Design, synthesis, and pharmacological profile of novel fused pyrazolo [4, 3-d] pyridine and pyrazolo [3, 4-b][1, 8] naphthyridine isosteres: A new class of potent and …
…, L Brazil-Más, NG Castro, WM Cintra…
Index: Barreiro, Eliezer J.; Camara, Celso A.; Verli, Hugo; Brazil-Mas, Leonora; Castro, Newton G.; Cintra, Wagner M.; Aracava, Yasco; Rodrigues, Carlos R.; Fraga, Carlos A. M. Journal of Medicinal Chemistry, 2003 , vol. 46, # 7 p. 1144 - 1152
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Citation Number: 83
Abstract
A new family of tacrine (THA) analogues (7-9, 12), containing the azaheterocyclic pyrazolo [4, 3-d] pyridine or pyrazolo [3, 4-b][1, 8] naphthyridine systems as isosteres of the quinoline ring of THA, has been synthesized. The compounds were tested in rat brain cholinesterases using Ellman's method, and all were fully efficacious in inhibiting the enzymes. Compounds 9 and 12b were the most potent against acetylcholinesterase (AChE), showing IC50 of 6.0 ...
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