Recommanded Product: 1-(4-Nitrophenyl)ethanone. In 2019.0 LETT DRUG DES DISCOV published article about ALPHA/GAMMA DUAL AGONISTS; BETA-AMINO KETONE; AROMATIC-ALDEHYDES; MANNICH REACTION; DISCOVERY; DESIGN; SERIES; COMPLEX; MOIETY in [Liu, Jinyu; Zhou, Zuwen; Liu, Jian; Fan, Li; Liu, Jie; Chen, Feifei; Yang, Dacheng] Southwest Univ, Sch Chem & Chem Engn, Chongqing 400715, Peoples R China; [Yan, Jufang] Chengdu DiAo Pharmaceut Grp Co Ltd, Drug Screening Ctr, Chengdu 610041, Sichuan, Peoples R China; [Tang, Xuemei] Southwest Univ, Sch Life Sci, Chongqing 400715, Peoples R China in 2019.0, Cited 33.0. The Name is 1-(4-Nitrophenyl)ethanone. Through research, I have a further understanding and discovery of 100-19-6.
Background: Diabetes mellitus is the third-largest non-communicable chronic disease worldwide. There are many effective drugs, but the long-term use of these clinical drugs may cause various side effects. Therefore, it is urgent to develop new antidiabetic molecules with higher efficacy and lower toxicity. Methods: Fifteen new 3-aryl-1-(5-methylisoxazol-3-ylamino)-1-(4-nitrophenyl)propan-1-one were synthesized directly through the Mannich reaction of 4-nitroacetophenone, 3-amino-5-methylisoxazole and aromatic aldehydes catalyzed by concentrated hydrochloric acid. The molecular structures of the products were fully characterized by H-1 NMR, C-13 NMR, ESI MS and HRMS. The peroxisome proliferator-activated receptor (PPAR) response element and alpha-glucosidase inhibitory activity of these compounds were evaluated in vitro. Molecular docking, molecular physical parameters calculation, and molecular toxicity prediction were performed to analyze the structure-activity relationship and evaluate the druggability of these compounds theoretically. Results: All compounds exhibited weak antidiabetic activities, but compound 15 showed promising as a high performance, dual-target antidiabetic lead compound with peroxisome proliferator-activated receptor (PPAR) response element relative agonist activity of 99.55% at 27.2 nmol.ml(-1) and alpha-glucosidase inhibitory activity of 35.21% at 13.6 nmol.mL(-1). All compounds obtained may have no cardiotoxicity, no acute toxicity, no carcinogenic, and within safe range of mutagenic risk. Conclusion: This study identified a potential PPAR lead molecule and presented an unusual strategy for antidiabetic drug development.
Recommanded Product: 1-(4-Nitrophenyl)ethanone. About 1-(4-Nitrophenyl)ethanone, If you have any questions, you can contact Liu, JY; Zhou, ZW; Liu, J; Yan, JF; Fan, L; Tang, XM; Liu, J; Chen, FF; Yang, DC or concate me.
Reference:
Benzodioxan,
,1,4-Benzodioxane | C8H8O2 – PubChem