18451-69-9Relevant academic research and scientific papers
Synthesis of azachalcones, their α-amylase, α-glucosidase inhibitory activities, kinetics, and molecular docking studies
Saleem, Faiza,Kanwal,Khan, Khalid Mohammed,Chigurupati, Sridevi,Solangi, Mehwish,Nemala, Appala Raju,Mushtaq, Maria,Ul-Haq, Zaheer,Taha, Muhammad,Perveen, Shahnaz
, (2020/12/09)
Diabetes being a chronic metabolic disorder have attracted the attention of medicinal chemists and biologists. The introduction of new and potential drug candidates for the cure and treatment of diabetes has become a major concern due to its increased pre
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
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
Aggregation induced emission (AIE) active 4-amino-1,8-naphthalimide-Tr?ger's base for the selective sensing of chemical explosives in competitive aqueous media
Delente, Jason M.,Gunnlaugsson, Thorfinnur,Kotova, Oxana,Shanmugaraju, Sankarasekaran,Umadevi, Deivasigamani,Watson, Graeme W.
supporting information, p. 2562 - 2565 (2020/03/10)
The 4-amino-1,8-naphthalimide-Tr?ger's base fluorophore, TBNap-TPy, adorned with phenyl-terpyridine moiety was synthesised and assessed for its aggregation-induced emission (AIE) behaviour. TBNap-TPy was further employed as a fluorescent sensor for the di
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.
A novel bis(terpyridine) with π?conjugated phenyl viologen and its metallo- supramolecular polymers: Synthesis and electrochromism
Qian, Yuchen,Wang, Yuechuan,Yang, Han
, (2020/02/11)
A novel phenylene viologen functionalized bis(terpyridine) is synthesized and characterized with 1HNMR and Maldi-tof-MS. This rod-like and π-conjugated molecule, 1,1'-[4'-(4-phenyl)-2,2:6′,2″- terpyridine-4,4′-bipyridine-1,1′-diium dichloride (
Design and development of a heterogeneous catalyst for the michael addition of malononitrile to 2-enoylpyridines: Influence of the primary amide decorated framework on catalytic activity and selectivity
Markad, Datta,Khullar, Sadhika,Mandal, Sanjay K.
supporting information, p. 12547 - 12554 (2019/10/11)
For the Michael addition of malononitrile to 2-enoylpyridines, we report the first heterogeneous catalyst, {[Zn2(2-bpbg)(fum)2]·4H2O·EtOH}n (1) (where 2-bpbg = N,N′-bis(2-pyridylmethyl)-1,4-diaminobutane-N,N′-di
Design, synthesis, pharmacological evaluation and DNA interaction studies of binuclear Pt(II) complexes with pyrazolo[1,5-a]pyrimidine scaffold
Lunagariya, Miral V.,Thakor, Khyati P.,Waghela, Bhargav N.,Pathak, Chadramani,Patel, Mohan N.
, (2018/01/22)
Substituted pyrazolo[1,5-a]pyrimidine ligands were synthesized by cyclization, using 3-(thiophen-2-yl)-1H-pyrazol-5-amine with substituted enones (3-phenyl-1-(pyridin-2-yl)prop-2-en-1-one) in presence of KOH and DMF as solvent to form cyclic aromatic compounds. The substituted pyrazolo[1,5-a] pyrimidine based binuclear PtII complexes containing neutral tetradentated ligands have general formula [Pt2(5a–5f)Cl4], (where, (5a -5f) = pyrazolo[1,5-a] pyrimidine ligand). This compounds were characterized by physicochemical and spectroscopic method like elemental analyses, UV-Visible, FT-IR, EDX, TGA, molar conductivity, magnetic susceptibility measurements, mass spectroscopy, 1H and 13C NMR method. The square planar geometry was predicted by electronic spectral study. All PtII compounds were evaluated by antimicrobial assay, in vitro brine shrimp assay, in vivo cellular level bioassay using S. Pombe cells and anti-tuberculosis study. LC50 (50% lethal concentration) values of compounds are observed between 6.450 - 102.07?μg/mL. UV-vis absorption titration, competitive displacement assay, molecular docking and viscosity measurement were carried out to examine the binding type and binding strength of complexes. The binding studies suggest partial intercalative binding mode of the complexes and the observed binding constant (Kb) values are found in the order of 6d > 6b > 6c > 6a > 6e > 6?f. The anti-proliferative cytotoxicity of the synthesized PtII complexes (6a-6f) were tested against the HCT-116 (Human Colorectal Carcinoma) cancer cell line.
Synthesis of heteroleptic terpyridyl complexes of Fe(II) and Ru(II): Optical and electrochemical studies
Mondal, Prakash Chandra,Manna, Arun Kumar
supporting information, p. 5775 - 5781 (2016/07/16)
We report the synthesis and characterization of heteroleptic terpyridyl complexes of d6 transition metal ions with Fe2+ and Ru2+ (1-3). Furthermore, we study the effect of substitution of either an electron donating group (-NH2) or electron withdrawing group (-NO2) at the 4′-position in the ligands by means of UV-vis, cyclic voltammetry, and differential pulse voltammetry measurements. The experimentally observed photophysical characteristics of the transition-metal based terpyridyl complexes are explained and supported by detailed quantum chemical calculations.
