- Efficient and Clean Aldol Condensation Catalyzed by Sodium Carbonate in Water
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Efficient and environmentally friendly synthesis of chalcone and azachalcone was performed by aldol condensation of aldehydes with ketones in pure water catalyzed by sodium carbonate. In this convenient methodology, side reactions were avoided and thus high yields were achieved.
- Zhang, Ze,Dong, Ya-Wei,Wang, Guan-Wu
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- Chalcone-derived thiosemicarbazones and their zinc(II) and gallium(III) complexes: Spectral studies and antimicrobial activity
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Chalcone-derived 3-phenyl-1-pyridin-2-ylprop-2-en-1-one thiosemicarbazone (HPyCTPh) (1), 3-(4-chlorophenyl)-1-pyridin-2-ylprop-2-en-1-one thiosemicarbazone (HPyCT4ClPh) (2), 3-(4-bromophenyl)-1-pyridin-2-ylprop-2-en-1- one thiosemicarbazone (HPyCT4BrPh) (
- Silva, Jeferson G. Da,Perdigao, Camila C. H.,Speziali, Nivaldo L.,Beraldo, Heloisa
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- Synthesis of azachalcones, their α-amylase, α-glucosidase inhibitory activities, kinetics, and molecular docking studies
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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
- Saleem, Faiza,Kanwal,Khan, Khalid Mohammed,Chigurupati, Sridevi,Solangi, Mehwish,Nemala, Appala Raju,Mushtaq, Maria,Ul-Haq, Zaheer,Taha, Muhammad,Perveen, Shahnaz
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- Coordination-driven self-assembly of anthraquinone-based metal-organic cages for photocatalytic selective [2 + 2] cycloaddition
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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
- Cui, Yong,Jiang, Hong,Jin, Yao,Liu, Yan,Tang, Xianhui,Zhang, Wenqiang
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supporting information
p. 8533 - 8539
(2021/06/28)
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- An Efficient Cyclic Di-AMP Based Artificial Metalloribozyme for Enantioselective Diels–Alder Reactions
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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.
- Qi, Qianqian,Lv, Shuting,Hao, Min,Dong, Xingchen,Gu, Youkun,Wu, Peizhe,Zhang, Wenyue,Chen, Yashao,Wang, Changhao
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p. 4417 - 4424
(2020/06/17)
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- Synthesis, characterization and biological application of pyrazolo[1,5-a]pyrimidine based organometallic Re(I) complexes
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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 =
- Bhatt, Bhupesh S.,Pandya, Juhee G.,Patel, Mohan N.,Pathak, Chandramani,Vaidya, Foram U.,Varma, Reena R.
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p. 957 - 969
(2020/10/02)
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- 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
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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
- Markad, Datta,Khullar, Sadhika,Mandal, Sanjay K.
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supporting information
p. 12547 - 12554
(2019/10/11)
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- Design, synthesis, pharmacological evaluation and DNA interaction studies of binuclear Pt(II) complexes with pyrazolo[1,5-a]pyrimidine scaffold
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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.
- Lunagariya, Miral V.,Thakor, Khyati P.,Waghela, Bhargav N.,Pathak, Chadramani,Patel, Mohan N.
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- Halo-substituted chalcones and azachalcones-inhibited, lipopolysaccharited-stimulated, pro-inflammatory responses through the TLR4-mediated pathway
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A series of B-ring, halo-substituted chalcones and azachalcones were synthesized to evaluate and compare their anti-inflammatory activity. Mouse BALB/c macrophage RAW 264.7 were pre-treated with 10 μg/mL of each compound for one hour before induction of i
- Shih, Tzenge-Lien,Liu, Ming-Hwa,Li, Chia-Wai,Kuo, Chia-Feng
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- N1-benzenesulfonyl-2-pyrazoline hybrids in neurological disorders: Syntheses, biological screening and computational studies
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A novel series of 1,3,5-trisubstituted-2-pyrazolines (5a-5t) was prepared via Claisen Schmidt condensation, followed by heterocyclization with hydrazine hydrate, substitution of N1 hydrogen of 2-pyrazoline nucleus with 4-chlorobenzenesulfonylchloride, app
- Tripathi, Avinash C.,Upadhyay, Savita,Paliwal, Sarvesh,Saraf, Shailendra K.
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p. 126 - 148
(2018/02/14)
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- Derivatives of 4,5-dihydro (1H) pyrazoles as possible MAO-A inhibitors in depression and anxiety disorders: synthesis, biological evaluation and molecular modeling studies
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A series of 1,3,5-trisubstituted-2-pyrazoline derivatives (3a–3t) were synthesized in appreciable yields by substituting N1 position of 2-pyrazoline nucleus with 4-nitrobenzenesulfonylchloride using conventional and microwave assisted synthetic approaches
- Tripathi, Avinash C.,Upadhyay, Savita,Paliwal, Sarvesh,Saraf, Shailendra K.
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p. 1485 - 1503
(2018/03/29)
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- Half Sandwich Rhodium(III) and Iridium(III) Complexes as Cytotoxic and Metallonuclease Agents
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Half sandwich complexes of the type [(η5-C5Me5)M(L1–3)Cl]Cl.2H2O were synthesized using [{(η5-C5Me5)M(μ-Cl)Cl}2], where M = Rh(III)/Ir(III) and L1–3 = pyrim
- Vekariya, Pankajkumar A.,Karia, Parag S.,Bhatt, Bhupesh S.,Patel, Mohan N.
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- Solvent-free enantioselective conjugate addition and bioactivities of nitromethane to Chalcone containing pyridine
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A series of chiral thioureas derived from quinine were tested as catalysts in the enantioselective Michael additions of nitromethane to α,β-unsaturated ketones containing pyridine. The best results were obtained with the bifunctional catalyst prepared from 3,5-di(trifluoromethyl)-aniline under solvent-free conditions. This thiourea promoted the reaction with high enantioselectivities and chemical yields for aryl ketones. The origins of enantioselectivity were further investigated via experiment and computation. Meanwhile, the products from our reaction showed potent antibacterial activities against rice bacterial leaf blight, with the S-enantiomer performing much better than the R-enantiomer. Given the promising bioactivity of this class of molecules, our work is expected to offer important applications in developing future generations for drug design.
- Zhang, Guoping,Zhu, Chun,Liu, Dengyue,Pan, Jianke,Zhang, Jian,Hu, Deyu,Song, Baoan
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p. 129 - 136
(2016/12/23)
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- Reinvestigation of synthesis of halo-substituted 3-phenyl-1-(2-pyridyl)-2-propen-1-ones (azachalcones). A tandem reaction for formation of penta-substituted cyclohexanols
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A systematic study of the synthesis of halo-substituted azachalcones was conducted. During the reaction course, we obtained not only the target azachalcones, but also penta-substituted cyclohexanols, which are seldom reported in the literatures. The forma
- Li, Chia-Wai,Shen, Tzu-Hsuan,Shih, Tzenge-Lien
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p. 4644 - 4652
(2017/07/11)
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- An expeditious one-pot microwave facilitated versus conventional syntheses: In vivo biological screening and molecular docking studies of some 3,5-disubstituted-4,5-dihydro-(1H)-pyrazole derivatives
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A series of 3,5-disubstituted-2-pyrazoline derivatives (2a-2t) were synthesized by reacting different aromatic/heteroaromatic aldehydes and ketones, in a two-step reaction through Claisen Schmidt condensation, followed by cyclization of the resulted chalc
- Tripathi, Avinash C.,Upadhyay, Savita,Paliwal, Sarvesh,Saraf, Shailendra K.
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p. 390 - 406
(2016/02/19)
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- N-Heterocyclic carbene-catalyzed diastereoselective synthesis of β-lactone-fused cyclopentanes using homoenolate annulation reaction
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NHC-catalyzed annulation of enals with 2-enoylpyridines or 2-enoylpyridine N-oxides leading to the diastereoselective synthesis of β-lactone-fused cyclopentanes is reported. The reaction proceeds via the generation of homoenolate equivalent intermediates and tolerates a broad range of functional groups.
- Mukherjee, Subrata,Mondal, Santigopal,Patra, Atanu,Gonnade, Rajesh G.,Biju, Akkattu T.
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supporting information
p. 9559 - 9562
(2015/06/08)
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- EGFR/HER-2 inhibitors: Synthesis, biological evaluation and 3D-QSAR analysis of dihydropyridine-containing thiazolinone derivatives
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A series of dihydropyridine containing thiazolinone derivatives (4a-4r) have been designed, synthesized and their biological activities evaluated as potential EGFR and HER-2 kinase inhibitors and in tumor cell antiproliferation. The synthesized compounds
- Ren, Yu-Jia,Wang, Zhong-Chang,Zhang, Xin,Qiu, Han-Yue,Wang, Peng-Fei,Gong, Hai-Bin,Jiang, Ai-Qin,Zhu, Hai-Liang
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p. 21445 - 21454
(2015/03/30)
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- Diastereo- and enantioselective direct vinylogous Michael addition of γ-substituted butenolides to 2-enoylpyridines catalyzed by chiral bifunctional amine-squaramides
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The diastereo- and enantioselective direct vinylogous Michael addition reaction of γ-substituted butenolides to 2-enoylpyridines has been achieved. A range of γ,γ-disubstituted butenolide derivatives, bearing two consecutive tri- and tetrasubstituted stereogenic centers, were readily obtained in good yields with excellent stereoselectivities (up to >99:1 dr and >99% ee).
- Wang, Zhen-Hua,Wu, Zhi-Jun,Huang, Xue-Qun,Yue, Deng-Feng,You, Yong,Xu, Xiao-Ying,Zhang, Xiao-Mei,Yuan, Wei-Cheng
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supporting information
p. 15835 - 15838
(2015/11/10)
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- Synthesis, physicochemical properties, antimicrobial and antioxidant studies of pyrazoline derivatives bearing a pyridyl moiety
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A series of new pyrazoline compounds bearing a pyridyl moiety (4a-i) were synthesized by condensing appropriate chalcones with hydrazine hydrate and tested for antimicrobial and antioxidant activities. According to in vitro antimicrobial activity against Bacillus subtilis, Staphylococcus epidermidis, Proteus vulgaris, Pseudomonas aeruginosa, Aspergillus niger and Penicillium chrysogenum and antioxidant activity by DPPH method, the compounds 4a, 4d, 4i and 4e, 4f, 4h showed maximum antimicrobial and antioxidant activities, respectively. Physiochemical properties and Lipinski's 'Rule of Five' analysis predicted higher intrinsic quality of the synthesized compounds and revealed that these compounds have good bioavailability and druglikeness properties.
- Lone, Imtiyaz Hussain,Khan, Khaliquz Zaman,Fozdar, Bharat Inder
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p. 363 - 369
(2014/03/21)
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- Spectral studies of 2-pyrazoline derivatives: Structural elucidation through single crystal XRD and DFT calculations
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A series of biologically active N-thiocarbamoyl pyrazoline derivatives have been synthesized using anhydrous potassium carbonate as the catalyst. All the synthesized compounds were characterized by FT-IR, 1H NMR, 13C NMR spectral stu
- Chinnaraja,Rajalakshmi,Srinivasan,Velmurugan,Jayabharathi
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supporting information
p. 30 - 33
(2014/02/14)
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- Novel 2-pyrazoline derivatives as potential anticonvulsant agents
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A series of new 2-pyrazoline derivatives has been synthesized by reacting 3-(substituted-phenyl)-1-pyridin-2-yl-propenones using two routes one using thiosemicarbazide and the other by hydrazine hydrate. The chemical structures were established by IR, Mas
- Bhandari, Shradha,Tripathi, Avinash C.,Saraf, Shailendra K.
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p. 5290 - 5296
(2013/12/04)
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- A new selective fluorescent sensor for Fe3+ based on a pyrazoline derivative
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(Graph Presented) A new pyrazoline derivative was designed and synthesized. The structure of the pyrazoline was confirmed by single crystal X-ray diffraction and its photophysical properties were studied by absorption and fluorescence spectra. This compound can be used to determine Fe3+ ion with high selectivity among a series of cations in tetrahydrofuran and even in aqueous tetrahydrofuran. This sensor forms a 1:1 complex with Fe3+ and displays fluorescent quenching.
- Hu, Shengli,Zhang, Shushu,Gao, Chan,Xu, Caihua,Gao, Qing
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p. 325 - 331
(2014/01/23)
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- Spectroscopic study of DNA hydrolysis, DNA intercalative, and electrostatic interaction activity exerted by drug based coordination compounds
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Our work emphasized on synthesizing and characterizing neutral mononuclear copper(II) complexes with second generation fluoroquinolone drug ciprofloxacin (CFL) and some bipyridine derivatives (An) of type [Cu(CFL)(A n)Cl]·2H2/s
- Patel, Mohan N.,Bhatt, Bhupesh S.,Dosi, Promise A.
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scheme or table
p. 152 - 162
(2012/03/13)
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- ALLOSTERIC PROTEIN KINASE MODULATORS
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The invention provides specific small molecule compounds that allosterically regulate the activity or modulate protein-protein interactions of AGC protein kinases and the Aurora family of protein kinases, methods for their production, pharmaceutical compositions comprising same, and their use for preparing medicaments for the treatment and prevention of diseases related to abnormal activities of AGC protein kinases or of protein kinases of the Aurora family.
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Page/Page column 142
(2010/04/30)
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- Synthesis of substituted 1-(2-arylvinyl)-2-azolyl-1-pyridylethanols-1
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A series of new 1-(2-arylvinyl)-2-azolyl-1-pyridylethanols-1 has been obtained with various positions of the nitrogen atom in the pyridine fragment and with substituents in the benzene ring, by the reaction of (2-arylvinyloxiran-2-yl)pyridines with triazole and imidazole, for agrochemical screening. The compounds mentioned displayed high fungicidal activity.
- Zakharychev,Kuzenkov
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p. 989 - 995
(2008/09/19)
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- Phenyl-substituted 2,2′:6′,2″-terpyridine as a new series of fluorescent compounds - Their photophysical properties and fluorescence tuning
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Several phenyl-substituted 2,2′:6′,2″-terpyridines (tpy) were synthesized and it was found that 4′-phenyl tpy (ptp, 3) exhibited the most effective fluorescence, whose quantum yield was up to 0.64 in cyclohexane. For further study on tuning the fluorescence properties of ptp, different substituents were introduced into the p-position of the phenyl group. While Br- 10, Cl- 11, and CH3-ptp 12 showed their absorption and fluorescence in the same region as 3, those of NH2- 14 and Me2N-ptp 15 were observed at much longer wavelengths. In addition, fluorescence maxima of 14 and 15 showed large (> 130 nm) solvent dependence. The difference between ground and excited state dipole moment (Δμ) for 15 was estimated to be 15.2 D by the Lippert-Mataga equation, indicating the intramolecular charge transfer (ICT) process. Semi-empirical MO calculation (MOPAC/AM1) demonstrated that the HOMO-1, HOMO and LUMO of 3, 10-12 were mainly localized on the phenyl (πph), tpy (πtpy) and tpy (π*tpy) part, respectively, indicating that the lowest energy absorption band of 3, 10-12 was the local excitation (πtpy-π*tpy). In the case of 14 and 15, which have an electron-donating substituent, πph instead of πtpy became the HOMO. Thus, the lowest energy absorption of 14 and 15 was an ICT transition (πph-π*tpy), and a large red shift of the fluorescence occurred. In these compounds, the energy level of πph is controlled without affecting that of πtpy and π*tpy, suggesting a novel approach for tuning the color of fluorescence.
- Mutai, Toshiki,Cheon, Jin-Dong,Arita, Shinpei,Araki, Koji
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p. 1045 - 1050
(2007/10/03)
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- Lewis acid catalysis of a Diels-Alder reaction in water
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Here we report the first detailed study of a Diels-Alder (DA) reaction that is catalyzed by Lewis acids in water. The effect of Co2+, Ni2+, Cu2+ and Zn2+ ions as Lewis acid catalysts on the rate and endo-exo selectivity of the DA reaction between the bidentate dienophiles 3-phenyl-1-(2-pyridyl)-2-propen-1-ones (1a-e) and cyclopentadiene (2) in water has been studied. Relative to the uncatalyzed reaction in acetonitrile, catalysis by 0.010 M Cu(NO3)2 in water accelerates the reaction by a factor of 79300. The kinetics of the catalyzed reaction were analyzed in terms of equilibrium constants for complexation of the Lewis acid with 1a-e and rate constants for the reaction of the resulting complexes with 2. The rate enhancement imposed upon the uncatalyzed DA reaction of substrates 1 with 2 by water is much more pronounced than that for the catalyzed reaction. The increase of the endo-exo selectivity induced by water in the uncatalyzed process is completely absent for the Lewis acid catalyzed reaction. The modest solvent and substituent effects observed for the catalyzed reaction indicate that the change in charge separation during the activation process is not larger than the corresponding change for the uncatalyzed reaction.
- Otto, Sijbren,Bertoncin, Federica,Engberts, Jan B. F. N.
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p. 7702 - 7707
(2007/10/03)
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- PHARMACEUTICAL USE OF TERPYRIDINE DERIVATIVE
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A terpyridine derivative represented by general formula (I) (wherein R represents hydrogen, (un)substituted phenyl, pyridyl, etc.), which has the effect of promoting the production of nerve growth factors or a neurotrophic factor activity. Hence it can be
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