Iwaki, Takehiko’s team published research in Bioorganic & Medicinal Chemistry in 2017 | CAS: 18621-18-6

Azetidin-3-ol hydrochloride(cas:18621-18-6) is one of azetidine.Azetidines (azacyclobutanes) constitute a well-known class of heterocyclic compounds. Azetidine scaffold has been discovered in several natural products.Computed Properties of C3H8ClNO Several pharmacologically important synthetic compounds also contain azetidine ring. Because of inherent ring strain, the synthesis of azetidines is a challenging endeavor.

Computed Properties of C3H8ClNOIn 2017 ,《Discovery and in vivo effects of novel human natriuretic peptide receptor A (NPR-A) agonists with improved activity for rat NPR-A》 appeared in Bioorganic & Medicinal Chemistry. The author of the article were Iwaki, Takehiko; Tanaka, Taisaku; Miyazaki, Kazuo; Suzuki, Yamato; Okamura, Yoshihiko; Yamaki, Akira; Iwanami, Makoto; Morozumi, Naomi; Furuya, Mayumi; Oyama, Yoshiaki. The article conveys some information:

Natriuretic peptide receptor A (NPR-A) agonists were evaluated in vivo by optimizing the structure of quinazoline derivatives to improve agonistic activity for rat NPR-A. A 1,4-Cis-aminocyclohexylurea moiety at 4-position and hydroxy group of D-alaninol at 2-position on the quinazoline ring were found to be important factors in improving rat NPR-A activity. The authors identified potent quinazoline and pyrido[2,3-d]pyrimidine derivatives against rat NPR-A, with double-digit nanomolar EC50 values. The in vivo results showed that compound 56b (1-((1S,4S)-4-((6-(3-fluorophenyl)-2-(((R)-1-hydroxypropan-2-yl)amino)pyrido[2,3-d]pyrimidin-4-yl)amino)cyclohexyl)-3-((R)-1-hydroxy-3-methylbutan-2-yl)urea) administered at 1.0 mg/kg/min significantly increased plasma cGMP concentration and urine volume in rats. The authors discovered novel potent NPR-A agonists that showed agonistic effects similar to those of atrial natriuretic peptide. After reading the article, we found that the author used Azetidin-3-ol hydrochloride(cas: 18621-18-6Computed Properties of C3H8ClNO)

Azetidin-3-ol hydrochloride(cas:18621-18-6) is one of azetidine.Azetidines (azacyclobutanes) constitute a well-known class of heterocyclic compounds. Azetidine scaffold has been discovered in several natural products.Computed Properties of C3H8ClNO Several pharmacologically important synthetic compounds also contain azetidine ring. Because of inherent ring strain, the synthesis of azetidines is a challenging endeavor.

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