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https://www.readbyqxmd.com/read/28863358/from-dual-binding-site-acetylcholinesterase-inhibitors-to-allosteric-modulators-a-new-avenue-for-disease-modifying-drugs-in-alzheimer-s-disease
#1
Talita P C Chierrito, Susimaire Pedersoli-Mantoani, Carlos Roca, Carlos Requena, Victor Sebastian-Perez, Willian O Castillo, Natalia C S Moreira, Concepción Pérez, Elza T Sakamoto-Hojo, Catarina S Takahashi, Jesús Jiménez-Barbero, F Javier Cañada, Nuria E Campillo, Ana Martinez, Ivone Carvalho
The lack of an effective treatment for Alzheimer' disease (AD), an increasing prevalence and severe neurodegenerative pathology boost medicinal chemists to look for new drugs. Currently, only acethylcholinesterase (AChE) inhibitors and glutamate antagonist have been approved to the palliative treatment of AD. Although they have a short-term symptomatic benefits, their clinical use have revealed important non-cholinergic functions for AChE such its chaperone role in beta-amyloid toxicity. We propose here the design, synthesis and evaluation of non-toxic dual binding site AChEIs by hybridization of indanone and quinoline heterocyclic scaffolds...
August 26, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28859234/side-chain-engineering-on-medium-bandgap-copolymers-to-suppress-triplet-formation-for-high-efficiency-polymer-solar-cells
#2
Lingwei Xue, Yankang Yang, Jianqiu Xu, Chunfeng Zhang, Haijun Bin, Zhi-Guo Zhang, Beibei Qiu, Xiaojun Li, Chenkai Sun, Liang Gao, Jia Yao, Xiaofeng Chen, Yunxu Yang, Min Xiao, Yongfang Li
Suppression of carrier recombination is critically important in realizing high-efficiency polymer solar cells. Herein, it is demonstrated difluoro-substitution of thiophene conjugated side chain on donor polymer can suppress triplet formation for reducing carrier recombination. A new medium bandgap 2D-conjugated D-A copolymer J91 is designed and synthesized with bi(alkyl-difluorothienyl)-benzodithiophene as donor unit and fluorobenzotriazole as acceptor unit, for taking the advantages of the synergistic fluorination on the backbone and thiophene side chain...
August 31, 2017: Advanced Materials
https://www.readbyqxmd.com/read/28837314/thieno-3-2-b-pyrrolo-fused-pentacyclic-benzotriazole-based-acceptor-for-efficient-organic-photovoltaics
#3
Liuliu Feng, Jun Yuan, Zhenzhen Zhang, Hongjian Peng, Zhi-Guo Zhang, Shutao Xu, Ye Liu, Yongfang Li, Yingping Zou
A novel nonfullerene small molecular acceptor (BZIC) based on a ladder-type thieno[3,2-b]pyrrolo-fused pentacyclic benzotriazole core (dithieno[3,2-b]pyrrolobenzotriazole, BZTP) and end-capped with 1,1-dicyanomethylene-3-indanone (INCN) has been first reported in this work. Through introducing multifused benzotriazole and INCN, BZIC could maintain a high-lying lowest unoccupied molecular orbital (LUMO) energy level of -3.88 eV. Moreover, BZIC shows a low optical bandgap of 1.45 eV with broad and efficient absorption band from 600 to 850 nm due to increased π-π interactions by the covalently locking thiophene and benzotriazole units...
September 20, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28836441/synthesis-of-%C3%AE-%C3%AE-disubstituted-indanones-via-the-pd-catalyzed-tandem-conjugate-addition-cyclization-reaction-of-arylboronic-acids-with-%C3%AE-%C3%AE-unsaturated-esters
#4
Ang Gao, Xiu-Yan Liu, Hao Li, Chang-Hua Ding, Xue-Long Hou
Under Pd catalysis with a newly synthesized electron-deficient heterocycle, 2-(4,5-dihydroimidazol-2-yl)pyrimidine (as the ligand), the reaction of α,β-unsaturated esters with arylboronic acids afforded a wide range of 3,3-disubstituted indan-1-ones bearing a quaternary carbon in high yields. Mechanistic studies revealed that the reaction involves a tandem conjugate addition/1,4-Pd shift followed by a cyclization.
August 24, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28803994/lepistatins-a-c-chlorinated-sesquiterpenes-from-the-cultured-basidiomycete-lepista-sordida
#5
Hahk-Soo Kang, So-Ae Ji, So-Hyun Park, Jong-Pyung Kim
Three new chlorinated sesquiterpenes, named lepistatins A-C, were isolated from the culture broth of Basidiomycete Lepista sordida. The structures were determined by the analysis of spectroscopic data including HREIMS and 1D and 2D NMR. The absolute configuration of lepistatin B was determined by comparing the specific rotation and circular dichroism spectrum with those of known structurally related compounds bearing the same chiral carbon. The structures of lepistatins A-C feature the indanone core structure, but differ from other indanone-containing sesquiterpenes of fungal origin by the alkyl substitution pattern...
August 9, 2017: Phytochemistry
https://www.readbyqxmd.com/read/28758653/a-rhodium-catalyzed-tandem-reaction-of-n-sulfonyl-triazoles-with-indoles-access-to-indole-substituted-indanones
#6
Hao Yuan, Jianxian Gong, Zhen Yang
An efficient strategy for the synthesis of structurally diverse indole-substituted indanones via a rhodium(ii)-catalyzed tandem reaction of N-sulfonyltriazoles with indoles was developed. The reaction involves rhodium(ii)-catalyzed denitrogenation of the N-sulfonyltriazoles to form an oxonium ylide, followed by nucleophilic addition of the indoles and subsequent skeletal rearrangement. This strategy provides straightforward access to indanone frameworks bearing quaternary carbon centers.
July 31, 2017: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/28714198/enhancing-performance-of-nonfullerene-acceptors-via-side-chain-conjugation-strategy
#7
Jiayu Wang, Wei Wang, Xiaohui Wang, Yang Wu, Qianqian Zhang, Cenqi Yan, Wei Ma, Wei You, Xiaowei Zhan
A side-chain conjugation strategy in the design of nonfullerene electron acceptors is proposed, with the design and synthesis of a side-chain-conjugated acceptor (ITIC2) based on a 4,8-bis(5-(2-ethylhexyl)thiophen-2-yl)benzo[1,2-b:4,5-b']di(cyclopenta-dithiophene) electron-donating core and 1,1-dicyanomethylene-3-indanone electron-withdrawing end groups. ITIC2 with the conjugated side chains exhibits an absorption peak at 714 nm, which redshifts 12 nm relative to ITIC1. The absorption extinction coefficient of ITIC2 is 2...
July 17, 2017: Advanced Materials
https://www.readbyqxmd.com/read/28696657/3d-structural-model-of-high-performance-non-fullerene-polymer-solar-cells-as-revealed-by-high-resolution-afm
#8
Shaowei Shi, Xiaofeng Chen, Xubo Liu, Xuefei Wu, Feng Liu, Zhi-Guo Zhang, Yongfang Li, Thomas P Russell, Dong Wang
Rapid improvements in nonfullerene polymer solar cells (PSCs) have brought power conversion efficiencies to greater than 12%. To further improve device performance, a fundamental understanding of the correlations between structure and performance is essential. In this paper, based on a typical high-performance system consisting of J61(one donor-acceptor (D-A) copolymer of benzodithiophene and fluorine substituted benzotriazole) and ITIC (3,9-bis(2-methylene-(3-(1,1-dicyanomethylene)-indanone)-5,5,11,11-tetrakis(4-hexylphenyl)-dithieno[2,3-d:2',3'-d']-s-indaceno[1,2-b:5,6-b']-dithiophene), a 3D structural model is directly imaged by employing high-resolution atomic force microscopy (AFM)...
July 17, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28667874/recent-developments-in-biological-activities-of-indanones
#9
REVIEW
Siddappa A Patil, Renukadevi Patil, Shivaputra A Patil
Indanone is one of the privileged structures in medicinal chemistry and it's commonly associated with various pharmacologically active compounds. The indanone moiety is found in several natural compounds and also, it can be used as intermediate in the synthesis of many different types of medicinally important molecules. Among the medicinally important indanones, the most significant drug probably is donepezil (IV), an acetylcholinesterase (AChE) inhibitor, which has been approved by the US Food and Drug Administration for the treatment of Alzheimer's disease (AD)...
September 29, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28660755/highly-efficient-inverted-d-a1-a2-ternary-blend-organic-photovoltaics-combining-a-ladder-type-non-fullerene-acceptor-and-a-fullerene-acceptor
#10
Shao-Ling Chang, Fong-Yi Cao, Wen-Chia Huang, Po-Kai Huang, Chain-Shu Hsu, Yen-Ju Cheng
A formylated benzodi(cyclopentadithiophene) (BDCPDT) ladder-type structure with forced coplanarity is coupled with two 1,1-dicyanomethylene-3-indanone (IC) moieties via olefination to form a non-fullerene acceptor, BDCPDT-IC. The BDCPDT-IC, as an acceptor (A1) with broad light-absorbing ability and excellent solution processability, is combined with a second PC71BM acceptor (A2) and a medium band gap polymer, PBDB-T, as the donor (D) to form a ternary blend with gradient HOMO/LUMO energy alignments and panchromatic absorption...
July 13, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28613859/donepezil-based-central-acetylcholinesterase-inhibitors-by-means-of-a-bio-oxidizable-prodrug-strategy-design-synthesis-and-in-vitro-biological-evaluation
#11
Ludovic Peauger, Rabah Azzouz, Vincent Gembus, Mihaela-Liliana Ţînţaş, Jana Sopková-de Oliveira Santos, Pierre Bohn, Cyril Papamicaël, Vincent Levacher
With the aim of reducing side effects of acetylcholinesterase inhibitors (AChEIs) during symptomatic treatment of Alzheimer's disease, we report herein a new class of donepezil-based "bio-oxidizable" prodrugs 1 designed to be converted into dual binding site AChEIs 2. While most of indanone-derived N-benzylpyridinium salts 2 revealed to be highly potent dual binding site hAChEIs (IC50 up to 3 nM), outperforming the standard drug donepezil (IC50 = 11 nM), most of the corresponding 1,4-dihydropyridines 1 were found to be inactive...
July 13, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28608531/fused-hexacyclic-nonfullerene-acceptor-with-strong-near-infrared-absorption-for-semitransparent-organic-solar-cells-with-9-77-efficiency
#12
Wei Wang, Cenqi Yan, Tsz-Ki Lau, Jiayu Wang, Kuan Liu, Yan Fan, Xinhui Lu, Xiaowei Zhan
A fused hexacyclic electron acceptor, IHIC, based on strong electron-donating group dithienocyclopentathieno[3,2-b]thiophene flanked by strong electron-withdrawing group 1,1-dicyanomethylene-3-indanone, is designed, synthesized, and applied in semitransparent organic solar cells (ST-OSCs). IHIC exhibits strong near-infrared absorption with extinction coefficients of up to 1.6 × 10(5) m(-1) cm(-1) , a narrow optical bandgap of 1.38 eV, and a high electron mobility of 2.4 × 10(-3) cm(2) V(-1) s(-1) . The ST-OSCs based on blends of a narrow-bandgap polymer donor PTB7-Th and narrow-bandgap IHIC acceptor exhibit a champion power conversion efficiency of 9...
June 13, 2017: Advanced Materials
https://www.readbyqxmd.com/read/28600079/synthesis-antiviral-evaluation-and-molecular-docking-studies-of-n-4-aryl-substituted-unsubstituted-thiosemicarbazones-derived-from-1-indanones-as-potent-anti-bovine-viral-diarrhea-virus-agents
#13
María C Soraires Santacruz, Matías Fabiani, Eliana F Castro, Lucía V Cavallaro, Liliana M Finkielsztein
A series of N(4)-arylsubstituted thiosemicarbazones derived from 1-indanones and a set of compounds lacking such substitution in the N(4) position of the thiosemicarbazone moiety were synthesized and evaluated for their anti-bovine viral diarrhea virus (BVDV) activity. Among these, derivatives 2 and 15 displayed high activity (EC50=2.7±0.4 and 0.7±0.1µM, respectively) as inhibitors of BVDV replication. Novel key structural features related to the anti-BVDV activity were identified by structure-activity relationship (SAR) analysis...
May 27, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28585823/copper-catalyzed-radical-cascade-difluoromethylation-cyclization-of-2-3-arylpropioloyl-benzaldehydes-a-route-to-difluoromethylated-naphthoquinones
#14
Yan Zhang, Shangyi Ye, Mingming Ji, Lisha Li, Dongmei Guo, Gangguo Zhu
A novel copper-catalyzed cascade difluoromethylation/cyclization of 2-(3-arylpropioloyl)benzaldehydes has been developed. This method affords an efficient and straightforward access to structurally diverse difluoromethylated naphthoquinones in one pot, starting from readily available starting materials. The reaction represents the first trans-acyldifluoromethylation of internal alkynes, which features aldehydes as acceptors for the addition of alkenyl radicals. Furthermore, this protocol can also access to monofluoromethylated naphthoquinone and difluoromethylated indanones in the same reaction condition...
June 12, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28570073/efficient-and-stable-ternary-organic-solar-cells-based-on-two-planar-nonfullerene-acceptors-with-tunable-crystallinity-and-phase-miscibility
#15
Jialin Wang, Jiajun Peng, Xiaoyu Liu, Ziqi Liang
Planar perylene diimides (PDIs), when used as nonfullerene acceptors for organic photovoltaics, are constrained by their large π-aggregation in solid state. To tackle this issue, another planar nonfullerene acceptor 3,9-bis(2-methylene-(3-(1,1-dicyanomethylene)-indanone)-5,5,11,11-tetrakis(4-hexylphenyl)-dithieno[2,3-d:2',3'-d']-s-indaceno[1,2-b:5,6-b']dithiophene (ITIC) with weak crystallinity and near-infrared light absorption is introduced into the PTB7-Th:PDI binary blend to fabricate efficient and stable ternary solar cells...
June 21, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28560364/copper-catalyzed-acyltrifluoromethylation-of-alkenes-rapid-access-to-trifluoroethyl-indanones-and-related-compounds
#16
Zhicheng Liu, Yihui Bai, Jian Zhang, Yongqi Yu, Ze Tan, Gangguo Zhu
Copper-catalyzed acyltrifluoromethylation of alkenes has been developed for the first time, affording trifluoroethyl indanones and related cyclic ketones in promising yields with excellent diastereoselectivity. The fast incorporation of CF3 and indanone into a single molecule renders it an efficient and valuable tool for the synthesis of biologically active compounds.
May 31, 2017: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/28557142/reaction-acceleration-in-thin-films-with-continuous-product-deposition-for-organic-synthesis
#17
Zhenwei Wei, Michael Wleklinski, Christina Ferreira, R Graham Cooks
Thin film formats are used to study the Claisen-Schmidt base-catalyzed condensation of 6-hydroxy-1-indanone with substituted benzaldehydes and to compare the reaction acceleration relative to the bulk. Relative acceleration factors initially exceeded 10(3) and were on the order of 10(2) at steady state, although the confined volume reaction was not electrostatically driven. Substituent effects were muted compared to those in the corresponding bulk and microdroplet reactions and it is concluded that the rate-limiting step at steady state is reagent transport to the interface...
August 1, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28526475/identification-and-preliminary-structure-activity-relationships-of-1-indanone-derivatives-as-novel-indoleamine-2-3-dioxygenase-1-ido1-inhibitors
#18
Dingding Gao, Yingxia Li
Indoleamine 2,3-dioxygenase 1 (IDO1) plays a vital role in the catabolism of tryptophan along with the kynurenine pathway which is involved in many human diseases including cancer, Alzheimer's disease, etc. In this study, compound 1 bearing a 1-Indanone scaffold was identified as a novel IDO1 inhibitor by structure-based virtual screening, with moderate to good enzymatic and cellular inhibitory activities. Also, surface plasmon resonance analysis validated the direct interaction between compound 1 and IDO1 protein...
May 10, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28504882/visible-light-induced-tandem-radical-addition-cyclization-of-alkenyl-aldehydes-leading-to-indanones-and-related-compounds
#19
Danyang Lu, Yimei Wan, Lichun Kong, Gangguo Zhu
Herein we describe a novel, visible light-induced tandem radical addition-cyclization of alkenyl aldehydes with α-bromocarbonyl compounds. A set of cyclic ketones, including indanones, cyclopentenones, 3,4-dihydronaphthalen-1(2H)-ones, and chroman-4-ones, are synthesized at room temperature with high efficiency and good functional group compatibility. It represents the first report on the catalytic 1,2-acylalkylation of unactivated alkenes.
May 15, 2017: Organic Letters
https://www.readbyqxmd.com/read/28481313/two-new-metabolites-from-the-endophytic-fungus-alternaria-sp-a744-derived-from-morinda-officinalis
#20
Ying Wang, Hong-Xin Liu, Yu-Chan Chen, Zhang-Hua Sun, Hao-Hua Li, Sai-Ni Li, Ming-Li Yan, Wei-Min Zhang
Two new compounds isobenzofuranone A (1) and indandione B (2), together with eleven known compounds (3-13) were isolated from liquid cultures of an endophytic fungus Alternaria sp., which was obtained from the medicinal plant Morinda officinalis. Among them, the indandione (2) showed a rarely occurring indanone skeleton in natural products. Their structures were elucidated mainly on the basis of extensive spectroscopic data analysis. All of the compounds were evaluated with cytotoxic and α-glucosidase inhibitory activity assays...
May 8, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
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