In 2013,Watanabe, Kazushi; Kakefuda, Akio; Yasuda, Minoru; Enjo, Kentaro; Kikuchi, Aya; Furutani, Takashi; Naritomi, Yoichi; Otsuka, Yukio; Okada, Minoru; Ohta, Mitsuaki published 《Discovery of 2-methyl-1-{1-[(5-methyl-1H-indol-2-yl)carbonyl]piperidin-4-yl}propan-2-ol: A novel, potent and selective type 5 17β-hydroxysteroid dehydrogenase inhibitor》.Bioorganic & Medicinal Chemistry published the findings.Computed Properties of C7H15NO The information in the text is summarized as follows:
Type 5 17β-hydroxysteroid dehydrogenase (17β-HSD5), also known as aldo-keto reductase 1C3 (AKR1C3), is a member of the aldo-keto reductase superfamily of enzymes and is expressed in the human prostate. One of the main functions of 17β-HSD5 is to catalyze the conversion of the weak androgen, androstenedione, to the potent androgen, testosterone. The concentration of intraprostatic 5α-dihydrotestosterone (DHT) in patients following chem. or surgical castration has been reported to remain as high as 39% of that of healthy men, with 17β-HSD5 shown to be involved in this androgen synthesis. Inhibition of 17β-HSD5 therefore represents a promising target for the treatment of castration-resistant prostate cancer (CRPC). To investigate this, we conducted high-throughput screening (HTS) and identified compound (I), which displayed a structure distinct from known 17β-HSD5 inhibitors. To optimize the inhibitory activity of compound (I), we first introduced a primary alc. group. We then converted the primary alc. group to a tertiary alc., which further enhanced the inhibitory activity, improved metabolic stability, and led to the identification of compound (II). Oral administration of compound II to castrated nude mice bearing the CWR22R xenograft resulted in the suppression of androstenedione (AD)-induced intratumoral testosterone production Compound II also demonstrated good isoform selectivity, minimal inhibitory activity against either CYP or hERG, and enhanced pharmacokinetic and physicochem. properties. After reading the article, we found that the author used 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Computed Properties of C7H15NO)
2-(Piperidin-4-yl)ethanol(cas: 622-26-4) can be used to synthese ursolic acid derivatives, spiroimidazolidinone NPC1L1 inhibitors, neurokinin-2 receptor antagonists, antagonists for inhibition of platelet aggregation.Computed Properties of C7H15NO
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem