Development of Proneurogenic, Neuroprotective Small Molecules was written by MacMillan, Karen S.;Naidoo, Jacinth;Liang, Jue;Melito, Lisa;Williams, Noelle S.;Morlock, Lorraine;Huntington, Paula J.;Estill, Sandi Jo;Longgood, Jamie;Becker, Ginger L.;McKnight, Steven L.;Pieper, Andrew A.;De Brabander, Jef K.;Ready, Joseph M.. And the article was included in Journal of the American Chemical Society in 2011.Category: indole-building-block This article mentions the following:
Degeneration of the hippocampus is associated with Alzheimer’s disease and occurs very early in the progression of the disease. Current options for treating the cognitive symptoms associated with Alzheimer’s are inadequate, giving urgency to the search for novel therapeutic strategies. Pharmacol. agents that safely enhance hippocampal neurogenesis may provide new therapeutic approaches. We discovered the first synthetic mol., named P7C3, which protects newborn neurons from apopotic cell death, and thus promotes neurogenesis in mice and rats in the subgranular zone of the hippocampal dentate gyrus, the site of normal neurogenesis in adult mammals. We describe the results of a medicinal chem. campaign to optimize the potency, toxicity profile, and stability of P7C3. Systematic variation of nearly every position of the lead compound revealed elements conducive toward increases in activity and regions subject to modification. We have discovered compounds that are orally available, nontoxic, stable in mice, rats, and cell culture, and capable of penetrating the blood-brain barrier. The most potent compounds are active at nanomolar concentrations Finally, we have identified derivatives that may facilitate mode-of-action studies through affinity chromatog. or photo-crosslinking. In the experiment, the researchers used many compounds, for example, 5-Bromo-2,3-dimethyl-1H-indole (cas: 4583-55-5Category: indole-building-block).
5-Bromo-2,3-dimethyl-1H-indole (cas: 4583-55-5) belongs to indole derivatives. In addition to tryptophan, indigo, and indoleacetic acid, numerous compounds obtainable from plant or animal sources contain the indole molecular structure. Due to this activity, the indole ring system has become an important component or intermediate in the synthesis of heterocycles.Category: indole-building-block
Referemce:
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