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Development of Novel NK3 Receptor Antagonists With Reduced Environmental Impact

Development of Novel NK3 Receptor Antagonists With Reduced Environmental Impact

Koki Yamamoto, Shiho Okazaki, Hiroaki Ohno, Fuko Matsuda, Satoshi Ohkura, Kei-Ichiro Maeda, Nobutaka Fujii, Shinya Oishi

Bioorg Med Chem. 2016 Aug 15;24(16):3494-500.

PMID: 27298001

Abstract:

The neurokinin B (NKB)-neurokinin-3 receptor (NK3R) signaling positively regulates the release of gonadotropin-releasing hormone (GnRH) from the hypothalamus. The NK3R-selective antagonists may suppress the reproductive functions of mammals. For development of novel NK3R antagonists with reduced environmental toxicity, a structure-activity relationship study of an NK3R antagonist, talnetant, was carried out. Among several talnetant derivatives with labile functional groups in the natural environment, 3-mercaptoquinoline 2f exhibited a comparable biological activity to that of the parent talnetant. Additionally, compound 2f was converted into the disulfide 3f or isothiazolone 8 by air-oxidation, both of which showed no binding affinity to NK3R.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP174636329	Talnetant		174636-32-9	Price

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