Discovery of a potent, orally available dual CysLT1 and CysLT2 antagonist with dicarboxylic acid was written by Itadani, Satoshi;Takahashi, Shinya;Ima, Masaki;Sekiguchi, Tetsuya;Aratani, Yoshiyuki;Egashira, Hiromu;Matsumura, Naoya;Inoue, Atsuto;Yonetomi, Yasuo;Fujita, Manabu;Nakayama, Yoshisuke;Takeuchi, Jun. And the article was included in Bioorganic & Medicinal Chemistry in 2015.Recommanded Product: 89245-41-0 This article mentions the following:
A potent, orally available dual CysLT1 and CysLT2 receptor antagonist with a dicarboxylic acid is described. 4-(3-(Carboxymethyl)-4-{(E)-2-[4-(4-phenoxybutoxy)phenyl]vinyl}-1H-indol-1-yl)butanoic acid (15: ONO-4310321, IC50: CysLT1 = 13 nM, CysLT2 = 25 nM) showed excellent pharmacokinetic profiles (%Frat = 100) compared with our previously reported compound 1 (%Frat = 1.5). In addition, we describe a new rule for dicarboxylic acid derivatives to show good oral bioavailability (%Frat ≥ 40) in rats (HBDs: ≤2, C log P: >6.5 and TPSA: <100). Especially, reduction of only one hydrogen-bond donor (HBDs) showed dramatically improved oral bioavailability. This small change of HBDs in dicarboxylic acid derivatives is generally a very effective modification. In the experiment, the researchers used many compounds, for example, 4-Bromoindole-3-acetic Acid (cas: 89245-41-0Recommanded Product: 89245-41-0).
4-Bromoindole-3-acetic Acid (cas: 89245-41-0) belongs to indole derivatives. Indole, first isolated in 1866, and it is commonly synthesized from phenylhydrazine and pyruvic acid, although several other procedures have been discovered. They are capable of binding to a variety of receptors with high affinity and thus have applications in a wide range of therapeutic areas.Recommanded Product: 89245-41-0
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