- One-dimensional Europium-coordination polymer as luminescent sensor for highly selective and sensitive detection of 2,4,6-trinitrophenol
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Three isostructural lanthanide coordination polymers (LnCPs), [Ln(L)6(DMF)]n {HL = 2-(2-formylphenoxy) acetic acid, Ln = Sm (1); Eu (2); Tb (3)} have been synthesized by solvothermal reaction and characterized. Single crystal analyse
- Gao, Hongyan,Li, Dongping,Li, Yongxiu,Liu, Yanzhu,Sun, Qingyan,Zhou, Hongbo
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- HEMIAMINAL-TAG FOR PROTEIN LABELING AND PURIFICATION
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The invention pertains to the synthesis, isolation, and characterization of hemiaminal for selective labeling of peptides, proteins, antibodies, and organic fragments with -C(=0) CH2NH2 and derivatives with -CH2NH2 group over -C(=0) CHRNH2 group (where R≠H). The invention also pertains to the method of single-site immobilization of proteins through N-terminus Gly on solid phase. The invention includes late-stage tagging of N-terminus Gly with an affinity tag, 19F NMR probe, and a fluorophore and a method for metal-free protein purification and isolation of analytically pure proteins.
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- Organocatalytic Synthesis of Fused Bicyclic 2,3-Dihydro-1,3,4-oxadiazoles through an Intramolecular Cascade Cyclization
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Hydrazone-carboxylic acids undergo intramolecular cyclization in the presence of pivaloyl chloride, iPr2NEt, and catalytic DABCO to form a range of substituted fused tricyclic 2,3-dihydro-1,3,4-oxadiazoles in high yields.
- Fugard, Alison J.,Thompson, Bethany K.,Slawin, Alexandra M. Z.,Taylor, James E.,Smith, Andrew D.
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supporting information
p. 5824 - 5827
(2015/12/11)
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- Design, synthesis, and biological evaluation of thiazolidine-2,4-dione conjugates as PPAR-γ agonists
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A library of synthesized conjugates of phenoxy acetic acid and thiazolidinedione 5a-m showed potent peroxisome proliferator activated receptor-γ (PPAR-γ) transactivation as well as significant blood glucose lowering effect comparable to the standard drugs pioglitazone and rosiglitazone. Most of the compounds showed higher docking scores than the standard drug rosiglitazone in the molecular docking study. Compounds 5l and 5m exhibited PPAR-γ transactivation of 54.21 and 55.41%, respectively, in comparison to the standard drugs pioglitazone and rosiglitazone, which showed 65.94 and 82.21% activation, respectively. Compounds 5l and 5m significantly lowered the blood glucose level of STZ-induced diabetic rats. Compounds 5l and 5m lowered the AST, ALT, and ALP levels more than the standard drug pioglitazone. PPAR-γ gene expression was significantly increased by compound 5m (2.00-fold) in comparison to the standard drugs pioglitazone (1.5-fold) and rosiglitazone (1.0-fold). Compounds 5l and 5m did not cause any damage to the liver and could be considered as promising candidates for the development of new antidiabetic agents.
- Nazreen, Syed,Alam, Mohammad Sarwar,Hamid, Hinna,Yar, Mohammad Shahar,Dhulap, Abhijeet,Alam, Perwez,Pasha, Mohammad Abdul Qadar,Bano, Sameena,Alam, Mohammad Mahboob,Haider, Saqlain,Kharbanda, Chetna,Ali, Yakub,Pillai, Kolakappi
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p. 421 - 432
(2015/06/08)
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- A new fluorescent pH probe for imaging lysosomes in living cells
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A new rhodamine B-based pH fluorescent probe has been synthesized and characterized. The probe responds to acidic pH with short response time, high selectivity and sensitivity, and exhibits a more than 20-fold increase in fluorescence intensity within the pH range of 7.5-4.1 with the pKa value of 5.72, which is valuable to study acidic organelles in living cells. Also, it has been successfully applied to HeLa cells, for its low cytotoxicity, brilliant photostability, good membrane permeability and no 'alkalizing effect' on lysosomes. The results demonstrate that this probe is a lysosome-specific probe, which can selectively stain lysosomes and monitor lysosomal pH changes in living cells.
- Lv, Hong-Shui,Huang, Shu-Ya,Xu, Yu,Dai, Xi,Miao, Jun-Ying,Zhao, Bao-Xiang
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supporting information
p. 535 - 538
(2014/01/23)
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- In situ Bronsted-Lowry acid catalyzed syntheses, characterization, single crystal XRD, electronic spectral-, DPPH radical scavenging-, and DNA protection studies of aryl-3,3′-bis(indolyl)methanes
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A series of novel aryl-3,3′-bis(indolyl)methanes (BIMs) were synthesized using indole and formylphenoxyaliphatic acid(s) in water in the absence of any catalyst. The formylphenoxyaliphatic acid behaves as an in situ Bronsted-Lowry acid catalyst in water. UV-Visible and fluorescence spectra of the compounds were recorded in selected solvents. The gas phase geometry optimization of the compounds were achieved using DFT calculations at B3LYP/3-21G(*) level of theory. The electronic properties, such as HOMO-LUMO energies were calculated using the above method based on the optimized structure. Compounds have better DPPH radical scavenging activity and reduction of oxidative damage of DNA.
- Suresh Kumar,Antony Muthu Prabhu,Seethalaksmi,Bhuvanesh,Kumaresan
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supporting information
p. 249 - 256
(2014/01/23)
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- POLYMORPHIC FORM OF 5-(4-[4-(5-CYANO-1H-INDOL-3-YL) BUTYL] PIPERAZIN-1-YL) BENZOFURAN-2-CARBOXAMIDE AND PROCESS FOR PREPARING THEREOF
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The present invention provides a solid state Form-Z of 5-(4-[4-(5-cyano-1H-indol-3-yl)butyl]piperazin-1-yl)benzofuran-2-carboxamide. The present invention also provides a process for preparing Form-Z of 5-(4-[4-(5-cyano-1H-indol-3-yl)butyl]piperazin-1-yl)benzofuran-2-carboxamide comprising the steps of i) reacting solid state form of 5-(1-piperazinyl)benzofuran-2-carboxamide or its salts with 3-(4-chlorobutyl)-1H-indole-5-carbonitrile an organic solvent in presence of a base to obtain crude vilazodone free base; ii) purifying the crude vilazodone free base of step (i) in an organic solvent; iii) treating the purified vilazodone free base of step (ii) with an organic solvent to obtain solid state form-Z of vilazodone. The present invention further provides a pharmaceutical composition comprising a therapeutically effective amount of an amorphous form of vilazodone hydrochloride and use of solid state Form-Z of vilazodone for the treatment of major depressive disorders.
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Paragraph 0080
(2014/07/08)
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- An efficient one pot syntheses of aryl-3,3′-bis(indolyl)methanes and studies on their spectral characteristics, DPPH radical scavenging-, antimicrobial-, cytotoxicity-, and antituberculosis activity
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An efficient one-pot syntheses of aryl-3,3′-bis(indolyl)methanes (BIMs) from indole/2-methylindole and formylphenoxyaliphatic acid(s) is described. Esterification of carboxylic acid and aromatic electrophilic substitution reactions are achieved simultaneous in the presence of potash alum as a catalyst. This catalyst could be recovered and reused without substantial loss in its catalytic activity and the methodology could be applied on a range of closely related substrates. The solvation characteristics in ground and excited states of the compounds by monitoring the absorbance and fluorescence band maxima have been studied. The fluorescence studies in protic and aprotic solvents were rationalized on the basis of solute-solvent interaction and substituents effect on these photophysical processes analyzed. The compounds prepared showed efficient antimicrobial effect against human pathogens, cytotoxicity against A431 cell line, and DPPH radical scavenging effect. Single crystal XRD studies have been carried out for a few compounds synthesized in this work.
- Suresh Kumar,Kumaresan,Antony Muthu Prabhu,Bhuvanesh,Seethalakshmi
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supporting information
p. 254 - 263
(2013/02/23)
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- POLYMORPHIC FORM OF 5-(4-[4-(5-CYANO-1H-INDOL-3- YL)BUTYL]PIPERAZIN-1-YL) BENZOFURAN-2-CARBOXAMIDE
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The present invention relates to a process for the preparation of 5-(4-[4-(5- cyano- 1 H-indol-3 -yl)butyl] piperazin- 1 -yl)benzofuran-2-carboxamide of Formula (1) or its pharmaceutically acceptable salt, solvates or hydrates thereof. In particular, the present invention provides a novel intermediate compound, 5-(4-substitutedpiperazin- 1-yl)benzofuran-2-carboxamide of Formula (X). The present invention further provides solid state form of 5-(4-[4-(5-cyano-1H-indol-3- yl) butyl]piperazin-1-yl)benzofuran-2-carboxamide of Formula (1) and process for its preparation.
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Page/Page column 21
(2014/01/07)
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- Synthesis and QSAR analysis of chalcone derivatives as nitric oxide inhibitory agent
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In this study, thirty-eight chalcone analogs were synthesized and evaluated for nitric oxide (NO) inhibition activity on RAW 264.7 cells. Among these compounds, chalcones bearing furanyl group showed remarkable anti-inflammatory activity. Both compounds 2d and 2j were identified as the most potent NO inhibitor on IFN-γ/LPS-activated RAW 264.7 cells. In order to examine the structure-activity relationship, a 3D QSAR analysis was carried out by comparative molecular field analysis (CoMFA) method on the selected chalcones. Partial least square analysis produced a statistically coherent model with good predictive value, r2 = 0.989 and a good cross validated value, q 2 = 0.583.
- Lam, Kok Wai,Lajis, Nordin H.,Uddin, Reaz,Ul-Haq, Zaheer,Liew, Choi Yi,Tham, Chau Ling,Israf, Daud A.,Syahida, Ahmad,Rahman, Mohd. Basyaruddin Abdul
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p. 1953 - 1966,14
(2020/07/30)
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- Synthesis and antimicrobial activity of Schiff bases derived from 2-Formylphenoxy acetic acid
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A series of seven Schiff bases were synthesized by reacting 2-formylphenoxy acetic acid with aromatic amines. The chemical structures of these compounds were confirmed by means of IR and 1H NMR. The compounds were assayed by the disc diffusion method for antibacterial activity against Staphylococcus aureus and Escherichia coli. Among the compounds tested, V1, V3, V4 and V6, exhibited good antibacterial activity, almost equal to that of ampicillin used as standard drug.
- Bala, Veenu,Chhonker,Hashim
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body text
p. 3447 - 3452
(2010/11/04)
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- Selective recognition of sodium cyanide and potassium cyanide by diaza-crown ether-capped Zn-porphyrin receptors in polar solvents
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Two new ditopic porphyrin receptors Zn1, incorporating a diaza-15-crown-5 unit, and Zn2, incorporating a diaza-18-crown-6 unit, have been prepared and characterized. UV-vis study in polar methanol has revealed that Zn1 is able to selectively recognize sodium cyanide over potassium cyanide (the ratio of their binding constant is ca. 56), whereas Zn2 exhibits a higher binding affinity for potassium cyanide over sodium cyanide (the ratio of their binding constant is ca. 12). In contrast, both receptors display substantially weaker binding affinity for sodium thiocyanate and potassium thiocyanate presumably due to a monotopic binding fashion.
- Liu, Hui,Shao, Xue-Bin,Jia, Mu-Xin,Jiang, Xi-Kui,Li, Zhan-Ting,Chen, Guang-Ju
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p. 8095 - 8100
(2007/10/03)
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- Asymmetric synthesis of polymer-supported cyanohydrin acetates
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A bimetallic titanium(salen) complex has been used to catalyze the asymmetric addition of potassium cyanide to aldehydes attached to Wang resin giving polymer supported cyanohydrin propionates with up to 91% enantiomeric excesses.
- Belokon', Yuri N.,Carta, Paola,North, Michael
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p. 4483 - 4486
(2007/10/03)
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- Electrosynthesis of substituted benzolactones by a nickel-catalyzed allyl transfer reaction from allyl benzoates
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Allyl-substituted benzolactones were obtained in good yields from allyl o-carbonyl benzoates in a Ni-catalyzed electrochemical reaction involving allyl cleavage, intramolecular allyl transfer to the carbonyl group and lactone formation, in a one-step procedure under mild conditions.
- Franco,Du?ach
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p. 806 - 808
(2007/10/03)
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- Process for nucleophilic fluoroalkylation of aldehydes
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Aryl difluoromethyl sulfone adds to alkehydes under phase transfer conditions to give novel substituted alcohols of the general formula wherein R is an aryl, cycloaliphatic, sec- or tert-aliphatic, or heterocyclic group and Ar is an aryl group. The substituted alcohols of formula I are of particular utility as intermediates in the synthesis of a variety of useful end products. For example, the products of formula I may be utilized in desulfonylation reactions, oxidation reactions and fluorination reactions.
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