2-ethyl-1(3)H-imidazo[4,5-c]pyridine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并吡啶类
• 英文名称: 2-ethyl-1(3)H-imidazo[4,5-c]pyridine
• 英文别名: 2-Aethyl-1(3)H-imidazo[4,5-c]pyridin；2-Ethyl-1H-imidazo[4,5-c]pyridine；2-ethyl-3H-imidazo[4,5-c]pyridine
• 化学式: C₈H₉N₃
• 分子量: 147.18
• InChiKey: OGAVLUMPEJJADN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  41.6
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-ethyl-1(3)H-imidazo[4,5-c]pyridine 在 potassium carbonate 、 sodium iodide 、 sodium hydroxide 作用下， 以 N,N-二甲基甲酰胺 、 丙酮 为溶剂， 生成 2-ethyl-1-(4-phenoxybutyl)-1H-imidazo[4,5-c]pyridine
  参考文献：
  名称：

  Identification of Phenoxyalkylbenzimidazoles with Antitubercular Activity

  摘要：

  We conducted an evaluation of the phenoxyalkylbenzimidazole series based on the exemplar 2-ethyl-1-(3-phenoxypropyl)-1H-benzo[d]imidazole for its antitubercular activity. Four segments of the molecule were examined systematically to define a structure activity relationship with respect to biological activity. Compounds had submicromolar activity against Mycobacterium tuberculosis; the most potent compound had a minimum inhibitory concentration (MIC) of 52 nM and was not cytotoxic against eukaryotic cells (selectivity index = 523). Compounds were selective for M. tuberculosis over other bacterial species, including the closely related Mycobacterium smegmatis. Compounds had a bacteriostatic effect against aerobically grown, replicating M. tuberculosis, but were bactericidal against nonreplicating bacteria. Representative compounds had moderate to high permeability in MDCK cells, but were rapidly metabolized in rodents and human liver microsomes, suggesting the possibility of rapid in vivo hepatic clearance mediated by oxidative metabolism. These results indicate that the readily synthesized phenoxyalkylbenzimidazoles are a promising class of potent and selective antitubercular agents, if the metabolic liability can be solved.

  DOI：

  10.1021/acs.jmedchem.5b00546
• 作为产物：
  描述：

  3,4-二氨基吡啶 、 丙酸 在 PPA 作用下， 反应 4.0h， 生成 2-ethyl-1(3)H-imidazo[4,5-c]pyridine
  参考文献：
  名称：

  抗病毒的2,5-二取代的咪唑并[4,5-c]吡啶类：从抗瘟病毒到抗丙型肝炎病毒活性。

  摘要：

  描述了新型的丙型肝炎病毒抑制剂[取代的2-（2-氟苯基）-5H-咪唑并[4,5-c]吡啶]。导致在抗瘟病毒的先导化合物1（5-[（4-溴苯基）甲基] -2-苯基-5H-咪唑并[4,5-c]吡啶）的2-苯基取代基的2位引入氟在亚基因组复制子系统中具有针对HCV的选择性活性的类似物。

  DOI：

  10.1016/j.bmcl.2006.10.039

文献信息

• [EN] HINDERED DISULFIDE DRUG CONJUGATES<br/>[FR] CONJUGUÉS MÉDICAMENTEUX À PONT DISULFURE ENCOMBRÉ
  申请人：GENENTECH INC

  公开号：WO2017064675A1

  公开（公告）日：2017-04-20

  The invention relates generally to disulfide drug conjugates wherein a linker comprising a sulfur-bearing carbon atom substituted with at least one hydrocarbyl or substituted hydrocarbyl is conjugated by a disulfide bond to a cysteine sulfur atom of a targeting carrier, and wherein the linker is further conjugated to a drug moiety. The invention further relates to activated linker-drug conjugates suitable for conjugation to a targeting carrier by a disulfide bond. The invention further relates to methods for preparing hindered disulfide drug conjugates.

  该发明一般涉及二硫键药物偶联物，其中含有至少一个被至少一个碳氢化合物或取代碳氢化合物所取代的含硫碳原子的连接剂通过二硫键与靶向载体的半胱氨酸硫原子偶联，并且连接剂进一步与药物部分偶联。该发明进一步涉及适合通过二硫键与靶向载体偶联的活化连接剂-药物偶联物。该发明还进一步涉及制备受阻二硫键药物偶联物的方法。
• Dihydrothienopyrimidines for the Treatment of Inflammatory Diseases
  申请人：Pouzet Pascale

  公开号：US20080096882A1

  公开（公告）日：2008-04-24

  The invention relates to new dihydrothienopyrimidine of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein X is SO or SO 2 , but preferably SO, and wherein R 1 , R 2 and R 3 have the meanings given in the description, and which are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.

  该发明涉及公式1的新二氢噻吡嘧啶，以及其药理学上可接受的盐、对映体、旋光异构体、消旋体、水合物或溶剂合物，其中X为SO或SO2，但最好为SO，R1、R2和R3在描述中给出的含义，并且适用于治疗呼吸道或胃肠道疾病、关节、皮肤或眼睛的炎症性疾病、外周或中枢神经系统疾病或癌症，以及含有这些化合物的药物组合物。
• PROCESS FOR PREPARING [(3-HYDROXYPYRIDINE-2-CARBONYL)AMINO]ALKANOIC ACIDS, ESTERS AND AMIDES
  申请人：Akebia Therapeutics, Inc.

  公开号：US20150361043A1

  公开（公告）日：2015-12-17

  Disclosed are processes for preparing [(3-hydroxypyridine-2-carbonyl)amino]-alkanoic acids, derivatives, inter alia, 5-aryl substituted and 5-heteroaryl substituted [(3-hydroxypyridine-2-carbonyl]amino}acetic acids. Further disclosed are methods for making prodrugs of [(3-hydroxypyridine-2-carbonyl)-amino]acetic acids, for example, [(3-hydroxypyridine-2-carbonyl]amino}acetic acid esters and [3-hydroxypyridine-2-carbonyl]amino}acetic acid amides. The disclosed compounds are useful as prolyl hydroxylase inhibitors or for treating conditions wherein prolyl hydroxylase inhibition is desired.

  本发明涉及制备[(3-羟基吡啶-2-羧基)氨基]-烷基酸，其衍生物，包括5-芳基取代和5-杂环芳基取代的[(3-羟基吡啶-2-羧基)氨基]乙酸。此外，还公开了制备[(3-羟基吡啶-2-羧基)氨基]乙酸的前药的方法，例如[(3-羟基吡啶-2-羧基)氨基]乙酸酯和[3-羟基吡啶-2-羧基]氨基}乙酸酰胺。所公开的化合物可用作脯氨酸羟化酶抑制剂或用于治疗需要脯氨酸羟化酶抑制的疾病。
• P38 KINASE INHIBITING AGENTS
  申请人：Sahoo Soumya P.

  公开号：US20090325953A1

  公开（公告）日：2009-12-31

  Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of asthma, COPD, ARDS, rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammation.

  化学式（I）或其药学上可接受的盐所描述的化合物：它们是p38的抑制剂，可用于治疗炎症，如哮喘、COPD、ARDS、类风湿关节炎、类风湿脊柱炎、骨关节炎、痛风性关节炎和其他关节炎症状；发炎的关节、湿疹、牛皮癣或其他炎症性皮肤状况，如晒伤；炎症性眼部状况，包括结膜炎；发热、疼痛和其他与炎症有关的状况。
• HETEROCYCLIC CETP INHIBITORS
  申请人：Wang Yufeng

  公开号：US20070135467A1

  公开（公告）日：2007-06-14

  Compounds of formula Ia and Ib wherein A, B, C and R 1 are described herein.

  本文描述的是化学式Ia和Ib的化合物，其中A、B、C和R1被定义。