- Synthesis and pharmacological investigation of aralkyl diamine derivatives as potential triple reuptake inhibitors
-
A series of aralkyl diamine derivatives were designed, synthesized, and evaluated for their triple reuptake inhibitory abilities. Compounds 18c (5-HT, NE, DA, IC50 = 389, 69, 238 nM), 36a (5-HT, NE, DA, IC50 = 378, 477, 247 nM), and
- Zheng, Yong-Yong,Weng, Zhi-Jie,Xie, Peng,Zhu, Mei-Yu,Xing, Long-Xuan,Li, Jian-Qi
-
p. 219 - 234
(2014/09/17)
-
- ARALKYL DIAMINE DERIVATIVES AND USES THEREOF AS ANTIDEPRESSANT
-
Aralkyl diamine derivative of the following formula, pharmaceutically acceptable salts or uses thereof as antidepressants. The derivatives have triplex inhibiting activities of the reuptake of 5-HT, dopamine and noradrenalin, which can be administered to the patients in need of such treatment in the form of compositions orally or injectedly et al.
- -
-
Paragraph 0030; 0049
(2013/03/28)
-
- Synthesis and pharmacological evaluation of 3-aryl-3-azolylpropan-1-amines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors
-
A series of 3-aryl-3-azolylpropan-1-amines was prepared and screened for its capability of inhibiting monoamine reuptake. Analogs with nanomolar potency, good human in vitro microsomal stability, and low drug-drug interaction potential were described. In
- Lee, Ki-Ho,Park, Chun-Eung,Min, Kyung-Hyun,Shin, Yong-Je,Chung, Coo-Min,Kim, Hui-Ho,Yoon, Hae-Jeoung,Won-Kim,Ryu, Eun-Ju,Shin, Yu-Jin,Nam, Hyun-Sik,Cho, Jeong-Woo,Lee, Hee-Yoon
-
scheme or table
p. 5567 - 5571
(2010/12/29)
-
- Scaffold oriented synthesis. Part 2: Design, synthesis and biological evaluation of pyrimido-diazepines as receptor tyrosine kinase inhibitors
-
We report the discovery of the pyrimido-diazepine scaffolds as novel adenine mimics. Structure-based design led to the discovery of analogs with potent inhibitory activity against receptor tyrosine kinases, such as KDR, Flt3 and c-Kit. Compound 14 exhibited low nanomolar KDR enzymatic and cellular potencies (IC50 = 9 and 52 nM, respectively).
- Gracias, Vijaya,Ji, Zhiqin,Akritopoulou-Zanze, Irini,Abad-Zapatero, Cele,Huth, Jeffrey R.,Song, Danying,Hajduk, Philip J.,Johnson, Eric F.,Glaser, Keith B.,Marcotte, Patrick A.,Pease, Lori,Soni, Nirupama B.,Stewart, Kent D.,Davidsen, Steven K.,Michaelides, Michael R.,Djuric, Stevan W.
-
p. 2691 - 2695
(2008/12/21)
-
- Anticonvulsant activity of semicarbazone derivatives of Mannich bases
-
A series of semicarbazones of semicarbazide/p-chlorophenyl semicarbazide and Mannich bases of acetophenone/p-chloroacetophenone has been synthesized and their anticonvulsant activity screened against MES and scPTZ test. p-Chlorophenyl semi-carbazone of N,N-dimethylaminopropiophenone has been found to be the most active in all these tests.
- Pandeya,Sowmyalakshmi,Panda,Pandeya,Stables
-
p. 2657 - 2661
(2007/10/03)
-
- A CONVENIENT SYNTHESIS OF 1H-1,2,4-TRIAZOL-1-YL-PROPAN-3-ONE DERIVATIVES BY MODIFIED MANNICH REACTION
-
1H-1,2,4-Triazol-yl-propan-3-ones were synthesized regioselectively using a modified Mannich reaction.Reactions of enones and Mannich bases with imidazole are also described.
- Takahashi, Kimio,Shimizu, Sumio,Ogata, Masaru
-
p. 809 - 816
(2007/10/02)
-