2-amino-5-phenylpent-4-enoic acid | 99855-10-4

• 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: 2-amino-5-phenylpent-4-enoic acid
• 英文别名: 2-azaniumyl-5-phenylpent-4-enoate
• CAS: 99855-10-4
• 化学式: C₁₁H₁₃NO₂
• 分子量: 191.23
• InChiKey: MCGSKGBMVBECNS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.8
• 重原子数：
  14
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  63.3
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  Acetamino-cinnamyl-malonsaeure-diethylester 在 盐酸 、 水 作用下， 反应 0.17h， 以94%的产率得到2-amino-5-phenylpent-4-enoic acid
  参考文献：
  名称：

  Microwave-assisted synthesis of unnatural amino acids

  摘要：

  Microwave irradiation has been proven to be a useful tool in the rapid assembly of racemic unnatural amino acids in only two steps. Additional benefits of this methodology are the commercial availability of the inexpensive starting materials and the high yields and high purities of the final amino acid products. (c) 2008 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2008.09.025

文献信息

• [EN] BICYCLIC MELANOCORIN-SPECIFIC COMPOUNDS<br/>[FR] COMPOSES BICYCLIQUES SPECIFIQUES DE LA MELANOCORTINE
  申请人：PALATIN TECHNOLOGIES INC

  公开号：WO2005079574A1

  公开（公告）日：2005-09-01

  Melanocortin receptor-specific bicyclic compounds having the structure (I) and stereoisomer and pharmaceutically acceptable salts thereof, where R1, R2, R3 X and z are as described in the specification, which are agonists, antagonists or mixed agonists and antagonists at one or more melanocortin receptors, and having utility in the treatment of melanocortin receptor­related disorders and conditions. Pharmaceutical compositions containing a compound of structure (I) and methods relating to the use thereof are also disclosed.

  具有结构（I）和其立体异构体以及药学上可接受的盐的黑色素皮质素受体特异性双环化合物，其中R1、R2、R3、X和z如规范中所述，这些化合物是一种或多种黑色素皮质素受体的激动剂、拮抗剂或混合激动剂和拮抗剂，并且在治疗黑色素皮质素受体相关疾病和症状方面具有用途。还公开了含有结构（I）化合物的药物组合物和与其使用相关的方法。
• [EN] PROTEOGLYCAN MIMETICS FOR ENHANCED WOUND HEALING, ANGIOGENESIS, AND VASCULAR REPAIR<br/>[FR] MIMÉTIQUES DE PROTÉOGLYCANE POUR UNE CICATRISATION, UNE ANGIOGENÈSE ET UNE RÉPARATION VASCULAIRE AMÉLIORÉES
  申请人：UNIV CALIFORNIA

  公开号：WO2019195780A1

  公开（公告）日：2019-10-10

  The present disclosure provides pro-angiogenic proteoglycan mimetics that can provide a provisional, pro-angiogenic scaffold to support tissue regeneration while limiting systemic exposure to VEGF activity. These mimetics can protect a collagen matrix from rapid degradation, and in conjunction with EPCs promote angiogenesis in order to accelerate ischemic wound healing. For example, the provided compounds can be delivered from the end of a catheter following balloon angioplasty to coat the collagen exposed areas, prevent platelet binding and thrombosis, support capture of EPCs from blood to facilitate reendothelialization, and reduce late-lumen loss (neointimal hyperplasia).

  本公开提供了促血管生成的蛋白聚糖类似物，可以提供一个暂时的、促血管生成的支架，支持组织再生，同时限制系统暴露于VEGF活性。这些类似物可以保护胶原基质免受快速降解，并与EPCs一起促进血管生成，以加速缺血性伤口愈合。例如，所提供的化合物可以从导管的末端输送，经过球囊扩张后涂覆暴露的胶原区域，防止血小板结合和血栓形成，支持从血液中捕获EPCs以促进再内皮化，减少晚期腔隙损失（内膜增生）。
• Substituted melanocortin receptor-specific piperazine compounds
  申请人：Sharma D. Shubh

  公开号：US20050176728A1

  公开（公告）日：2005-08-11

  Melanocortin receptor-specific compounds of the general formulas and pharmaceutically acceptable salts thereof, where J is a substituted or unsubstituted monocyclic or bicyclic ring structure, L is a linker, W is a heteroatom unit with at least one cationic center, hydrogen bond donor or hydrogen bond acceptor, Q includes a substituted or unsubstituted aromatic carbocyclic ring, R 6 , R 7 , y and z are as defined in the specification, and the carbon atom marked with an asterisk can have any stereochemical configuration, and optionally with one or two additional ring substituents as defined, which compounds bind to one or more melanocortin receptors and are optionally an agonist, a partial agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist, and may be employed for treatment of one or more melanocortin receptor-associated conditions or disorders, and methods for the use of the compounds of the invention.

  具有以下一般式及其药学上可接受的盐的黑色素皮质素受体特异性化合物，其中J是取代或未取代的单环或双环环结构，L是连接子，W是具有至少一个阳离子中心、氢键供体或氢键受体的杂原子单元，Q包括取代或未取代的芳香环烷基环，R6、R7、y和z如规范中所定义，标有星号的碳原子可以具有任何立体化学构型，并且可选择具有一个或两个附加环取代基，所述化合物结合一个或多个黑色素皮质素受体，可选择是激动剂、部分激动剂、拮抗剂、反向激动剂或反向激动剂的拮抗剂，并可用于治疗一个或多个黑色素皮质素受体相关的疾病或症状，并提供了使用该发明化合物的方法。
• Peptidomimetics selective for the somatostatin receptor subtypes 1 and/or 4
  申请人：Tomperi Jussi

  公开号：US20100048549A1

  公开（公告）日：2010-02-25

  The invention relates to (hetero)arylsulfonylamino based peptidomimetics of formula (I), wherein A, D, E, J, Q1 R1, R2, R3, p and j are defined as disclosed, or a pharmaceutically acceptable salt or ester thereof. Compounds of formula (I) possess high affinity and selectivity for the somatostatin receptor subtypes sst 1 and/or sst 4 and can be used for the treatment or diagnosis of diseases or conditions wherein sst 1 and/or sst 4 agonists or antagonists are indicated to be useful.

  本发明涉及公式（I）中基于（杂）芳基磺酰氨基的肽类类似物，其中A，D，E，J，Q1，R1，R2，R3，p和j如所述定义，或其药学上可接受的盐或酯。公式（I）化合物具有对生长抑素受体亚型sst1和/或sst4的高亲和力和选择性，并可用于治疗或诊断sst1和/或sst4激动剂或拮抗剂被认为有用的疾病或情况。
• Novel non selective analogs of somatostatin
  申请人：ITALFARMACO S.p.A.

  公开号：EP2067786A1

  公开（公告）日：2009-06-10

  The present invention relates to a new class of cyclopeptides of formula (I), reported here below, which are non-selective functional analogues of somatostatin.

  本发明涉及一种新的环肽类别，其化学式为(I)，如下所述，它们是生长抑素的非选择性功能类似物。