18451-44-0Relevant articles and documents
Synthesis, growth, and characterization of 3-(4-Methoxyphenyl)-1-(pyridin- 2-yl) prop-2-en-1-one single crystal: A potential NLO material
Jayarama,Ravindra,Menezes, Anthoni Praveen,Dharmaprakash,Ng, Seik Weng
, p. 285 - 291 (2013)
New nonlinear optical chalcone material, 3-(4-Methoxyphenyl)-1-(pyridin-2- yl) prop-2-en-1-one (MPP) has been synthesized and grown as a high quality single crystal by the slow evaporation solution growth technique using acetone as solvent. The grown crys
From Celecoxib to a Novel Class of Phosphodiesterase 5 Inhibitors: Trisubstituted Pyrazolines as Novel Phosphodiesterase 5 Inhibitors with Extremely High Potency and Phosphodiesterase Isozyme Selectivity
Abdel-Halim, Mohammad,Sigler, Sara,Racheed, Nora A. S.,Hefnawy, Amr,Fathalla, Reem K.,Hammam, Mennatallah A.,Maher, Ahmed,Maxuitenko, Yulia,Keeton, Adam B.,Hartmann, Rolf W.,Engel, Matthias,Piazza, Gary A.,Abadi, Ashraf H.
supporting information, p. 4462 - 4477 (2021/05/04)
A ligand-based approach involving systematic modifications of a trisubstituted pyrazoline scaffold derived from the COX2 inhibitor, celecoxib, was used to develop novel PDE5 inhibitors. Novel pyrazolines were identified with potent PDE5 inhibitory activit
Coordination-driven self-assembly of anthraquinone-based metal-organic cages for photocatalytic selective [2 + 2] cycloaddition
Cui, Yong,Jiang, Hong,Jin, Yao,Liu, Yan,Tang, Xianhui,Zhang, Wenqiang
supporting information, p. 8533 - 8539 (2021/06/28)
Visible-light-promoted [2 + 2] cycloaddition provides a straightforward and efficient way to produce cyclobutanes, which are the core skeleton in commercial pharmaceuticals and fine chemicals. However, the control of the conformation to producesyn-head-to
Design, Synthesis, and Evaluation of Chalcone Derivatives as Multifunctional Agents against Alzheimer's Disease
Wang, Xiao-Qin,Zhou, Lu-Yi,Tan, Ren-Xian,Liang, Guo-Peng,Fang, Si-Xian,Li, Wei,Xie, Mei,Wen, Yu-Hao,Wu, Jia-Qiang,Chen, Yi-Ping
, (2021/10/19)
Fifteen chalcone derivatives 3a–3o were synthesized, and evaluated as multifunctional agents against Alzheimer's disease. In vitro studies revealed that these compounds inhibited self-induced Aβ1-42 aggregation effectively ranged from 45.9–94.5
Chiral bipyridine-annulated bicyclo[3.3.1]nonane N-oxide organocatalysts for stereoselective allylation and hydrosilylation reactions
?eimyt?, Simona,Ston?ius, Sigitas
, (2020/12/21)
The synthesis of chiral C2-symmetric bis(bipyridine N,N′-dioxide) and bis(bipyridine N-monooxide) derivatives featuring bipyridine-annulated bicyclo[3.3.1]nonane framework is reported. The new Lewis basic bipyridine N,N′-dioxides exhibited good
Light-Driven Enantioselective Synthesis of Pyrroline Derivatives by a Radical/Polar Cascade Reaction
Rodríguez, Ricardo I.,Mollari, Leonardo,Alemán, José
supporting information, p. 4555 - 4560 (2021/01/18)
Herein, a light-driven, atom-economical process that provides access to enantiomerically enriched substituted chiral 1-pyrroline derivatives is introduced. The strategy involves the distal functionalization of acyl heterocycles through a hydrogen-atom transfer (HAT) process and the use of tailor-made ketimines as reliable electrophilic partners. This transformation is translated into an enantiomerically controlled radical/polar cascade reaction in which water is produced as the sole by-product and stereoselectivity is dictated by coordination to a chiral-at-rhodium catalyst.
Synthesis and Luminescence Spectral Properties of New Cyano-Substituted 2,2′-Bipyridine Derivatives
Bardasov, I. N.,Belikov, M. Yu.,Ershov, O. V.,Ievlev, M. Yu.,Mayorov, N. S.,Shishlikova, M. A.
, p. 1961 - 1967 (2022/01/24)
Abstract: Previously unknown 2-{4-aryl-5-cyano-[2,2′-bipyridin]-6(1H)-ylidene}malononitriles were synthe-sized by reaction of 3-aryl-1-(pyridin-2-yl)prop-2-en-1-ones (azachalcones) with malononitrile dimer. Their colored solutions showed fluorescence in t
An Efficient Cyclic Di-AMP Based Artificial Metalloribozyme for Enantioselective Diels–Alder Reactions
Qi, Qianqian,Lv, Shuting,Hao, Min,Dong, Xingchen,Gu, Youkun,Wu, Peizhe,Zhang, Wenyue,Chen, Yashao,Wang, Changhao
, p. 4417 - 4424 (2020/06/17)
The diverse structures of nucleic acids as scaffolds have brought the significant advancement for DNA-based enantioselective catalysis, yet RNA-based enantioselective catalysis is lacking investigation. Herein, we report a small, natural RNA of cyclic di-AMP (c-di-AMP) and Cu2+ ions assemble into an artificial metalloribozyme (c-di-AMP·Cu2+), that could effectively catalyze the enantioselective Diels–Alder reactions with up to 80 percent ee. The enantioselective catalytic performance of c-di-AMP·Cu2+ has been studied by thorough investigations of different metal cofactors, c-di-AMP/Cu2+ molar ratios, additives, buffers and c-di-AMP analogues. In addition, the assembly of c-di-AMP·Cu2+ gives rise to 300-fold and 5-fold rate acceleration compared to the uncatalyzed reaction and Cu2+ ions, respectively. This work provides a simple and efficient strategy to construct the RNA-based catalysts that would expand the current nucleic acids-based catalysis and might hint the possible catalytic RNA in primordial chemistry.
Design, synthesis and neuropharmacological evaluation of new 2,4-disubstituted-1,5-benzodiazepines as CNS active agents
Bhatia, Rohit,Kumar, Bhupinder,Mehan, Sidharth,Monga, Vikramdeep,Singh, Gurpreet,Verma, Ramesh
, (2020/07/03)
Benzodiazepines (BZDs) represent a class of privilege scaffold in the modern era of medicinal chemistry as CNS active agents and BZD based drugs are used to treat different psychotic disorders. Inspired from the therapeutic potential of BZDs as promising CNS active agents, in the present work three different series of 1,5-benzodiazepines bearing various substitutions at position 2 and 4 of the benzodiazepine core were synthesized by condensing different substituted chalcones with o-phenylenediamine in the presence of piperidine as a base catalyst. Structural characterization of title compounds was done by using various analytical techniques such as IR, NMR, elemental analysis and mass spectral data. All the synthesized compounds (9a-d, 10a-e and 11a-c) were subjected to in vivo neuropharmacological studies to evaluate their CNS depressant and antiepileptic activity. Results of in vivo evaluation data showed that analogue 11b exhibited potent CNS depressant activity which was comparable to the standard drug diazepam. Compounds 10b and 10c displayed significant antiepileptic activity however they were less potent than the standard drug phenobarbitone. Molecular docking studies were performed using MOE software to find the interaction pattern and binding mode at the GABAA receptor (PDB Id: 6HUP). The results of the docking studies were in good agreement with the observed in vivo activity and revealed the satisfactory binding mode of the compounds within the binding site of the protein. The docking scores for the most promising candidates 10c, 11b and Diazepam were found to be ?9.18, ?9.46 and ?9.88, respectively. Further, the compounds showed compliance with the Lipinski's ‘rule of five’ and exhibited favourable drug-likeness scores. The identified leads can be explored further for the design and development of new BZD based psychotropic agents.
Synthesis, characterization and biological application of pyrazolo[1,5-a]pyrimidine based organometallic Re(I) complexes
Bhatt, Bhupesh S.,Pandya, Juhee G.,Patel, Mohan N.,Pathak, Chandramani,Vaidya, Foram U.,Varma, Reena R.
, p. 957 - 969 (2020/10/02)
The neutral rhenium(I) complexes (I-VI) of type [ReCl(CO)3Ln] {where L1 = 7-phenyl-5-(pyridin-2-yl)pyrazolo[1,5-a] pyrimidine, L2 = 7-(4-bromophenyl)-5-(pyridin-2-yl)pyrazolo[1,5-a]pyrimi- dine, L3 =
