Safety of 3,4-Dimethoxybenzaldehyde. In 2021 EUR J MED CHEM published article about ALZHEIMERS-DISEASE; A-BETA; CHEMICAL-SYNTHESIS; DESIGN; ABAD/17-BETA-HSD10; IDENTIFICATION; OPTIMIZATION; DERIVATIVES; CHEMISTRY; PEPTIDE in [Boutin, Sophie; Maltais, Rene; Roy, Jenny; Poirier, Donald] CHU Quebec, Res Ctr, Lab Med Chem, Endocrinol & Nephrol Unit, Quebec City, PQ, Canada; [Boutin, Sophie; Poirier, Donald] Univ Laval, Fac Med, Dept Mol Med, Quebec City, PQ, Canada in 2021, Cited 47. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9.
17beta-Hydroxysteroid dehydrogenase type 10 (17 beta-HSD10) is the only mitochondrial member of 17 beta-HSD family. This enzyme can oxidize estradiol (E2) into estrone (E1), thus reducing concentration of this neuroprotective steroid. Since 17 beta-HSD10 possesses properties that suggest a possible role in Alzheimer’s disease, its inhibition appears to be a therapeutic strategy. After we identified the androsterone (ADT) derivative 1 as a first steroidal inhibitor of 17 beta-HSD10, new analogs were synthesized to increase the metabolic stability, to improve the selectivity of inhibition over 17 beta-HSD3 and to optimize the inhibitory potency. From six D-ring derivatives of 1 (17-C = O), two compounds (17 beta-H/17 alpha-OH and 17 beta-OH/17aC CH) were more metabolically stable and did not inhibit the 17 beta-HSD3. Moreover, solid phase synthesis was used to extend the molecular diversity on the 3b-piperazinylmethyl group of the steroid base core. Eight over 120 new derivatives were more potent inhibitors than 1 for the transformation of E2 to E1, with the 4-(4-trifluoromethyl-3-methoxybenzyl)piperazin-1-ylmethyl-ADT (D-3,7) being 16 times more potent (IC50 = 0.14 mM). Finally, D-ring modification of D-3,7 provided 17 beta-OH/17 alpha-C CH derivative 25 and 17 beta-H/17 alpha-OH derivative 26, which were more potent inhibitor than 1 (1.8 and 2.4 times, respectively). (C) 2020 Elsevier Masson SAS. All rights reserved.
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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles