dansyl chloride | 51278-32-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: dansyl chloride
• 英文别名: 1-Dimethylamino-4-naphthalinsulfonylchlorid；4-(Dimethylamino)naphthalene-1-sulfonyl chloride
• CAS: 51278-32-1
• 化学式: C₁₂H₁₂ClNO₂S
• 分子量: 269.752
• InChiKey: RYROYNBRZNYMLE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  45.8
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  dansyl chloride 、 Boc-Tyr-D-Ala-Gly-Phe-NH-NH2 在 吡啶 、 三氟乙酸 作用下， 生成 L-Tyr-D-Ala-Gly-L-Phe-NH-NH-DNS
  参考文献：
  名称：

  Biological properties of a new fluorescent biphalin fragment analogue

  摘要：

  Previous studies of structure- activity of biphalin defined fragments which expressed the full biological potency of the parent compound. The most simple fragment was Tyr-D-Ala-Gly-Phe-NH-NH<--X, where X=Phe, but it also could be other hydrophobic amino acids. This paper presents data that replacement of the phenylalanine with a dansyl (X=DNS) groups gives an analogue (AA2016) that fully preserves the high affinity of the initial analogue for both R and 8 opioid receptors. In the tail flick test in rats, intrathecal injection of the compound produces strong antinociception, comparable to the parent biphalin. Because AA2016 contains a strong fluorescent group, it can be a very useful tool for prospective studies in vivo, including biological barrier permeability, tissue distribution, metabolism and receptor-ligand complex formation. (C) 2002 Elsevier Science Inc. All rights reserved.

  DOI：

  10.1016/s0024-3205(01)01467-9

文献信息

• [EN] F2 DERIVATIVES AS ANTIBACTERIAL AGENTS<br/>[FR] DÉRIVÉS DE F2 COMME AGENTS ANTIBACTÉRIENS
  申请人：PENN STATE RES FOUND

  公开号：WO2013154793A1

  公开（公告）日：2013-10-17

  A compound or its pharmaceutically acceptable salt, as well as a pharmaceutical composition containing that compound or salt dissolved or dispersed in a pharmaceutically acceptable carrier, and a method of using that compound or salt in an antibacterial treatment. A contemplated compound corresponds in structure to structural Formula I or a pharmaceutically acceptable salt of that compound, wherein V is O or NR9, Y is halogen, OR10, C1-C4 hydrocarbyl or NHR10, Z is NR2-X-R1 or CH2-R8, n is 1-6, X is H, S(O)2, C(O), C(O)NR7, C(NH)NR7 or C (O) O, and R1, R2, R7 ' R8, R9 and R10 are defined within. ( l )

  一种化合物或其药学上可接受的盐，以及含有该化合物或盐溶解或分散在药学上可接受的载体中的制药组合物，以及使用该化合物或盐进行抗菌治疗的方法。所考虑的化合物在结构上对应于结构式I或该化合物的药学上可接受的盐，其中V为O或NR9，Y为卤素，OR10，C1-C4烃基或NHR10，Z为NR2-X-R1或CH2-R8，n为1-6，X为H，S(O)2，C(O)，C(O)NR7，C(NH)NR7或C(O)O，R1，R2，R7，R8，R9和R10在内部有定义。
• Aromatic sulphonamides of aziridine-2-carboxylic acid derivatives as novel PDIA1 and PDIA3 inhibitors
  作者：D. Zelencova-Gopejenko、V. Andrianov、I. Domracheva、I. Kanepe-Lapsa、M. Milczarek、M. Stojak、K. Przyborowski、F. A. Fedak、M. Walczak、K. Kramkowski、J. Wietrzyk、S. Chlopicki、I. Kalvins

  DOI：10.1080/14756366.2022.2158187

  日期：2023.12.31

  Abstract In this study, we report a series of newly synthesised sulphonamides of aziridine-2-carboxylic acid (Az-COOH) ester and amide analogues as potent protein disulphide isomerase (PDI, EC 5.3.4.1) inhibitors. The inhibitory activity on PDI was determined against recombinant human PDIA1 and PDIA3 proteins using an insulin reduction assay. These compounds in low micromolar to low nanomolar concentrations

  摘要 在这项研究中，我们报告了一系列新合成的氮丙啶-2-羧酸 (Az-COOH) 酯和酰胺类似物磺胺类化合物作为有效的蛋白质二硫化物异构酶 (PDI, EC 5.3.4.1) 抑制剂。使用胰岛素减少测定法针对重组人 PDIA1 和 PDIA3 蛋白确定对 PDI 的抑制活性。低微摩尔至低纳摩尔浓度的这些化合物显示出有效的PDIA1体外抑制特性，对 PDIA3 的影响较弱。15 N- 和15 N, 13的配合物C-均匀标记的重组人 PDIA1a 与两种 PDIA1 抑制剂被生产并通过蛋白质核磁共振 (NMR) 光谱进行研究。发现 PDIA1 酶的 C53 和 C56 均参与共价结合。最后，在一系列药理学研究中，我们证明了所研究的化合物具有抗癌和抗血栓形成活性。这些发现表明，Az-COOH 衍生物的磺胺类药物是开发新型抗癌剂和抗血栓剂的有前途的候选者。
• Synthesis of 1-Thiaphenalene Derivatives via Radical Cyclization of 1-Naphthalenesulfonyl Chlorides with Alkynes
  作者：Youhao Wei、Jige Liu、Chen Zhu、Xinxin Wu、Yasu Chen

  DOI：10.1055/a-2020-8828

  日期：——

  Functionalized thiaphenalene derivatives are of high synthetic value, yet their preparation remains underexplored. Herein, we report an efficient approach for the synthesis of 1-thiaphenalene derivatives through radical cyclization of 1-naphthalenesulfonyl chlorides with alkynes. A variety of 1-thiaphenalene derivatives are readily furnished that are otherwise difficult to prepare by present methods

  功能化的噻吩衍生物具有很高的合成价值，但其制备方法仍未得到充分探索。在此，我们报告了一种通过 1-萘磺酰氯与炔烃的自由基环化合成 1-噻吩衍生物的有效方法。各种 1-thiaphenalene 衍生物很容易提供，否则很难通过现有方法制备。该协议具有温和的光催化条件、广泛的功能组兼容性和高产品多样性。
• Tissue-integrating electronic apparatus
  申请人：PROFUSA, Inc.

  公开号：US10010272B2

  公开（公告）日：2018-07-03

  Tissue-integrating electronic apparatuses, systems comprising such apparatuses and methods of using these apparatuses and systems for the detection of one or more signals are provided.

  提供了用于检测一个或多个信号的组织集成电子装置、包含这些装置的系统以及使用这些装置和系统的方法。
• Synthesis and in vitro evaluation of leishmanicidal and trypanocidal activities of N-quinolin-8-yl-arylsulfonamides
  作者：Luiz Everson da Silva、Antônio Carlos Joussef、Letícia Kramer Pacheco、Daniela Gaspar da Silva、Mário Steindel、Ricardo Andrade Rebelo

  DOI：10.1016/j.bmc.2007.09.007

  日期：2007.12

  In the present paper 12 N-quinolin-8-yl-arylsulfonamides synthesized by coupling 8-aminoquinolines with various arylsulfonylchlorides were assayed in vitro against Leishmania amazonensis, L. chagasi and Trypanosoma cruzi strains. This series of new compounds were found to be selective for Leishmania spp. promastigote and amastigote forms. The most active compound was the N-(8-quinolyl)-3,5-diflu. uoro-benzenesulfonamide 10 with an IC50 against L. amazonensis and L. chagasi of 2.12 and 0.45 mu M, respectively. The less cytotoxic biphenyl derivative 7 was very e. ffective against intracellular L. amazonensis with a reduction of macrophage cell infection of 82.1% at 25 mu M. In addition, a copper complex 17 of an inactive ligand was readily synthesized and showed high leishmanicidal and trypanocidal activity against both extra and intracellular forms. (c) 2007 Elsevier Ltd. All rights reserved.