
scheme or table, p. 2040 - 2055 (2011/10/04)
Nonviral gene therapy continues to require novel synthetic vectors to deliver therapeutic nucleic acids effectively and safely. The majority of synthetic nonviral vectors employed in clinical trials to date have been cationic liposomes; however, cationic
Synthesis of thiazolidine-2-thione derivatives and evaluation of their hepatoprotective effects
Yoneda,Ota,Kawashima
, p. 876 - 881 (2007/10/02)
A series of N-(mercaptoalkyl)thiazolidine-2-thiones and their derivatives were synthesized and evaluated for hepatoprotective activities against Propionibacterium acnes-lipopolysaccharide (R. acnes-LPS)-induced liver injury in mice and in vitro lipid pero
Design of novel inhibitors of aminopeptidases. Synthesis of peptide-derived diamino thiols and sulfur replacement analogues of bestatin
Gordon,Godfrey,Delaney,Asaad,Von Langen,Cushman
, p. 2199 - 2211 (2007/10/02)
Investigations were directed toward inhibition of an aminopeptidase, isolated from rat brain, which has been implicated in the metabolic inactivation of enkephalins. The design rationale and synthesis of novel peptidyl diamino thiol inhibitors of rat brain aminopeptidase are presented, along with accompanying structure-activity analysis. Some of the reported compounds are highly active aminopeptidase inhibitors and possess enzyme inhibitory potency in the nanomolar range (62; I50 = 1 nM). Analysis of the data permits speculations on possible modes of binding of diamino thiols to aminopeptidase. Other investigations were directed toward understanding the mode of enzyme binding of the naturally occurring aminopeptidase inhibitor bestatin. On the basis of published models of enzyme binding, replacement of the C-2 hydroxyl group of bestatin by a sulfhydryl group was anticipated to lead to enhanced inhibition due to a strengthened interaction of this group with enzymic zinc. Contrary to expectations, 'thiobestatin' inhibited rat brain aminopeptidase with only the same degree of effectiveness as the corresponding alcohol. Speculations on the possible mode of enzyme-inhibitor binding of bestatin are offered.
A novel synthesis of 5,6-dihydro-2,3-bisaryl-8H-imidazo[2,1-c][2,1-c][1,4]thiazine
Lantos,Razgaitis,Sutton
, p. 1375 - 1376 (2007/10/02)
Bisaryl-8H-imidazo[2,1-c][1,4]thiazine were prepared from the corresponding 2-thiomethylimidazoles. A novel and efficient synthesis is presented for these intermediates based on the condensation of benzils with protected 2-thioacetaldehydes.
