- Synthesis and SAR of highly potent dual 5-HT1A and 5-HT 1B antagonists as potential antidepressant drugs
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Novel 5-HT1 autoreceptor ligands based on the N-4-aryl-piperazinyl-N′-ethyl-5,6,7,8-tetrahydropyrido[4′, 3′:4,5]thieno[2,3-d]pyrimidin-4(3H)-one core are described. Aiming at antidepressants with a novel mode of action our objective was to identify potent antagonists showing balanced affinities and high selectivity for the 5-HT 1A and 5-HT1B receptors. Strategies for the development of dual 5-HT1A and 5-HT1B antagonists based on 1 and 2 as leads and the corresponding results are discussed. Isoquinoline analogue 33 displayed high affinity and an antagonistic mode of action for the 5-HT 1A and the 5-HT1B receptors and was characterized further with respect to selectivity, electrically stimulated [3H]5-HT release and in vivo efficacy.
- Kling, Andreas,Lange, Udo E. W.,Mack, Helmut,Bakker, Margot H. M.,Drescher, Karla U.,Hornberger, Wilfried,Hutchins, Charles W.,Moeller, Achim,Mueller, Reinhold,Schmidt, Martin,Unger, Liliane,Wicke, Karsten,Schellhaas, Kurt,Steiner, Gerd
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Read Online
- Fe-Catalyzed Amination of (Hetero)Arenes with a Redox-Active Aminating Reagent under Mild Conditions
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A novel and efficient Fe-catalyzed direct C?H amination (NH2) of arenes is reported using a new redox-active aminating reagent. The reaction is simple, and can be performed under air, mild, and redox-neutral conditions. This protocol has a broad substrate scope and could be used in the late-stage modification of bioactive compounds. Mechanistic studies demonstrate that a radical pathway could be involved in this transformation.
- Liu, Jianzhong,Wu, Kai,Shen, Tao,Liang, Yujie,Zou, Miancheng,Zhu, Yuchao,Li, Xinwei,Li, Xinyao,Jiao, Ning
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supporting information
p. 563 - 567
(2017/01/18)
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- 2, 4- DI (PHENYLAMINO) PYRIMIDINES USEFUL IN THE TREATMENT OF NEOPLASTIC DISEASES, INFLAMMATORY AND IMMUNE SYSTEM DISORDERS
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Novel pyrimidine derivatives of formula (I), to processes for their production, their use as pharmaceuticals in the treatment of neoplastic diseases, inflammatory and immune system disorders and to pharmaceutical compositions comprising them.
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Page 138; 144
(2010/02/08)
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- Tricyclic furo-quinazolinones
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Anti-inflammatories and analgesics of the formula SPC1 Wherein X y is --OCH2 CH2 -- or --CH2 CH2 O--, R is lower alkyl, allyl or cycloalkylalkyl and R' is phenyl or phenyl monosubstituted by halo, alkyl, alkoxy
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