N-acryloyl-1,3-diaminopropane hydrochloride

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: N-acryloyl-1,3-diaminopropane hydrochloride
• 英文别名: N-acryloyl-1,3-propanediamine hydrochloride；3-aminopropyl acrylamide hydrochloride salt；N-(3-aminopropyl)-acrylamide hydrochloride；3-(Prop-2-enoylamino)propylazanium;chloride；3-(prop-2-enoylamino)propylazanium;chloride
• 化学式: C₆H₁₂N₂O*ClH
• 分子量: 164.635
• InChiKey: WOSHDWLEPRMIPR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.06
• 重原子数：
  10
• 可旋转键数：
  4
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  55.1
• 氢给体数：
  3
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  N-acryloyl-1,3-diaminopropane hydrochloride 、 3,5-吡啶二甲酰氯 在 sodium hydride 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 16.17h， 以40%的产率得到N³,N⁵-bis(3-acrylamidopropyl)pyridine-3,5-dicarboxamide
  参考文献：
  名称：

  Synthesis of Pyridine Acrylates and Acrylamides and Their Corresponding Pyridinium Ions as Versatile Cross-Linkers for Tunable Hydrogels

  摘要：

  A small library of cross-linkers for hydrogels was synthesized. The cross-linkers consisted of 2,6- and 3,5-diacylpyridine or 2,4,6-triacylpyridine as the core unit, which were tethered via ethylene glycol, amino ethanol, and 1,n-diamine spacers to terminal acrylate or acrylamide moieties. Esterification and amide formation of the terminal acryl units were found to be dependent on the ratio of NH/O in the spacer, the constitution pattern of the pyridine ring, and the total number of acryl groups. Thus, esters generally gave higher yields than amides decreasing with increasing number of NH in the spacer and with increasing number of acryl units. In the case of 3,5-diacylpyridine derivatives, these trends were less prominent as compared to the 2,6-diacylpyridine series, indicating that steric hindrance and unfavorable hydrogen bonding interaction of the spacers might influence the observed reactivity differences. The 3,5-diacylpyridines were converted to the N-methylpyridinium salts and selected members of both neutral and cationic 3,5-diacylpyridinium derivatives were submitted to hydrogelations with synthetic polymer poly(1-glycidylpiperazine) via aza-Michael addition and thiolated natural hyaluronan via thio-Michael reaction, respectively. Rheological properties of the resulting hydrogels were studied, revealing that both spacer type as well as charge affected elastic moduli and degree of swelling.

  DOI：

  10.1055/s-0033-1338614
• 作为产物：
  描述：

  tert-butyl (3-acrylamidopropyl)carbamate 在 盐酸 作用下， 以 乙醚 、 乙酸乙酯 为溶剂， 以93%的产率得到N-acryloyl-1,3-diaminopropane hydrochloride
  参考文献：
  名称：

  [EN] ZAP-70 KINASE INHIBITOR COMPOSITIONS, METHODS AND USES THEREOF
  [FR] COMPOSITIONS D'INHIBITEUR DE KINASE ZAP-70, PROCÉDÉS ET UTILISATIONS DE CELLES-CI

  摘要：

  揭示了化合物的化学式(I)和(V)，以及这些化合物的组合物，可用作ZAP-70激酶的抑制剂。还提供了合成方法和使用ZAP-70抑制剂治疗器官移植排斥、自身免疫疾病和癌症的方法。

  公开号：

  WO2019067396A1

文献信息

• [EN] BIOCOMPATIBLE POLYMERIC DRUG CARRIERS FOR DELIVERING ACTIVE AGENTS<br/>[FR] SUPPORTS DE MÉDICAMENT POLYMÈRES BIOCOMPATIBLES PERMETTANT L'ADMINISTRATION D'AGENTS ACTIFS
  申请人：CIS PHARMA AG

  公开号：WO2021084087A1

  公开（公告）日：2021-05-06

  The present disclosure relates to the delivery of multiple copies of a payload molecule such as an active agent or a chelating agent capable of capturing an active agent, using as a carrier for their delivery a biocompatible copolymer comprising side chain-linked amino acids functionalized at their alpha-amino group by a reactive azide moiety by means of which the payload molecules are coupled to the copolymer. The copolymer is typically further functionalized to contain a single copy of a cell type- or tissue type-specific targeting moiety.

  本公开涉及使用生物相容性共聚物作为载体，传递多个剂量分子副本，如活性剂或能够捕获活性剂的螯合剂。这些共聚物包含通过其α-氨基团上的反应性叠氮基团功能化的侧链连接氨基酸，通过这种方式，荷载分子与共聚物耦合。通常，这种共聚物进一步功能化，以包含细胞类型或组织类型特异性靶向基团的单个副本。
• [EN] ZAP-70 KINASE INHIBITOR COMPOSITIONS, METHODS AND USES THEREOF<br/>[FR] COMPOSITIONS D'INHIBITEUR DE KINASE ZAP-70, PROCÉDÉS ET UTILISATIONS DE CELLES-CI
  申请人：SNAP BIO INC

  公开号：WO2019067396A1

  公开（公告）日：2019-04-04

  Disclosed are compounds of formulas (I) and (V) and compositions thereof useful as inhibitors of ZAP-70 kinase. Also provided are methods of synthesis and methods of use of ZAP-70 inhibitors in treating individuals suffering from organ transplant rejection, autoimmune diseases and cancer.

  揭示了化合物的化学式(I)和(V)，以及这些化合物的组合物，可用作ZAP-70激酶的抑制剂。还提供了合成方法和使用ZAP-70抑制剂治疗器官移植排斥、自身免疫疾病和癌症的方法。
• Ink jet composition containing microgel particles
  申请人：Uerz S. David

  公开号：US20060100307A1

  公开（公告）日：2006-05-11

  This invention relates to an ink jet ink composition comprising an aqueous medium and microgel particles, said particles comprising a crosslinked copolymer prepared from a monomer mixture comprising at least a crosslinking monomer, a polymerizable carboxylic acid monomer, and one or more polymerizable water insoluble vinyl type monomers. The ink composition may be a colorless ink or it may contain a colorant.

  本发明涉及一种墨水喷射墨水组成物，包括水性介质和微凝胶颗粒，所述颗粒包括由单体混合物制备的交联共聚物，该单体混合物包括至少一种交联单体，一种可聚合的羧酸单体和一种或多种可聚合的水不溶性乙烯类单体。该墨水组成物可以是无色墨水，也可以含有着色剂。
• SEQUESTRANTS OF ADVANCED GLYCATION END PRODUCT (AGE) PRECURSORS
  申请人：GENZYME CORPORATION

  公开号：US20160024233A1

  公开（公告）日：2016-01-28

  Sequestrants of AGE precursors comprise amines separated by 2, 3 or 4 carbons. Sequestrants of AGE precursors can be used as pharmaceutical agents and in pharmaceutical compositions. The sequestrants of AGE precursors are particularly useful binding AGE precursors and dietary dicarbonyls in mammals in the gastrointestinal tract for the treatment of ailments such as diabetic nephropathy, chronic renal disease, atherosclerosis, stroke, cataracts, and Alzheimer's disease.

  AGE前体的螯合剂包括间隔2、3或4个碳的胺类物质。AGE前体的螯合剂可用作药物剂和药物配方。AGE前体的螯合剂特别有用于在哺乳动物的胃肠道中结合AGE前体和饮食中的二羧基化合物，用于治疗糖尿病肾病、慢性肾脏疾病、动脉硬化、中风、白内障和阿尔茨海默病等疾病。
• Synthesis of antimicrobial polymers with mannose residues as binders for the <scp>FimH</scp> adhesin of <i>Escherichia coli</i>
  作者：Atsushi Miyagawa、Shinya Ohno、Hatsuo Yamamura

  DOI：10.1002/pol.20220540

  日期：2023.2.15

  16 μg/ml) against E. coli selectivity (no effect on Staphylococcus aureus was observed). Further, the polymer containing the hexyl mannose residue did not develop resistance in E. coli after 15 passages. Consequently, polymers with mannose units, which have a high affinity for the FimH adhesin, can serve as effective and selective antimicrobial agents against E. coli.

  最近，抗菌聚合物已被开发为新型抗生素，它们对人类健康有益。这些聚合物的一个优点是它们可以很容易地通过添加或修改单体进行功能化。在这项研究中，为了提高聚合物的细菌选择性和抗菌活性，将甘露糖单体与氨基丙基单体和异烷基单体共聚。发现这些甘露糖单体模拟哺乳动物细胞上与大肠杆菌的 FimH 粘附素相互作用的甘露聚糖和N-聚糖部分。具有短乙基接头的甘露糖单体不会增强对大肠杆菌的抗菌活性（最小抑菌浓度 (MIC)：32 μg/ml）; 然而，使用较长的己基接头可增强针对大肠杆菌的抗菌活性（MIC：16 μg/ml） （未观察到对金黄色葡萄球菌有影响）。此外，含有己基甘露糖残基的聚合物在大肠杆菌传代 15 次后未产生耐药性。因此，具有对 FimH 粘附素具有高亲和力的甘露糖单元的聚合物可以用作针对大肠杆菌的有效且选择性的抗菌剂。