Recommanded Product: 1129-28-8In 2022 ,《Design, synthesis and biological evaluation of novel 1H-pyrazole-4-carbonyl-4,5,6,7-tetrahydrobenzo[b]thiophene derivatives as gut-selective NaPi2b inhibitors》 appeared in Bioorganic & Medicinal Chemistry Letters. The author of the article were Ushiki, Yasunobu; Kawabe, Kenichi; Yamamoto-Okada, Kumiko; Uneuchi, Fumito; Asanuma, Yuta; Yamaguchi, Chitose; Ohta, Hiroshi; Shibata, Tsuyoshi; Abe, Tomohiro; Okumura-Kitajima, Lisa; Kosai, Yuki; Endo, Mayumi; Otake, Katsumasa; Munetomo, Eiji; Takahashi, Teisuke; Kakinuma, Hiroyuki. The article conveys some information:
Intestinal sodium-dependent phosphate transport protein 2b (SLC34A2, NaPi2b) inhibitors are expected to be potential new candidates for anti-hyperphosphatemia drugs. However, a risk of on-target side effects based on the inhibition of NaPi2b in the lung and testis has been reported. To identify gut-selective (minimally systemic) NaPi2b inhibitors, authors prepared and evaluated 1H-pyrazole-4-carbonyl-4,5,6,7-tetrahydrobenzo[b]thiophene derivatives with highly polar functional groups to reduce systemic exposure. As a result, compounds I (R = NH(CH)2O(CH2)2O(CH2)2O(CH2)2OH) and I (R = NHC(Me)2C(O)NH(CH2)2N(Me)2) showed a good activity in vitro and a low bioavailability in Sprague-Dawley (SD) rats. However, these compounds did not suppress phosphate absorption in SD rats. This lack of in vivo efficacy could be due to the high hydrophobicity of these compounds The results of further investigations of other classes of compounds with appropriate phys. properties will be reported in due course. In the experimental materials used by the author, we found Methyl 3-(bromomethyl)benzoate(cas: 1129-28-8Recommanded Product: 1129-28-8)
Methyl 3-(bromomethyl)benzoate(cas: 1129-28-8) belongs to organobromine compounds. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals. The most pervasive is the naturally produced bromomethane.Recommanded Product: 1129-28-8
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary