134081-15-5Relevant academic research and scientific papers
Determination of absolute stereochemistry, total synthesis, and evaluation of peptides from the myxomycete Physarum melleum
Hanazawa, Shuwa,Arai, Midori A.,Li, Xiaofan,Ishibashi, Masami
, p. 95 - 98 (2008/09/17)
The absolute stereochemistry of melleumin A (1) and B (2), novel peptide compounds isolated from the myxomycete Physarum melleum, was determined by synthesis of their segments and by a modified Mosher's method. Total synthesis of melleumin B (2) was achie
A facile access to pyrroles from amino acids via an aza-Wacker cyclization
Zhang, Zuhui,Zhang, Jintang,Tan, Jiajing,Wang, Zhiyong
, p. 5180 - 5182 (2008/12/20)
(Chemical Equation Presented) A facile and efficient synthesis of pyrroles from readily available amino acids is described. The key step in the method is an aza-Wacker oxidative cyclization catalyzed by palladium(II)/Cu(OTf) 2. A series of pyrroles were obtained by this method under mild conditions.
Novel CADD-based peptidyl vinyl ester derivatives as potential proteasome inhibitors
Mou, Ke,Xu, Bo,Ma, Chao,Yang, Xiaoming,Zou, Xiaomin,Lue, Yang,Xu, Ping
, p. 2198 - 2202 (2008/12/22)
A series of peptidyl vinyl ester derivatives bearing three different P1 substitutions as potential proteasome inhibitors were studied. The target molecules were designed based on CADD (computer aided drug design) protocol and synthesized. Their activities
Novel cell-penetrating α-keto-amide calpain inhibitors as potential treatment for muscular dystrophy
Lescop, Cyrille,Herzner, Holger,Siendt, Herve,Bolliger, Reto,Henneboehle, Marco,Weyermann, Philipp,Briguet, Alexandre,Courdier-Fruh, Isabelle,Erb, Michael,Foster, Mark,Meier, Thomas,Magyar, Josef P.,Von Sprecher, Andreas
, p. 5176 - 5181 (2007/10/03)
Dipeptide-derived α-keto-amide compounds with potent calpain inhibitory activity have been identified. These reversible covalent inhibitors have IC50 values down to 25 nM and exhibit greatly improved activity in muscle cells compared to the reference compound MDL28170. Several novel calpain inhibitors have shown positive effects on histological parameters in an animal model of Duchenne muscular dystrophy demonstrating their potential as a treatment option for this fatal disease.
Inhibitors of protein tyrosine phosphatase
-
Page column 59,60, (2010/11/29)
The present invention comprises small molecular weight, non-peptidic inhibitors of formula I and II of Protein Tyrosine Phosphatase 1 (PTP1) which are useful for the treatment and/or prevention of Non-Insulin Dependent Diabetes Mellitus (NIDDM).
The total synthesis of the diepoxycyclohexanone antibiotic aranorosin and novel synthetic analogues
McKillop, Alexander,McLaren, Lee,Taylor, Richard J. K.,Watson, Robert J.,Lewis, Norman J.
, p. 1385 - 1393 (2007/10/03)
A short synthesis of the novel antibiotic aranorosin in chiral form is described which employs (i) a novel hypervalent iodine-mediated oxidative hydroxylation of a tyrosinal derivative and (ii) a stereocontrolled cis-bisepoxidation in the key steps. A similar procedure was employed to prepare 6′-epiaranorosin, and hence establish the stereochemistry of the natural compound, and to prepare novel aranorosin analogues. An organometallic route is described which gives desamidoaranorosin.
Synthesis of 2-isoxazoline and α-hydroxy ketomethylene dipeptide isosteres
Chung, Yong Jun,Ryu, Eun Jung,Keum, Gyochang,Kim, Byeang Hyean
, p. 209 - 225 (2007/10/03)
We have developed a simple and stereoselective method for synthesizing novel dipeptide isosteres using nitrile oxide cycloaddition as a key reaction. Employing this method, we have prepared efficiently various peptidomimetics containing 2-isoxazolines and
A concise synthesis of the novel antibiotic aranorosin
McKillop,McLaren,Watson,Taylor,Lewis
, p. 5519 - 5522 (2007/10/02)
A short synthesis of the novel antibiotic aranorosin is described which employs a novel hypervalent iodine-mediated oxidative hydroxylation of a tyrosinal derivative in the key step. A similar procedure was employed to prepare 6'-epiaranorosin, and hence establish the stereochemistry of the natural compound.
