Xue, Si-tu published the artcileSubstituted benzothiophene and benzofuran derivatives as a novel class of bone morphogenetic protein-2 upregulators: Synthesis, anti-osteoporosis efficacies in ovariectomized rats and a zebrafish model and ADME properties, Computed Properties of 622-40-2, the publication is European Journal of Medicinal Chemistry (2020), 112465, database is CAplus and MEDLINE.
This study optimized the structure of the anti-osteoporosis compound I [R1 = H; R2 = OMe; R5 = OEt; X = O] by balancing its lipophilicity and improving its stability. Substituted benzothiophenes/benzofurans derivatives I [R1 = H; R2 = OMe; R1R2 = OCH2O; R5 = Cl, OH, OEt; X = O, S] and II [R1 = H; R2 = OMe; R1R2 = OCH2O; R3 = n-Pr, P(O)(OH)2, CH2N(CH3)2, etc.; X = O, S; Y = O, NH, NMe] which were not reported in the literature were designed and synthesized. The ovariectomized rat model of osteoporosis was selected to evaluate the therapeutic effects, compound II [R1 = H; R2 = OMe; R3 = CH2N(CH3)2, etc.; X = O; Y = NH] showed better therapeutic efficacy than that of compound I [R1 = H; R2 = OMe; R5 = OEt; X = O]. The anti-osteoporosis activity and BMP-2 (bone morphogenetic protein-2) protein upregulation after treatment with compound II [R1 = H; R2 = OMe; R3 = CH2N(CH3)2, etc.; X = O; Y = NH] in a zebrafish osteoporosis model was verified. Compound II [R1 = H; R2 = OMe; R3 = CH2N(CH3)2, etc.; X = O; Y = NH] improved the ADME properties, therapeutic efficacy and pharmacokinetics of the drug than that of compound I [R1 = H; R2 = OMe; R5 = OEt; X = O]. Overall, the anti-osteoporosis effects of the compounds I and II of this type, preliminarily determined the target patient population, verified the mechanism of action, clarified the level of toxicity and provided preliminary ADME data was evaluated. These compounds I and II could both correct bone loss that was already occurring in patients and had broad clin. applicability.
European Journal of Medicinal Chemistry published new progress about 622-40-2. 622-40-2 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Alcohol, name is 2-Morpholinoethanol, and the molecular formula is C6H4ClNO2, Computed Properties of 622-40-2.
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https://en.wikipedia.org/wiki/Alcohol,
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