- Kinetic studies of pepsin active site model compound and porcine pepsin
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The kinetic parameters for the hydrolysis of the heptapeptide Pro-Thr-Glu-Phe-(4-NO2)Phe-Arg-Leu by the pepsin model compound tetrabutylammonium monosalt of m-aminobenzoic acid diamide of fumaric acid (TBA m-FUM) and porcine pepsin were determined using a spectrophotometric technique. According to the AS* values obtained, in the transition state the inner motion in the TBA m-FUM-heptapeptide complex is more restricted than that in the pepsin-heptapeptide complex. The model compound TBA m-FUM can cause a cleavage of the Phe -(4-NO2)Phe bond in the substrate molecules following a mechanism similar as that suggested for pepsin. but its catalytic activity is much lower. Copyright
- Swoboda, Bogdan,Beltowska-Brzezinska, Maria,Schroeder, Grzegorz,Brzezinski, Bogumil,Zundel, Georg
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Read Online
- Synthesis of a Thiophene Analogue of Isoindigo by C–H Activation/Oxidative Cyclization and Application of Its Copolymeric Materials to Organic Transistors
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A novel method for the synthesis of a thiophene analogue of isoindigo (TIIG) is described. The reaction involves a palladium-catalyzed C–H activation/oxidative cyclization sequence. This new methodology has potential for diversifying the isoindigo family. The thin-film transistors (TFTs) prepared from a TIIG-based copolymer (PIDTT-TIIG) with indacenodithieno[3,2-b]thiophene (IDTT) exhibit unipolar charge-transport properties with hole mobilities of 0.17 cm2 V–1 s–1.
- Wang, Hua-Chun,Tao, Jingwei,Bai, Wei-Yun,Xie, Zi-Yi,Li, Hongxiang,Ren, Xiancheng,Xu, Yun-Xiang
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Read Online
- Synthesis and characterization of ferrocenyl esters: Their anti-oxidant activity and DNA-binding ability
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In continuation to our work on biologically active material, some new ferrocenyl esters were prepared by condensation of 4-ferrocenyl phenol (ROH) with ferrocenyl dicarboxylic acid chlorides (DCC) at low temperature. The synthesized compounds (E1-E9) were characterized by analyzing their physical properties, FT-IR, 1H-NMR, UV-visible spectroscopic and cyclic voltammetric studies. The DPPH free radical scavenging assay was performed to explore their potential as antioxidant which showed that the E1 had maximum scavenging ability (77.11%) whereas E3 showed minimum (52%) compared with the standard. Cyclic voltammetric studies indicated that these compounds were electroactive in potential window of 2.0-0.0V. Binding mode found in these esters was an electrostatic interaction which is considered as strongest amongst all. Therefore, these compounds are considered to have DNA-binding capability and are potential DNA binders.
- Bukhari, Syeda Anam,Gul, Asghari,Akhter, Zareen,Bashir, Amna
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p. 375 - 382
(2018/06/06)
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- ADENYLYL CYCLASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND METHOD OF USE THEREOF
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The present invention relates to novel adenine based inhibitors of adenylyl cyclase of the formula: wherein X, L, R1, R2, R5 are those defined herein. Compounds of the present invention are useful to treat cardiovascular diseases. The present invention also relates to a method of preventing heart failure by administering an effective amount of compound according to the invention following vascular injury and reperfusion therapy.
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Paragraph 0251
(2018/01/20)
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- Undeca-nuclear-iron cluster compound as well as synthesis method and application thereof
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The invention discloses an undeca-nuclear-iron cluster compound as well as a synthesis method and application thereof. The chemical formula of the cluster compound is [Fe11(L)6(DMF)5(H2O)].4DMF.H2O.3C2H8N.0.5Py, wherein L represents N,N'-dis(salicylic acyl)-(E)-butenyl hydrazine; the ligand is subjected to six-hydrogen-atom removal and is charged with six negative charges, and three non-coordinated dimethylamine cations still exist outside. The synthesis method of the cluster compound comprises the following steps: dissolving the N,N'-dis(salicylic acyl)-(E)-butenyl hydrazine and FeCl3.6H2O with a mixed solvent, then adjusting the pH value of the obtained solution to be 5.3 to 5.9 with pyridine, putting the obtained mixed solution into a hydrothermal reaction kettle, performing reaction under a heating condition, cooling a reactant, and leaving to stand and crystallizing the reactant, namely obtaining the cluster compound. The anti-ferromagnetic exchange interaction exists among intramolecular iron ions of the cluster compound, so that the whole compound shows paramagnetism and can be used for preparing a magnetic material.
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Paragraph 0025; 0026
(2017/09/01)
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- Sixteen-core manganese cluster as well as synthetic method and application thereof
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The invention discloses a sixteen-core manganese cluster as well as a synthetic method and application thereof. The chemical formula of the cluster is [MnII4MnIII12(L)6([Mu]3-O)4H2O)12].7DMF.H2O, L indicates N,N'-di(salicyloyl)-(E)-butylene hydrazide taking off six hydrogen atoms with six units of negative charges. The coordination compound belongs to a triclinic system, P-1 space group. The synthetic method of the cluster comprises the following steps: taking N,N'-di(salicyloyl)-(E)-butylene hydrazide and Mn(OAc)2.4H2O to be dissolved with a mixed solvent, adjusting the pH of an obtained solution to be 5.1 to 5.6, putting the mixed solution into a hydrothermal reaction kettle, reacting in a heating condition, cooling the reaction product, and standing for crystallization to obtain the cluster. Antiferromagnetic exchange exists among manganese ions in molecules of the cluster disclosed by the invention, and the cluster has good adsorption effect for carbon dioxide gas.
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Paragraph 0024; 0025; 0026
(2017/09/02)
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- Preparation method of acyl chloride
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The invention relates to a preparation method of acyl chloride. The method comprises the following steps that 1, carboxylic acid is added into a reactor, or carboxylic acid is dissolved in organic solvent, a device is connected, and the temperature is raised to 100 DGE C-250 DEG C; 2, phosgene is introduced into the reactor for a reaction, and then the temperature is decreased to room temperature; 3, nitrogen is introduced, residual phosgene and hydrogen chloride are cleaned away, reaction liquid which is reacted without solvent is subjected to decompression distillation and purification directly, and needed acyl chloride is obtained; reaction liquid which is reacted with the solvent is subjected to decompression distillation to remove the solvent, and needed acyl chloride is obtained. According to the preparation method of acyl chloride, no catalyst is added, the risks that in the synthesizing process, due to the fact that the catalyst is dissolved, color of the finial product of acyl chloride is increased, and the catalyst is remained in late products are avoided, after the reaction is finished, high-quality acyl chloride can be obtained through decompression distillation, and the technological process is simple; due to the fact that in the whole technological process, except for absorbable and available phosgene, hydrogen chloride and carbon dioxide, no other three waste is discharged, the preparation method of acyl chloride is environmentally friendly, and the good implement value is achieved.
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Paragraph 0052; 0053
(2016/11/28)
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- Studies on the synthesis of bis-quaternary ammonium salts of geometrical isomers and its potential as bioregulators
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Tertiary amine N,N-dimethyl-2-nitrophenylmethanamine 4 prepared from 2-nitrobenzaldehyde 3 by Leuckart's reaction and (3-N,N-diethylamino-2- hydroxypropyl)-3-(3-nitrophenyl) prop-2-en-oate 9 and 3-(diethylamino)-2- hydroxypropyl 2-(4-chloro-3-methylphenoxy)acetate 14 prepared through the formation of glycidyl ester have been reacted with dichlorides of maleic acid and fumaric acid, which in turn have been prepared by reacting these acids with thionyl chloride to get bis-quaternary ammonium salts 1a-c and 2a-c. The synthesized salts 1a-c and 2a-c are tested on rice (Oryza sativa, PR-114) for their biological activity. All the tested compounds are found to possess good plant growth retardant activity. Compound 2c is found to be the best plant growth retardant among the six newly synthesized compounds.
- Seth, Anubhuti,Rani, Simmi,Garg, Anita,Sharma
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experimental part
p. 290 - 298
(2011/05/02)
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- Lewis acid-catalyzed one-pot, three-component route to chiral 3,3′-bipyrroles
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(Chemical Equation Presented) 3,3′-Bipyrroles 3 could be synthesized using a double Michael addition reaction involving diaroyl acetylene 1 and the appropriate 1,3-dicarbonyls 2 using ammonium acetate as a nitrogen source. The axial chirality of bipyrrole was anticipated from the X-ray crystal structure and DFT calculations and confirmed by separating the racemates on a chiral column and subsequent CD spectra of the enantiomers. The absolute configuration of the enantiomers was achieved by theoretical CD spectra calculation using the ZINDO method.
- Dey, Sumit,Pal, Churala,Nandi, Debkumar,Giri, Venkatachalam Sesha,Zaidlewicz, Marek,Krzeminski, Marek,Smentek, Lidia,Hess Jr., B. Andes,Gawronski, Jacek,Kwit, Marcin,Babu, N. Jagadeesh,Nangia, Ashwini,Jaisankar, Parasuraman
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supporting information; experimental part
p. 1373 - 1376
(2009/04/10)
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- Synthesis and characterization of 2-phenyl-4-benzoyl-6,7-dihydro-5H-cyclopenta[b]pyridine and its derivatives
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Amination-cyclization of triketones derived from variously substituted dibenzoyl ethylene and cyclopentanone furnished 2-phenyl-4-benzoyl-6,7-dihydro-5H-cyclopenta[b]pyridine and its derivatives.
- Rao, H. Surya Prakash,Senthilkumar,Jeyalakshmi
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- Synthesis and phospholipase A2 inhibitory activity of thielocin B3 derivatives.
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We prepared several types of derivatives of thielocin B3, a very potent naturally occurring inhibitor for human nonpancreatic secretory PLA2 (sPLA2-II), and conducted a structure-activity relationship study to identify potent sPLA2-II inhibitors with the aim of developing antiinflammatory drugs. The total number of aromatic rings is critical for sPLA2-II inhibition, and the best result was obtained in the case of six rings. The structure of the central part of the inhibitors was not specific, and potent inhibitors were found among the sulfide, sulfone, ether, methylene, and amino derivatives. Although a diester of the terminal carboxylic acid lost its inhibitory activity, having both of the carboxylic acids was not necessary for expression of activity, as illustrated by a glycine derivative with the benzyl ester group 36. Among the newly synthesized derivatives, 18, 20, 29, and 36 showed very potent human sPLA2-II inhibitory activity comparable to that of natural thielocin B3. Their IC50 values are in the range 0.069-0.14 microM, and they are a class of compounds showing the most potent sPLA2-II inhibition to date.
- Teshirogi,Matsutani,Shirahase,Fujii,Yoshida,Tanaka,Ohtani
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p. 5183 - 5191
(2007/10/03)
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- A Useful Synthesis of Chiral Glyoxylates
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A convenient synthesis of the cyclohexyl, (1R,3R,4S)-3-p-methyl and (1S-endo)-2-bornyl glyoxylates, from the respective alcohols and other very available materials, as a model applicable to that of other chiral, sensitive glyoxylates, is described.
- Fernandez, Franco,Garcia, Gerardo,Rodriguez, Jose E.
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p. 2837 - 2847
(2007/10/02)
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- Studies on Coordination Polymers of Fumaryl-bis-N-phenylhydroxamic Acid and Fumaryl-bis-N-m-tolylhydroxamic Acid with some Group III Elements
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Coordination polymers of fumaryl-bis-N-phenylhydroxamic acid (FPHA) and fumaryl-bis-N-m-tolylhydroxamic acid (FTHA) with some group III metals were synthesised.These coordination polymers have been characterised by their elemental analysis, ir and reflectance spectral data, conductance and DTA measurements.
- Kumari, Druga V.,Munshi, K. N.
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p. 191 - 194
(2007/10/02)
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- Synthesis of p-Phenylene-di-Acrylyl-Bis-N-Phenyl (PAPHA), Fumaryl-Bis-N-Phenyl (FPHA), Isophthalyl-Bis-N-Phenyl (IPHA) Hydroxamic Acids and Spectral and Magnetic Studies of their Polymers with Mn(II), Fe(II), Co(II), Ni(II), Cu(II) and Zn(II)
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Three new bis-ligands, PAPHA, FPHA and IPHA have been synthesized and their polymers with Mn(II), Fe(II), Co(II), Ni(II), Cu(II) and Zn(II) have been prepared.The compositions of the polymers have been proposed on the basis of elemental analysis, and their infrared and electronic spectra and magnetic susceptibilities have been reported.On the basis of these observations, their structures have been discussed.
- Gandhi, N. R.,Munshi, K. N.
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p. 1290 - 1295
(2007/10/02)
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- Optical brightening agents of naphthalimide derivatives
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A naphthalimide derivative having the formula STR1 wherein R is an alkyl, or cycloalkyl, an aralkyl, a haloalkyl, an alkoxyalkyl, a hydroxyalkyl, an N,N-dialkylaminoalkyl, an unsubstituted or halogen-, alkyl-, alkoxy- or hydroxy-substituted aryl, or an ammoniumalkyl; X is a group of the formula, STR2 wherein A is STR3 or an unsubstituted or halogen-substituted arylene, or a group of the formula, STR4 wherein R1 is hydrogen, an alkyl, phenyl, a hydroxyalkyl, or an alkoxyalkyl; Y is --CO--, --COO--, --CONR3 -- (where R3 is hydrogen or an alkyl), or --SO2 --; R2 is hydrogen, an alkyl, a cycloalkyl, an aralkyl, a haloalkyl, an alkyl- or aryl-substituted amino-alkyl, an unsubstituted or halogen-, alkyl-, alkoxy-, hydroxy-, amino- or alkylamino-substituted aryl, a group of the formula, STR5 (where R, R1 and Y are as defined above and R4 is a bivalent group), or a group of the formula, (where R5 is direct linkage or a bivalent group; Q+ is a substituted ammonium, a cycloammonium or a hydrazinium; and α- is an anion), Which is useful for optically brightening an organic polymer material.
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