wang resin

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: wang resin
• 英文别名: Paramax Wang resin；Cyclopropyl-ethyl-(4-ethynyl-2-methyl-benzyl)-amine；N-ethyl-N-[(4-ethynyl-2-methylphenyl)methyl]cyclopropanamine
• 化学式: C₁₄H₁₃O₂Pol
• 分子量: 213.32
• InChiKey: BTNWMNYMIWSIFL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  16
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  3.2
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  wang resin 在 Jones reagent 作用下， 以 二氯甲烷 、 丙酮 为溶剂， 反应 24.0h， 生成
  参考文献：
  名称：

  Novel steroidal antiestrogens and antiandrogens and uses thereof

  摘要：

  本发明涉及设计、合成和开发一类新型化疗药物，用于哺乳动物，特别是人类的预防性和治疗性治疗，被认为处于患有激素敏感性疾病风险中。在本发明的实施例中，这些治疗包括包含新型类固醇抗雌激素和抗雄激素化合物的治疗组合物。在一个首选实施例中，本发明的这种新型化合物具有地址和消息组件，这些组件被制成单个复合实体，用于更积极地干预和有效治疗激素敏感性疾病，从而延长患者的无病间隔时间并减少副作用数量。

  公开号：

  US20040002484A1
• 作为产物：
  描述：

  cyclopropyl-ethyl-(2-methyl-4-trimethylsilanylethynyl-benzyl)-amine 在 potassium carbonate 作用下， 以 甲醇 为溶剂， 以99%的产率得到wang resin
  参考文献：
  名称：

  Compounds having activity as inhibitors of cytochrome P450RAI

  摘要：

  具有化学式1的化合物，在该化学式中符号的含义如规范中定义的那样，是细胞色素P450RAI（视黄酸诱导）酶的抑制剂，并用于治疗对视黄醇类药物治疗有效的疾病。

  公开号：

  US06252090B1
• 作为试剂：
  描述：

  Fmoc-L-亮氨酸 、 (2S,3R)-3-(Boc-氨基)-2-羟基-4-苯基丁酸 在 4-二甲氨基吡啶 、 wang resin 、 N,N-二异丙基乙胺 、 Methanaminium,N-[(dimethylamino)(3H-1,2,3-triazolo[4,5-b]pyridin-3-yloxy)methylene]-N-methyl-, hexafluorophosphate(1-) 、 哌啶 、 1,8-二氮杂双环[5.4.0]十一碳-7-烯 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 1.5h， 生成 乌苯美司
  参考文献：
  名称：

  Synthesis of New (−)-Bestatin-Based Inhibitor Libraries Reveals a Novel Binding Mode in the S1 Pocket of the Essential Malaria M1 Metalloaminopeptidase

  摘要：

  The malarial PfA-M1 metalloaminopeptidase is considered a putative drug target. The natural product dipeptide mimetic, bestatin, is a potent inhibitor of PfA-M1. Herein we present a new, efficient, and high-yielding protocol for the synthesis of bestatin derivatives from natural and unnatural N-Boc-D-amino acids. A diverse library of bestatin derivatives was synthesized with variants at the side chain of either the alpha-hydroxy-beta-amino acid (P1) or the adjacent natural a-amino add (P1'). Surprisingly, we found that extended aromatic side chains at the P1 position resulted in potent inhibition against PfA-M1. To understand these data, we determined the X-ray cocrystal structures of PfA-M1 with two derivatives having either a Tyr(OMe) 15 or Tyr(OBz1) 16 at the 131 position and observed substantial inhibitor-induced rearrangement of the primary loop within the PEA-M1 pocket that interacts with the PI side chain. Our data provide important insights for the rational design of more potent and selective inhibitors of this enzyme that may eventually lead to new therapies for malaria.

  DOI：

  10.1021/jm101227t

文献信息

• Solid phase synthesis of new thiazolidinedione-pyrimidine conjugates and their antibacterial properties
  作者：Veronika Šlachtová、Lucie Janovská、Lucie Brulíková

  DOI：10.1016/j.molstruc.2019.01.073

  日期：2019.5

  Abstract The polymer-supported synthetic protocol for preparation of thiazolidinedione-pyrimidine hybrids was developed and applied for rapid and effective synthesis of a library of variously substituted conjugates. Reported synthetic methodology is based on easy accessible building blocks and very simple chemical operations enabling effective development of potent experimental therapeutics of this

  摘要 开发了用于制备噻唑烷二酮-嘧啶杂化物的聚合物支持的合成方案，并用于快速有效地合成各种取代的缀合物文库。报道的合成方法基于易于获取的构建块和非常简单的化学操作，能够通过组合方式有效开发此类有效的实验疗法。测试合成的模型化合物对结核分枝杆菌 H37Rv 的抗结核活性，对几种革兰氏阳性和革兰氏阴性菌株的抗菌活性，如金黄色葡萄球菌、铜绿假单胞菌、大肠杆菌和粪肠球菌以及两种真菌菌株（白色念珠菌和黑曲霉） . 他们中的一些人发现了轻微的活动。
• Water soluble multi-biotin-containing compounds
  申请人：Wilbur Scott D.

  公开号：US20060228325A1

  公开（公告）日：2006-10-12

  Water-soluble discrete multi-biotin-containing compounds with at least three (3) biotin moieties are disclosed. The water-soluble biotin-containing compounds may additionally comprise one or more moieties that confer resistance to cleavage by biotinidase or that is cleavable in vitro or in vivo. The discrete multi-biotin-containing compounds may include a reactive moiety that provides a site for reaction with yet another moiety, such as a targeting, diagnostic or therapeutic functional moiety. Biotinylation reagents comprising water-soluble linker moieties are also disclosed and may additionally comprise a biotinidase protective group. Methods for amplifying the number of sites for binding biotin-binding proteins at a selected target using multi-biotin compounds also are disclosed.

  可溶于水的离散多生物素含有化合物，至少含有三个（3）生物素基团。这些可溶于水的生物素含有化合物可能还包括一个或多个使其对生物素酶的裂解具有抗性的基团，或者在体外或体内可被裂解的基团。这些离散的多生物素含有化合物可能包括一个反应性基团，提供与另一个基团（如靶向、诊断或治疗功能基团）反应的位点。还公开了包含可溶于水的连接基团的生物素化试剂，可能还包括生物素酶保护基团。还公开了使用多生物素化合物扩增在选定靶点上结合生物素结合蛋白的位点数量的方法。
• [EN] BIORESPONSIVE POLYMER SYSTEM FOR DELIVERY OF MICROBICIDES<br/>[FR] SYSTEME POLYMERE BIOSENSIBLE POUR L'ADMINISTRATION DE MICROBICIDES
  申请人：UNIV UTAH RES FOUND

  公开号：WO2005097210A1

  公开（公告）日：2005-10-20

  The polymer systems of the present invention degrade in the presence of an ejaculate. They may further provide degradable sequences that degrade upon contact with an ejaculate and/or microbicides. The polymer systems of the present invention are of use in the oral, rectal or vaginal cavities of an individual for such purposes as the treatment or prevention of sexually transmitted disease, the prevention or promotion of fertility or for hormone replacement therapy.

  本发明的聚合物系统在射精的存在下降解。它们还可以提供在接触射精和/或杀微生物剂时降解的可降解序列。本发明的聚合物系统适用于个人的口腔、直肠或阴道腔道，用于治疗或预防性传播疾病、预防或促进生育或用于激素替代疗法。
• Peptides for inhibition of apoptosis and pharmaceutical compositions containing them
  申请人：Ziv Ilan

  公开号：US06849603B1

  公开（公告）日：2005-02-01

  The present invention relates to an isolated and purified peptide of the RY domain having an amino acid sequence of general formula (I) comprising a sequence of the following amino acids: X 1 —X 2 —X 3 —X 4 —X 1 —X 4 —X 4 —X 3 —X 1 , X 1 =Phe, Tyr, or any amino acid having a substituted aromatic residue; X 2 =Glu, Asp, Ser, or any amino acid having a —(CH 2 ) n —COO residue, wherein n=0-3; X 3 =Asp, Thr, any aliphatic amino acid, or any of amino acids X 4 ; and X 4 =Arg, Lys, or any amino acid having a —(CH 2 ) n —NH 3 + residue, or a —(CH 2 ) n —NH—C(NH 3 + )NH 2 residue wherein n=0-4; as well as functional equivalents thereof. The invention relates also to pharmaceutical compositions comprising a compound of general formula (I), the use of said RY peptide and of said pharmaceutical composition in the preparation of a medicament and in method for the treatment of disorders of inappropriate activation of apoptosis; for increasing the number of viable cells in a biological tissue; and in a method for the enhancement for the survival of biological cells. The invention also relates to a method for the preparation of a RY-peptide of general formula (I). Furthermore, the invention also relates to an in vitro assay system for the regulation of cell death by the Bcl-2 family of test compounds (as hereinbefore defined).

  本发明涉及一种具有一般式(I)氨基酸序列的RY结构域的分离和纯化肽，包括以下氨基酸序列：X1—X2—X3—X4—X1—X4—X4—X3—X1，其中X1=Phe、Tyr或具有取代芳香基的任何氨基酸；X2=Glu、Asp、Ser或具有—(CH2)n—COO残基的任何氨基酸，其中n=0-3；X3=Asp、Thr、任何脂肪族氨基酸或任何氨基酸X4；X4=Arg、Lys或具有—(CH2)n—NH3+残基的任何氨基酸，或具有—(CH2)n—NH—C(NH3+)NH2残基的任何氨基酸，其中n=0-4；以及其功能等效物。该发明还涉及包含一般式(I)化合物的药物组合物，以及利用所述RY肽和所述药物组合物制备药物和治疗不恰当激活凋亡的疾病的方法；用于增加生物组织中存活细胞数量的方法；以及用于增强生物细胞存活的方法。该发明还涉及一种制备一般式(I)的RY-肽的方法。此外，该发明还涉及一种用于通过Bcl-2家族的试验化合物（如前文所定义）调节细胞死亡的体外测定系统。
• Sequence-Independent Traceless Method for Preparation of Peptide/Protein Thioesters Using CPaseY-Mediated Hydrazinolysis
  作者：Masahiro Ueda、Chiaki Komiya、Sayuki Arii、Kohshi Kusumoto、Masaya Denda、Keiichiro Okuhira、Akira Shigenaga、Akira Otaka

  DOI：10.1248/cpb.c20-00674

  日期：2020.12.1

  CPaseY-mediated hydrazinolysis of C-terminal Xaa (X)-Cys-proline (Pro)-leucine (Leu)-OH sequence followed by an auto-processing of the Cys-Pro (CP) dipeptide unit, affording the corresponding X-thioester (X-SR). However, hydrazinolysis of the amide bond in the prolyl leucine junction depends significantly on the nature of X. In the case of hydrophobic X residues, the hydrazinolysis overreacts to give

  结合了人工部分（例如荧光团和药物）的蛋白质已在化学生物学和药物开发研究中得到越来越多的使用。这种人工蛋白质衍生物的制备主要依赖于天然化学连接，其中肽/蛋白质硫酯与N-末端半胱氨酸（Cys）肽化学选择性反应以提供蛋白质分子。衍生自表达蛋白质的蛋白质硫酯代表硫酯，通过与具有N端Cys的合成肽进行天然化学连接，对于制备人工蛋白质非常有用。我们最近开发了一种使用羧肽酶Y（CPaseY）的无痕硫代酸酯生产协议，该协议可与表达的蛋白质相容。通过CPaseY介导的C端Xaa（X）-Cys-脯氨酸（Pro）-亮氨酸（Leu）-OH序列的肼解反应，然后自动处理Cys-Pro（CP）二肽单元，确保了无痕特征。得到相应的X-硫酯（X-SR）。但是，脯氨酰亮氨酸连接处酰胺键的肼解作用很大程度上取决于X的性质。在疏水性X残基的情况下，肼解反应会过度反应生成数个酰肼，而亲水性X残基的反应则缓慢进行。在这项研究中，我们