A Divergent SAR Study Allows Optimization of a Potent 5-HT2c Inhibitor to a Promising Antimalarial Scaffold was written by 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. And the article was included in ACS Medicinal Chemistry Letters in 2012.Application In Synthesis of 5-Fluoroindoline This article mentions 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. In the experiment, the researchers used many compounds, for example, 5-Fluoroindoline (cas: 2343-22-8Application In Synthesis of 5-Fluoroindoline).
5-Fluoroindoline (cas: 2343-22-8) belongs to indole derivatives. Indole, also called Benzopyrrole, a heterocyclic organic compound occurring in some flower oils, such as jasmine and orange blossom, in coal tar, and in fecal matter. It is used in perfumery and in making tryptophan, an essential amino acid, and indoleacetic acid (heteroauxin), a hormone that promotes the development of roots in plant cuttings.Application In Synthesis of 5-Fluoroindoline
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Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles