Day: October 13, 2022

Ye, Chanyuan; Xu, Rui; Cao, Zhongcheng; Song, Qing; Yu, Guangjun; Shi, Yichun; Liu, Zhuoling; Liu, Xiuxiu; Deng, Yong published the artcile< Design, synthesis, and in vitro evaluation of 4-aminoalkyl-1(2H)-phthalazinones as potential multifunctional anti-Alzheimer's disease agents>, Application of C10H10O4, the main research area is aminoalkylphthalazinone preparation cholinesterase inhibitor SAR antioxidant neuroprotective Alzheimer disease; 4-(aminoalkyl)-1(2H)-phthalazinone derivatives; Acetylcholinesterase inhibitors; Alzheimer’s disease; Anti-neuroinflammation; Aβ aggregation inhibitors; Monoamine oxidases inhibitors; Multifunctional agents.

A series of 4-aminoalkyl-1(2H)-phthalazinone derivatives I (R1 = benzyl, 2-methoxybenzyl, 2-dimethylaminobenzyl, 4-dimethylaminobenzyl, ethyl; R2 = Me, Et; R1R2 = -(CH2)5-, -(CH2)2O(CH2)2-, -(CH2)2N(CH3)(CH2)2-; n = 1, 3, 5) was designed and synthesized as potential multifunctional agents for Alzheimer’s disease (AD) treatment. In vitro biol. assay results demonstrated that most synthesized compounds I exhibited significant AChE inhibition, moderate to high monoamine oxidases (MAO) inhibitory potencies and good anti-platelet aggregation abilities. Among them, compound I (R1 = Bn; R2 = Et; n = 3) (II) exhibited the highest inhibitory potencies towards MAO-B and MAO-A (IC50 = 0.7μM and 6.4μM resp.), moderate inhibition towards AChE (IC50 = 8.2μM), and good activities against self- and Cu2+-induced Aβ1-42 aggregation and platelet aggregation. Moreover, II also displayed antioxidant capacity, neuroprotective potency, anti-neuroinfammation and BBB permeability. These excellent results indicated that compound II could be worthy of further studies to be considered as a promising multifunctional candidate for the treatment of AD.

Bioorganic Chemistry published new progress about Alzheimer disease. 531-88-4 belongs to class benzofurans, and the molecular formula is C10H10O4, Application of C10H10O4.

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Cai, Lingchao; Zhang, Kui; Chen, Shuming; Lepage, Romain J.; Houk, K. N.; Krenske, Elizabeth H.; Kwon, Ohyun published the artcile< Catalytic Asymmetric Staudinger-aza-Wittig Reaction for the Synthesis of Heterocyclic Amines>, Category: benzofurans, the main research area is amine heterocycle preparation catalyst asym Staudinger aza Wittig.

Many natural products and medicinal drugs are heterocyclic amines possessing a chiral quaternary carbon atom in their heterocyclic ring. Herein, the authors report the first catalytic and asym. Staudinger-aza-Wittig reaction for the desymmetrization of ketones. This highly enantioselective transformation proceeds at room temperature to provide high yields-even on multigram scales-of nitrogen heterocycles featuring a chiral quaternary center. The products of this reaction are potential precursors for the synthesis of pharmaceuticals. A com. available small P-chiral phosphine catalyst, HypPhos, induces the asymmetry and is recycled through in situ reduction of its oxide, mediated by phenylsilane in the presence of a carboxylic acid. The efficiency, selectivity, scalability, mild reaction conditions, and broad substrate scope portend that this process will expedite the syntheses of chiral heterocyclic amines of significance to chem., biol., and medicine.

Journal of the American Chemical Society published new progress about Aromatic heterocyclic amines Role: SPN (Synthetic Preparation), PREP (Preparation). 531-88-4 belongs to class benzofurans, and the molecular formula is C10H10O4, Category: benzofurans.

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Ibrahimi, Maroua; Khoumeri, Omar; Abderrahim, Raoudha; Terme, Thierry; Vanelle, Patrice published the artcile< Synthesis of 3-Benzylphthalide Derivatives by Using a TDAE Strategy>, HPLC of Formula: 531-88-4, the main research area is benzylphthalide preparation; nitrobenzyl chloride tetrakisdimethylaminoethylene formylbenzoate nucleophilic addition.

A one-pot synthesis of new 3-benzylphthalide derivatives I (X = CH, N; R1 = 4-NO2, 3-OMe-4-NO2, 2-NO2-4-C6H4, etc.; R2 = 4-CN, 5-Cl, 4-COOMe, etc.) was developed by using a strategy based on tetrakis(dimethylamino)ethylene (TDAE). The reactions in the presence of TDAE of substituted benzyl chlorides with Me 2-formylbenzoate or of substituted methyl-2-formylbenzoates with 4-nitrobenzyl chloride furnished the corresponding isobenzofuran-1(3H)-one products in moderate to good yields.

Synlett published new progress about Benzaldehydes Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 531-88-4 belongs to class benzofurans, and the molecular formula is C10H10O4, HPLC of Formula: 531-88-4.

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Luo, Li; Song, Qing; Li, Yan; Cao, Zhongcheng; Qiang, Xiaoming; Tan, Zhenghuai; Deng, Yong published the artcile< Design, synthesis and evaluation of phthalide alkyl tertiary amine derivatives as promising acetylcholinesterase inhibitors with high potency and selectivity against Alzheimer's disease>, Computed Properties of 531-88-4, the main research area is aminoalkyl dihydrobenzofuranone preparation cholinesterase SAR mol docking; Acetylcholinesterase inhibitors; Alzheimer’s disease; Anti-Aβ aggregation; Antioxidant; DL-3-n-butylphthalide derivatives; Multi-target agents.

A series of phthalide alkyl tertiary amine derivatives I, II and III [R1 = Me, Et; R = Et, MeO, Bn, 2-MeOBn, 2-Me2NBn] were designed, synthesized and evaluated as potential multi-target agents against Alzheimer’s disease (AD). The results indicated that almost all the compounds I, II and III displayed significant AChE inhibitory and selective activities. Besides, most of the derivatives I, II and III exhibited increased self-induced Aβ1-42 aggregation inhibitory activity compared to the lead compound DL-NBP, and some compounds also exerted good antioxidant activity. Specifically, compound I [R1 = R2 = Et] showed the highest inhibitory potency toward AChE (IC50 = 2.66 nM), which was significantly better than Donepezil (IC50 = 26.4 nM). Moreover, mol. docking studies revealed that compound I [R1 = R2 = Et] was bind to both the catalytic active site and peripheral anionic site of AChE. Furthermore, compound I [R1 = R2 = Et] displayed excellent BBB permeability in-vitro. Importantly, the step-down passive avoidance test indicated that I [R1 = R2 = Et] significantly reversed scopolamine-induced memory deficit in mice. Collectively, these results suggested that I [R1 = R2 = Et] was a potent and selective AChE inhibitor for further anti-AD drug development.

Bioorganic & Medicinal Chemistry published new progress about Cholinesterase inhibitors. 531-88-4 belongs to class benzofurans, and the molecular formula is C10H10O4, Computed Properties of 531-88-4.

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem