Preparation of the 15-membered cycle (E,E,E)-1,6,11-tris[(2,4,6-triisopropylphenyl)sulfonyl]-1,6,11-triazacyclopentadeca3,8,13-triene (8) is reported. This cyclic triolefin forms a stable Pd0 complex 9 which catalyzes several cross-coupling reactions and can be recovered. Anchoring to a polystyrene framework affords a solid version of the catalyst, which is recovered by simple filtration and reused
Novel agmatine and agmatine-like peptidomimetic inhibitors of the West Nile virus NS2B/NS3 serine protease
作者:Huichang Annie Lim、Joma Joy、Jeffrey Hill、Cheng San Brian Chia
DOI:10.1016/j.ejmech.2011.04.055
日期:2011.7
This communication reports the synthesis and inhibitory activities of novel non-covalent peptidomimetic inhibitors of the West Nile virus NS2B/NS3 protease containing a decarboxylated P1 arginine (agmatine; 4-aminobutylguanidine) and related analogues. One agmatine peptidomimetic (4-phenyl-phenacetyl-Lys-Lys-agmatine; compound 2) was shown to be a competitive inhibitor with a binding affinity of Ki
该信息通报了西尼罗河病毒NS2B / NS3蛋白酶的新型非共价拟肽抑制剂的合成和抑制活性,该抑制剂含有脱羧化的P1精氨酸(胍丁胺; 4-氨基丁基胍)和相关类似物。一种胍丁胺肽模拟物(4-苯基-苯乙酰基-Lys-Lys-胍丁胺;化合物2)显示为竞争性抑制剂,结合亲和力为K i 2.05±0.13μM,对凝血酶没有活性(IC 50 > 100μM)。我们的结果表明,与含反应性亲电战斗部的抑制剂相比,由于它们的相对稳定性和化学合成的简便性,在P1位置具有胍丁胺的拟肽可能被用作设计非共价竞争性蛋白酶抑制剂的起始工具。
Steric Control over Hydrogen Bonding in Crystalline Organic Solids: A Structural Study ofN,N?-Dialkylthioureas
作者:Radu Custelcean、Maryna G. Gorbunova、Peter V. Bonnesen
DOI:10.1002/chem.200400973
日期:2005.2.18
single-crystal X-ray diffraction, DFT calculations, and Cambridge Structural Database (CSD) analysis. A CSD survey indicated that unlike the related urea derivatives, which persistently self-assemble into one-dimensional hydrogen-bonded chains, the analogous thioureas can form two different hydrogen-bonding motifs in the solid state: chains, structurally similar with those found in ureas, and dimers, that further
作者:Gabriela Chiosis、Julia Aguirre、Christopher V. Nicchitta
DOI:10.1016/j.bmcl.2006.03.092
日期:2006.7
The synthesis and evaluation of several chemical modulators of heat shock protein 90 (Hsp90) dimerization is presented. These agents may represent useful tools to study the importance of N-terminal dimerization and also to determine subunit interface(s) in Hsp90. (c) 2006 Elsevier Ltd. All rights reserved.