Development of Novel Mitochondrial Pyruvate Carrier Inhibitors to Treat Hair Loss was written by Liu, Xiaoguang;Flores, Aimee A.;Situ, Lisa;Gu, Wen;Ding, Hui;Christofk, Heather R.;Lowry, William E.;Jung, Michael E.. And the article was included in Journal of Medicinal Chemistry in 2021.HPLC of Formula: 827-01-0 This article mentions the following:
Herein, we report the synthesis and evaluation of novel analogs of UK-5099 both in vitro and in vivo for the development of mitochondrial pyruvate carrier (MPC) inhibitors to treat hair loss. A comprehensive understanding of the structure-activity relationship was obtained by varying four positions of the hit compound, namely, the alkyl group on the N1 position, substituents on the indole core, various aromatic and heteroaromatic core structures, and various Michael acceptors. The major discovery was that the inhibitors with a 3,5-bis(trifluoromethyl)benzyl group at the N1 position were shown to have much better activity than JXL001 (UK-5099) to increase cellular lactate production Addnl., analog JXL069, possessing a 7-azaindole heterocycle, was also shown to have significant MPC inhibition activity, which further increases the chem. space for drug design. Finally, more than 10 analogs were tested on shaved mice by topical treatment and promoted obvious hair growth on mice. In the experiment, the researchers used many compounds, for example, 5-Chloroindole-3-carboxaldehyde (cas: 827-01-0HPLC of Formula: 827-01-0).
5-Chloroindole-3-carboxaldehyde (cas: 827-01-0) 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. 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.HPLC of Formula: 827-01-0
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