On May 10, 2012, Calderon, Felix; Vidal-Mas, Jaume; Burrows, Jeremy; de la Rosa, Juan Carlos; Jimenez-Diaz, Maria Belen; Mulet, Teresa; Prats, Sara; Solana, Jorge; Witty, Michael; Gamo, Francisco Javier; Fernandez, Esther published an article.Application In Synthesis of 6-Chloro-2,3-dihydro-1H-indole The title of the article was A Divergent SAR Study Allows Optimization of a Potent 5-HT2c Inhibitor to a Promising Antimalarial Scaffold. And the article contained the following:
From the 13 533 chem. structures published by GlaxoSmithKline in 2010, we identified 47 quality starting points for lead optimization. One of the most promising hits was the TCMDC-139046, a mol. presenting an indoline core, which is well-known for its anxiolytic properties by interacting with serotonin antagonist receptors 5-HT2. The inhibition of this target will complicate the clin. development of these compounds as antimalarials. Herein, we present the antimalarial profile of this series and our efforts to avoid interaction with this receptor, while maintaining a good antiparasitic potency. By using a double-divergent structure-activity relationship anal., we have obtained a novel lead compound harboring an indoline core. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Application In Synthesis of 6-Chloro-2,3-dihydro-1H-indole
The Article related to sar antimalaria 5ht antagonist indole, tres cantos antimalarial set, divergent sar, indoline, malaria, open-innovation, Pharmacology: Effects Of Antimicrobials and Parasiticides and other aspects.Application In Synthesis of 6-Chloro-2,3-dihydro-1H-indole
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Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles