29876-14-0
29876-14-0 结构式
基本信息
尼可曲朵
N-(2-(1H-吲哚-3-基)乙基)烟酰胺
Nicotredole
N-[2-(3-indolyl)ethyl]nicotinamide
N-(2-(1H-Indol-3-yl)ethyl)nicotinaMide
N-[2-(1H-indol-3-yl)ethyl]pyridine-3-carboxamide
3-Pyridinecarboxamide, N-[2-(1H-indol-3-yl)ethyl]-
物理化学性质
制备方法
59-67-6
61-54-1
29876-14-0
一般步骤：向烟酸（0.5 mmol）、三乙胺（1.2 mmol）、HOBT（0.6 mmol）和EDCI（0.6 mmol）在二氯甲烷（8 mL）中的溶液中加入色胺（0.5 mmol）。将反应混合物在室温下搅拌过夜，随后在减压下蒸发除去二氯甲烷。将残余物溶解于乙酸乙酯（10 mL）中，并依次用10%碳酸氢钠水溶液（3×10 mL）和水（10 mL）洗涤。有机相用无水硫酸钠干燥，并在减压下浓缩至干。残余物通过硅胶柱色谱纯化，使用二氯甲烷/甲醇混合溶剂作为洗脱剂，得到纯固体产物N-(2-(1H-吲哚-3-基)乙基)烟酰胺（4a）。白色固体；产率72%；1H NMR（500 MHz, DMSO-d6）δ 10.84（s, 1H）, 9.02（d, J = 1.3 Hz, 1H）, 8.82（t, J = 5.0 Hz, 1H）, 8.72（dd, J = 4.6, 1.3 Hz, 1H）, 8.20（d, J = 7.9 Hz, 1H）, 7.60（d, J = 7.8 Hz, 1H）, 7.52（dd, J = 7.6, 5.1 Hz, 1H）, 7.37（d, J = 8.1 Hz, 1H）, 7.21（s, 1H）, 7.09（t, J = 7.5 Hz, 1H）, 7.00（t, J = 7.4 Hz, 1H）, 3.59（dd, J = 13.6, 6.9 Hz, 2H）, 3.00（t, J = 7.4 Hz, 2H）。
参考文献：
[1] ACS Medicinal Chemistry Letters, 2014, vol. 5, # 8, p. 884 - 888
[2] Patent: CN105198786, 2018, B. Location in patent: Paragraph 0111; 0138; 0139
[3] European Journal of Medicinal Chemistry, 2015, vol. 103, p. 302 - 311
[4] Journal of the American Chemical Society, 2004, vol. 126, # 40, p. 12897 - 12906
[5] Tetrahedron Asymmetry, 2010, vol. 21, # 16, p. 1988 - 1992
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2025/05/22 | HY-137394 | 尼可曲朵 Nicotredole | 29876-14-0 | 1 mg | 216元 |
| 2025/05/22 | HY-137394 | 尼可曲朵 Nicotredole | 29876-14-0 | 5mg | 496元 |
| 2025/05/22 | HY-137394 | 尼可曲朵 Nicotredole | 29876-14-0 | 10mg | 745元 |
常见问题列表
Nicotredole inhibits prostaglandin synthetase activity in vitro.
Nicotredole produces antiinflammatory effects in carrageenin-induced rat paw oedema.
Nicotredole reverses pyrogen-induced hyperthermia in rats, elicits analgesic effects in rats, prolongs the time of hexobarbital sleep in rats and inhibits locomotor activity in rats and mice.
Nicotredole (i.p.) has LD50s of 1260 mg/kg and 1980 mg/kg for male rats and male mice, respectively.
Nicotredole (p.o.) has LD50s of 8.5 g/kg and 9.3 g/kg for male rats and male mice, respectively.
Nicotredole (25 mg/kg; p.o. or i.p.) undergoes fast absorption (t
1/2
=4.92-17.5 min) and elimination (t
1/2
=55.72-74.52 min), can reach C
max
(11-13 μg/cm
3
) after 30 min, and gives AUC values in the range of 21.40-27.30 (μg•h/cm
3
).