CAS: 868273-06-7; 5-Chloro-3-Ethyl-N-[2-(4-Piperidin-1-Ylphenyl)Ethyl]-1H-Indole-2-Carboxamide

该化合物是合成有机化合物,其结构复杂,包括一个非单极核,一个氯替代体和一个管状动物.该化合物通常具有与非单极衍生物有关的特性,例如潜在的生物活动,包括与各种受体或酶的相互作用.氯组的存在可能会影响其脂性与再活性,而乙基和管状物质组则能够加强其药理特征.该化合物可能溶于有机溶剂,并根据其特定功能组分,在水中具有中度至低溶性.其潜在用途可能包括药化学,特别是在针对...

英文名称5-Chloro-3-Ethyl-N-[2-(4-Piperidin-1-Ylphenyl)Ethyl]-1H-Indole-2-Carboxamide
中文名称5-氯-3-乙基-N-[2-[4-(1-哌啶基)苯基]乙基-1H-吲哚-2-甲酰胺
IUPAC名称5-chloro-3-ethyl-N-(4-(piperidin-1-yl)phenethyl)-1H-indole-2-carboxamide
CAS编号868273-06-7
MFCD编号:MFCD11045300
FDA UNII编号:7YW2S3Z2CB
分子式:C24H28ClN3O分子量:409.95
产品CID: 1871514
产品分类生物化工 → 抑制剂 → G蛋白偶联受体(GPCR & G Protein)

相似结构搜索
InChIKey: AHFZDNYNXFMRFQ-UHFFFAOYSA-N
1S/C24H28ClN3O/c1-2-20-21-16-18(25)8-11-22(21)27-23(20)24(29)26-13-12-17-6-9-19(10-7-17)28-14-4-3-5-15-28/h6-11,16,27H,2-5,12-15H2,1H3,(H,26,29)
计算化学: 氢键受体数2.0氢键供体数2.0可旋转键数6.0

物理性质

沸点660.3±55.0 °C at 760 mmHg
闪点353.2±31.5 °C
密度1.2±0.1 g/cm3
pKa:14.87±0.30(预测)
PSA:48.13
LogP:6.36
折射率1.635
蒸汽压0.0±2.0 mmHg at 25°C
溶解性水: <2mg/mL
外观形态白色粉末
储存条件2-8°C
产品应用该化合物用于研究作为CB1受体活性活性诱导器的不单分子-碳酸铵的结构性-活性关系.

上下游产品

2-[4-(piperidin-1-yl)phenyl]ethan-1-amine 5-chloro-3-ethyl-1H-indole-2-carboxylic acid ethyl 3-acetyl-5-chloro-1H-indole-2-carboxylate 2-(4-(piperidin-1-yl)phenethyl)isoindoline-1,3-dione

合成工艺路线路线简述

446830-67-7 + 38589-09-2 = 868273-06-7
反应条件:1.1 Reagents: Triethylamine,2-Phenylbenzoxazole Solvents: Dimethylformamide; 16 H,Rt
标题:Indole-2-Carboxamides As Allosteric Modulators Of The Cannabinoid Cb1 Receptor
作者:Piscitelli,Francesco; Et Al
参考文献:Journal Of Medicinal Chemistry 日期:2012 卷标:55(11) 页码:5627-5631]

94838-59-2 + 111-24-0 = 868273-06-7
反应条件:1.1 Reagents: Potassium Carbonate Solvents: Water; 20 Min,17 Psi,120 °C2.1 Reagents: Diisopropylethylamine,Bop Reagent Solvents: Dimethylformamide; 16 H,Rt
标题:Structure-Activity Relationships Of Substituted 1H-Indole-2-Carboxamides As Cb1 Receptor Allosteric Modulators
作者:Nguyen,Thuy; Et Al
参考文献:Bioorganic & Medicinal Chemistry 日期:2015 卷标:23(9) 页码:2195-2203]

124499-18-9 = 868273-06-7
反应条件:1.1 Reagents: Cesium Carbonate Catalysts: Tris(Dibenzylideneacetone)Dipalladium,X-Phos Solvents: Toluene; 12 H,110 °C; Cooled1.2 Reagents: Hydrochloric Acid Solvents: Water; Acidified,Cooled1.3 Reagents: Sodium Carbonate Solvents: Water; Neutralized,Rt2.1 Reagents: Hydrazine Hydrate (1:1) Solvents: Ethanol; 2 H,Reflux; Cooled2.2 Reagents: Hydrochloric Acid Solvents: Diethyl Ether,Water; Cooled2.3 Reagents: Sodium Carbonate Solvents: Water; Neutralized,Rt3.1 Reagents: Triethylamine,2-Phenylbenzoxazole Solvents: Dimethylformamide; 16 H,Rt
标题:Indole-2-Carboxamides As Allosteric Modulators Of The Cannabinoid Cb1 Receptor
作者:Piscitelli,Francesco; Et Al
参考文献:Journal Of Medicinal Chemistry 日期:2012 卷标:55(11) 页码:5627-5631]

1374964-61-0 = 868273-06-7
反应条件:1.1 Reagents: Trifluoroacetic Acid,Triethylsilane; 5 H,Rt1.2 Reagents: Sodium Carbonate Solvents: Water; Rt2.1 Reagents: Sodium Hydroxide Solvents: Ethanol,Water; 1.5 H,60 °C; Cooled2.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 2,Cooled3.1 Reagents: Triethylamine,2-Phenylbenzoxazole Solvents: Dimethylformamide; 16 H,Rt
标题:Indole-2-Carboxamides As Allosteric Modulators Of The Cannabinoid Cb1 Receptor
作者:Piscitelli,Francesco; Et Al
参考文献:Journal Of Medicinal Chemistry 日期:2012 卷标:55(11) 页码:5627-5631]

24424-99-5 + 24954-67-4 = 868273-06-7
反应条件:1.1 Reagents: Sodium Hydroxide Solvents: 1,4-Dioxane,Water; Rt -> 0 °C1.2 1 H,Rt1.3 Reagents: Hydrazine Hydrate (1:1) Catalysts: Nickel Solvents: Ethanol; 1 H,50 °C2.1 Reagents: Potassium Carbonate Solvents: Water; 20 Min,17 Psi,120 °C3.1 Reagents: Diisopropylethylamine,Bop Reagent Solvents: Dimethylformamide; 16 H,Rt
标题:Structure-Activity Relationships Of Substituted 1H-Indole-2-Carboxamides As Cb1 Receptor Allosteric Modulators
作者:Nguyen,Thuy; Et Al
参考文献:Bioorganic & Medicinal Chemistry 日期:2015 卷标:23(9) 页码:2195-2203]

141-97-9 = 868273-06-7
反应条件:1.1 Reagents: Sodium Ethoxide Solvents: Ethanol; 30 Min,Reflux; Reflux -> Rt1.2 30 Min,Rt; 12 H,Reflux; Reflux -> Rt1.3 Reagents: Hydrochloric Acid Solvents: Water; Neutralized2.1 Reagents: Sodium Acetate Solvents: Ethanol; 45 Min,Rt; Rt -> 0 °C2.2 3 H,Ph 5,0 - 5 °C2.3 Reagents: Sodium Bicarbonate Solvents: Water2.4 Reagents: Sulfuric Acid Solvents: Ethanol; 24 H,Reflux; Reflux -> Rt2.5 Reagents: Sodium Bicarbonate Solvents: Water; Neutralized3.1 Reagents: Potassium Hydroxide Solvents: 1,4-Dioxane,Water; 2 H,Reflux; Reflux -> Rt3.2 Reagents: Hydrochloric Acid Solvents: Water; Neutralized4.1 Reagents: 1-Hydroxybenzotriazole,Diisopropylethylamine,1-Ethyl-3-(3′-Dimethylaminopropyl)Carbodiimide Hydrochloride Solvents: N-Methyl-2-Pyrrolidone; Overnight,Rt
标题:Novel Electrophilic And Photoaffinity Covalent Probes For Mapping The Cannabinoid 1 Receptor Allosteric Site(S)
作者:Kulkarni,Pushkar M.; Et Al
参考文献:Journal Of Medicinal Chemistry 日期:2016 卷标:59(1) 页码:44-60]

4792-67-0 = 868273-06-7
反应条件:1.1 Reagents: Aluminum Chloride Solvents: 1,2-Dichloroethane; 5 Min,Cooled1.2 Solvents: 1,2-Dichloroethane; Cooled; 1 H,Reflux; Reflux -> Rt1.3 Solvents: Water; Cooled2.1 Reagents: Trifluoroacetic Acid,Triethylsilane; 3 H,Rt3.1 Reagents: Sodium Hydroxide Solvents: Ethanol,Water; 3 H,Reflux3.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 34.1 Reagents: Diisopropylethylamine,Bop Reagent Solvents: Dimethylformamide; 16 H,Rt
标题:Structure-Activity Relationships Of Substituted 1H-Indole-2-Carboxamides As Cb1 Receptor Allosteric Modulators
作者:Nguyen,Thuy; Et Al
参考文献:Bioorganic & Medicinal Chemistry 日期:2015 卷标:23(9) 页码:2195-2203]

4792-67-0 = 868273-06-7
反应条件:1.1 Reagents: Aluminum Chloride Solvents: 1,2-Dichloroethane; 2.5 H,Reflux; Cooled1.2 Reagents: Hydrochloric Acid Solvents: Water; Cooled2.1 Reagents: Trifluoroacetic Acid,Triethylsilane; 5 H,Rt2.2 Reagents: Sodium Carbonate Solvents: Water; Rt3.1 Reagents: Sodium Hydroxide Solvents: Ethanol,Water; 1.5 H,60 °C; Cooled3.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 2,Cooled4.1 Reagents: Triethylamine,2-Phenylbenzoxazole Solvents: Dimethylformamide; 16 H,Rt
标题:Indole-2-Carboxamides As Allosteric Modulators Of The Cannabinoid Cb1 Receptor
作者:Piscitelli,Francesco; Et Al
参考文献:Journal Of Medicinal Chemistry 日期:2012 卷标:55(11) 页码:5627-5631]

10517-21-2 = 868273-06-7
反应条件:1.1 Reagents: Hydrochloric Acid Solvents: Ethanol,Water; 18 H,Reflux2.1 Reagents: Aluminum Chloride Solvents: 1,2-Dichloroethane; 5 Min,Cooled2.2 Solvents: 1,2-Dichloroethane; Cooled; 1 H,Reflux; Reflux -> Rt2.3 Solvents: Water; Cooled3.1 Reagents: Trifluoroacetic Acid,Triethylsilane; 3 H,Rt4.1 Reagents: Sodium Hydroxide Solvents: Ethanol,Water; 3 H,Reflux4.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 35.1 Reagents: Diisopropylethylamine,Bop Reagent Solvents: Dimethylformamide; 16 H,Rt
标题:Structure-Activity Relationships Of Substituted 1H-Indole-2-Carboxamides As Cb1 Receptor Allosteric Modulators
作者:Nguyen,Thuy; Et Al
参考文献:Bioorganic & Medicinal Chemistry 日期:2015 卷标:23(9) 页码:2195-2203]

459-57-4 = 868273-06-7
反应条件:1.1 Reagents: Potassium Carbonate Solvents: N-Methyl-2-Pyrrolidone; 12 H,135 °C2.1 Catalysts: Ammonium Acetate Solvents: Nitromethane; 2 H,Reflux3.1 Reagents: Sodium Borohydride Solvents: Methanol; 2 H,5 °C -> Rt3.2 Reagents: Ammonium Chloride Solvents: Water4.1 Reagents: Nickel Dichloride Solvents: Methanol,Tetrahydrofuran; 45 Min,Rt; Rt -> -5 °C4.2 Reagents: Sodium Borohydride; -5 °C; 3 H,-5 °C -> Rt4.3 Reagents: Ammonium Chloride Solvents: Water5.1 Reagents: 1-Hydroxybenzotriazole,Diisopropylethylamine,1-Ethyl-3-(3′-Dimethylaminopropyl)Carbodiimide Hydrochloride Solvents: N-Methyl-2-Pyrrolidone; Overnight,Rt
标题:Novel Electrophilic And Photoaffinity Covalent Probes For Mapping The Cannabinoid 1 Receptor Allosteric Site(S)
作者:Kulkarni,Pushkar M.; Et Al
参考文献:Journal Of Medicinal Chemistry 日期:2016 卷标:59(1) 页码:44-60]

446830-67-7 + 38589-09-2 = 868273-06-7
反应条件:1.1 Reagents: 1-Hydroxybenzotriazole,Diisopropylethylamine,1-Ethyl-3-(3′-Dimethylaminopropyl)Carbodiimide Hydrochloride Solvents: N-Methyl-2-Pyrrolidone; Overnight,Rt
标题:Novel Electrophilic And Photoaffinity Covalent Probes For Mapping The Cannabinoid 1 Receptor Allosteric Site(S)
作者:Kulkarni,Pushkar M.; Et Al
参考文献:Journal Of Medicinal Chemistry 日期:2016 卷标:59(1) 页码:44-60]

446830-67-7 + 1377838-24-8 = 868273-06-7
反应条件:1.1 Reagents: Diisopropylethylamine,Bop Reagent Solvents: Dimethylformamide; 16 H,Rt
标题:Structure-Activity Relationships Of Substituted 1H-Indole-2-Carboxamides As Cb1 Receptor Allosteric Modulators
作者:Nguyen,Thuy; Et Al
参考文献:Bioorganic & Medicinal Chemistry 日期:2015 卷标:23(9) 页码:2195-2203]

1377838-23-7 = 868273-06-7
反应条件:1.1 Reagents: Potassium Hydroxide Solvents: 1,4-Dioxane,Water; 2 H,Reflux; Reflux -> Rt1.2 Reagents: Hydrochloric Acid Solvents: Water; Neutralized2.1 Reagents: 1-Hydroxybenzotriazole,Diisopropylethylamine,1-Ethyl-3-(3′-Dimethylaminopropyl)Carbodiimide Hydrochloride Solvents: N-Methyl-2-Pyrrolidone; Overnight,Rt
标题:Novel Electrophilic And Photoaffinity Covalent Probes For Mapping The Cannabinoid 1 Receptor Allosteric Site(S)
作者:Kulkarni,Pushkar M.; Et Al
参考文献:Journal Of Medicinal Chemistry 日期:2016 卷标:59(1) 页码:44-60]

1377838-23-7 = 868273-06-7
反应条件:1.1 Reagents: Sodium Hydroxide Solvents: Ethanol,Water; 3 H,Reflux1.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 32.1 Reagents: Diisopropylethylamine,Bop Reagent Solvents: Dimethylformamide; 16 H,Rt
标题:Structure-Activity Relationships Of Substituted 1H-Indole-2-Carboxamides As Cb1 Receptor Allosteric Modulators
作者:Nguyen,Thuy; Et Al
参考文献:Bioorganic & Medicinal Chemistry 日期:2015 卷标:23(9) 页码:2195-2203]

1377838-23-7 = 868273-06-7
反应条件:1.1 Reagents: Sodium Hydroxide Solvents: Ethanol,Water; 1.5 H,60 °C; Cooled1.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 2,Cooled2.1 Reagents: Triethylamine,2-Phenylbenzoxazole Solvents: Dimethylformamide; 16 H,Rt
标题:Indole-2-Carboxamides As Allosteric Modulators Of The Cannabinoid Cb1 Receptor
作者:Piscitelli,Francesco; Et Al
参考文献:Journal Of Medicinal Chemistry 日期:2012 卷标:55(11) 页码:5627-5631]

1377838-25-9 = 868273-06-7
反应条件:1.1 Reagents: Hydrazine Hydrate (1:1) Solvents: Ethanol; 2 H,Reflux; Cooled1.2 Reagents: Hydrochloric Acid Solvents: Diethyl Ether,Water; Cooled1.3 Reagents: Sodium Carbonate Solvents: Water; Neutralized,Rt2.1 Reagents: Triethylamine,2-Phenylbenzoxazole Solvents: Dimethylformamide; 16 H,Rt
标题:Indole-2-Carboxamides As Allosteric Modulators Of The Cannabinoid Cb1 Receptor
作者:Piscitelli,Francesco; Et Al
参考文献:Journal Of Medicinal Chemistry 日期:2012 卷标:55(11) 页码:5627-5631]

= 868273-06-7
反应条件:1.1 Reagents: Nickel Dichloride Solvents: Methanol,Tetrahydrofuran; 45 Min,Rt; Rt -> -5 °C1.2 Reagents: Sodium Borohydride; -5 °C; 3 H,-5 °C -> Rt1.3 Reagents: Ammonium Chloride Solvents: Water2.1 Reagents: 1-Hydroxybenzotriazole,Diisopropylethylamine,1-Ethyl-3-(3′-Dimethylaminopropyl)Carbodiimide Hydrochloride Solvents: N-Methyl-2-Pyrrolidone; Overnight,Rt
标题:Novel Electrophilic And Photoaffinity Covalent Probes For Mapping The Cannabinoid 1 Receptor Allosteric Site(S)
作者:Kulkarni,Pushkar M.; Et Al
参考文献:Journal Of Medicinal Chemistry 日期:2016 卷标:59(1) 页码:44-60]

1374964-61-0 = 868273-06-7
反应条件:1.1 Reagents: Trifluoroacetic Acid,Triethylsilane; 3 H,Rt2.1 Reagents: Sodium Hydroxide Solvents: Ethanol,Water; 3 H,Reflux2.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 33.1 Reagents: Diisopropylethylamine,Bop Reagent Solvents: Dimethylformamide; 16 H,Rt
标题:Structure-Activity Relationships Of Substituted 1H-Indole-2-Carboxamides As Cb1 Receptor Allosteric Modulators
作者:Nguyen,Thuy; Et Al
参考文献:Bioorganic & Medicinal Chemistry 日期:2015 卷标:23(9) 页码:2195-2203]

1446648-75-4 = 868273-06-7
反应条件:1.1 Reagents: Sodium Borohydride Solvents: Methanol; 2 H,5 °C -> Rt1.2 Reagents: Ammonium Chloride Solvents: Water2.1 Reagents: Nickel Dichloride Solvents: Methanol,Tetrahydrofuran; 45 Min,Rt; Rt -> -5 °C2.2 Reagents: Sodium Borohydride; -5 °C; 3 H,-5 °C -> Rt2.3 Reagents: Ammonium Chloride Solvents: Water3.1 Reagents: 1-Hydroxybenzotriazole,Diisopropylethylamine,1-Ethyl-3-(3′-Dimethylaminopropyl)Carbodiimide Hydrochloride Solvents: N-Methyl-2-Pyrrolidone; Overnight,Rt
标题:Novel Electrophilic And Photoaffinity Covalent Probes For Mapping The Cannabinoid 1 Receptor Allosteric Site(S)
作者:Kulkarni,Pushkar M.; Et Al
参考文献:Journal Of Medicinal Chemistry 日期:2016 卷标:59(1) 页码:44-60]

1540-28-9 + 2028-74-2 = 868273-06-7
反应条件:1.1 Reagents: Sodium Acetate Solvents: Ethanol; 45 Min,Rt; Rt -> 0 °C1.2 3 H,Ph 5,0 - 5 °C1.3 Reagents: Sodium Bicarbonate Solvents: Water1.4 Reagents: Sulfuric Acid Solvents: Ethanol; 24 H,Reflux; Reflux -> Rt1.5 Reagents: Sodium Bicarbonate Solvents: Water; Neutralized2.1 Reagents: Potassium Hydroxide Solvents: 1,4-Dioxane,Water; 2 H,Reflux; Reflux -> Rt2.2 Reagents: Hydrochloric Acid Solvents: Water; Neutralized3.1 Reagents: 1-Hydroxybenzotriazole,Diisopropylethylamine,1-Ethyl-3-(3′-Dimethylaminopropyl)Carbodiimide Hydrochloride Solvents: N-Methyl-2-Pyrrolidone; Overnight,Rt
标题:Novel Electrophilic And Photoaffinity Covalent Probes For Mapping The Cannabinoid 1 Receptor Allosteric Site(S)
作者:Kulkarni,Pushkar M.; Et Al
参考文献:Journal Of Medicinal Chemistry 日期:2016 卷标:59(1) 页码:44-60]

= 868273-06-7
反应条件:1.1 Reagents: Sulfuric Acid Solvents: Ethanol; 24 H,Reflux; Reflux -> Rt1.2 Reagents: Sodium Bicarbonate Solvents: Water; Neutralized2.1 Reagents: Potassium Hydroxide Solvents: 1,4-Dioxane,Water; 2 H,Reflux; Reflux -> Rt2.2 Reagents: Hydrochloric Acid Solvents: Water; Neutralized3.1 Reagents: 1-Hydroxybenzotriazole,Diisopropylethylamine,1-Ethyl-3-(3′-Dimethylaminopropyl)Carbodiimide Hydrochloride Solvents: N-Methyl-2-Pyrrolidone; Overnight,Rt
标题:Novel Electrophilic And Photoaffinity Covalent Probes For Mapping The Cannabinoid 1 Receptor Allosteric Site(S)
作者:Kulkarni,Pushkar M.; Et Al
参考文献:Journal Of Medicinal Chemistry 日期:2016 卷标:59(1) 页码:44-60]

10338-57-5 = 868273-06-7
反应条件:1.1 Catalysts: Ammonium Acetate Solvents: Nitromethane; 2 H,Reflux2.1 Reagents: Sodium Borohydride Solvents: Methanol; 2 H,5 °C -> Rt2.2 Reagents: Ammonium Chloride Solvents: Water3.1 Reagents: Nickel Dichloride Solvents: Methanol,Tetrahydrofuran; 45 Min,Rt; Rt -> -5 °C3.2 Reagents: Sodium Borohydride; -5 °C; 3 H,-5 °C -> Rt3.3 Reagents: Ammonium Chloride Solvents: Water4.1 Reagents: 1-Hydroxybenzotriazole,Diisopropylethylamine,1-Ethyl-3-(3′-Dimethylaminopropyl)Carbodiimide Hydrochloride Solvents: N-Methyl-2-Pyrrolidone; Overnight,Rt
标题:Novel Electrophilic And Photoaffinity Covalent Probes For Mapping The Cannabinoid 1 Receptor Allosteric Site(S)
作者:Kulkarni,Pushkar M.; Et Al
参考文献:Journal Of Medicinal Chemistry 日期:2016 卷标:59(1) 页码:44-60]

= 868273-06-7
反应条件:1.1 Reagents: Sodium Nitrite,Hydrochloric Acid Solvents: Water; 1 H,0 - 5 °C2.1 Reagents: Sodium Acetate Solvents: Ethanol; 45 Min,Rt; Rt -> 0 °C2.2 3 H,Ph 5,0 - 5 °C2.3 Reagents: Sodium Bicarbonate Solvents: Water2.4 Reagents: Sulfuric Acid Solvents: Ethanol; 24 H,Reflux; Reflux -> Rt2.5 Reagents: Sodium Bicarbonate Solvents: Water; Neutralized3.1 Reagents: Potassium Hydroxide Solvents: 1,4-Dioxane,Water; 2 H,Reflux; Reflux -> Rt3.2 Reagents: Hydrochloric Acid Solvents: Water; Neutralized4.1 Reagents: 1-Hydroxybenzotriazole,Diisopropylethylamine,1-Ethyl-3-(3′-Dimethylaminopropyl)Carbodiimide Hydrochloride Solvents: N-Methyl-2-Pyrrolidone; Overnight,Rt
标题:Novel Electrophilic And Photoaffinity Covalent Probes For Mapping The Cannabinoid 1 Receptor Allosteric Site(S)
作者:Kulkarni,Pushkar M.; Et Al
参考文献:Journal Of Medicinal Chemistry 日期:2016 卷标:59(1) 页码:44-60

📜4-溴苯乙酸甲酯置于tris-(Dibenzylideneacetone)Dipalladium(0),Lithium Aluminium Tetrahydride,(Benzotriazo-1-Yloxy)Tris(Dimethylamino)Phosphonium Hexafluorophosphate,Caesium Carbonate,一水合肼,三乙胺,三苯基膦,偶氮二甲酸二乙酯,2-二环己基磷-2,4,6-三异丙基联苯体系中,用四氢呋喃,乙醇,N,N-二甲基甲酰胺,甲苯作为反应溶剂,化学反应 22.0H,反应生成 5-氯-3-乙基-N-[2-[4-(1-哌啶基)苯基]乙基-1H-吲哚-2-甲酰胺
参考文献:吲哚-2-羧酰胺作为大麻素cb 1受体的变构调节剂
标题:吲哚-2-羧酰胺作为大麻素cb 1受体的变构调节剂
摘要:我们合成了新的n-苯乙基-1 H-吲哚-2-羧酰胺作为cb 1受体的变构调节剂的第一个sar研究.为了获得刺激作用,需要羧酰胺官能团的存在.cb 1的最大刺激活性是由分别在苯乙部分的4位带有二甲氨基或哌啶基的羧酰胺13(ec 50 = 50 Nm)和21(ec 50 = 90 Nm)发挥的.吲哚的5.
DOI:10.1021/jm201485C

海关参考信息

2902600000-乙苯
2903919090-氯苯
2912110000-甲醛
2924199090-其他无环酰胺
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主要参考文献

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合成参考文献

参考文献:10.1038/srep15453
摘要:Stornaiuolo M, Bruno A, Botta L, La Regina G, Cosconati S, Silvestri R, Marinelli L, Novellino E. Endogenous vs Exogenous Allosteric Modulators in GPCRs: A dispute for shuttling CB1 among different membrane microenvironments. Sci Rep. 2015 Oct 20;5():15453.