Der Pharma Chemica

DNA methyltransferases catalyses the transfer of methyl group to DNA. However, in the current study, a series of DNA methyltransferase inhibitors and new compound with better efficacy were predicted. Hence quantitative structure activity relationship (QSAR) studies were done on the series of constrained (L-)-S-adenosyl-L-homocysteine (SAH) analogues acting as DNA methyltransferase inhibitors, and afterwards followed by molecular modelling which gives cross-validated result (r 2 cv) of 0.653 carried out by Leave one out (LOO) method, and predicted (r 2 pred.) is 0.600 with coefficient of correlation of (r) get by the multiple regression analysis is 0.934. Based on the model generated by the quantitative structure-activity relationship (QSAR) series of new compounds have been generated. Then these compounds were docked with the protein and ADME properties of each of the newly proposed compounds were studied using SwissADME that highlights properties of the compounds, their lipophilicity, solubility, drug likeliness, pharmacokinetics, etc. Toxicity prediction of these compounds is also made using PROTOX 2, making them suitable leads against DNA methyltransferase.

Arshita Jindal

Anjali Sharma

Neeraj Agarwal

Der pharma chemica

Quantitative Structure-Activity Relationship and Molecular Modeling Studies on a series of constrained (L-)-S-adenosyl-L-homocysteine (SAH) analogues acting as DNA methyltransferase inhibitors.

定量构效关系与分子建模研究：一系列作为DNA甲基转移酶抑制剂的受限(L)-S-腺苷-L-高半胱氨酸(SAH)类似物。

Due to their importance as catalysts in many reactions and their biological activities, an interest in the synthesis and characterization of transition metal complexes containing Schiff bases is increasing. The major aim of this study was to compare the antibacterial activity of the ligands with their metal complexes. We have successfully synthesized Cu (II), Ni (II) and Co (II) complexes of N, N-Bis(vanillinidene )-1,2-phenylenediamine and N,N-Bis(salicylidene)-1,2-phenylenediamine. The Schiff’s bases were synthesized by the reaction of o-phenylenediamine with salisaldehyde or o-vanillin and their metal complex were synthesized by the reaction of the ligands with the metal salts. The structure of all the synthesized ligands were confirmed using NMR, IR and UV-Vis spectral analysis and their metal complexes were confirmed using IR and UV-vis spectra. The synthesized ligands and their metal complexes were screened for their antibacterial activities against Escherichia coli, Staphylococcus aureus, and Klebsiella pneumonia bacterial strains by using disc diffusion method. Among the synthesized compounds, the ligand L1 is moderately active against Staphylococcus aureus, K. pneumonia and Escherichia coli bacteria strain, CoL1 exhibited the highest activity, with 22mm zone of inhibition against staphylococcus aureus, compared to standard gentamycin activity, with 21 mm zone of inhibition.

Salah Hamza Sherif

Dagne Addisu Kure

Endalkachew Asefa Moges

Akmal Nur Negash

Daniel Mamo

Synthesis, characterization and antibacterial activity of Schiff base of Cu (II), Ni (II) and Co (II) complexes

铜(II)、镍(II)和钴(II)席夫碱配合物的合成、表征及抗菌活性研究

This study was designed to investigate the pharmacotoxicity of methanolic extracts of Punica granatum cortex and Zingiber officinales rhizome at different doses 800,400 and 200mg/kg to rats via oral route, The methanolic extract of Punica granatum cortex (400 mg/kg+ PHA) in days 45 showed significant increase in IL-2 and IL-6 level. While the methanolic extract of Zingiber officinales rhizome (400 mg/kg+ PHA) in days 45, showed significant increase in IL-10 level.

Esraa. M.M. Ali

Hasan M.H. Muhaisen

GC.MS Analysis and Immuo Modulatory Activities of Punica granatum (Cortex) and Zingiber officinales (rhizome)

GC.MS分析及石榴皮和姜的免疫调节活性

The work describes a precise, accurate and reproducible Reverse Phase High Performance Liquid Chromatographic (RP-HPLC) method for development and validation of Pioglitazone in tablet dosage form on Lachrome Liquid chromatographic system having PDA-20 A UV/VIS Detector using stationary phase C18 column (300 mm × 3.9 mm, 5 μm, particle size) and acetonitrile:phosphate buffer, (50:50 v/v) as mobile phase at flow rate of 1.00 ml/min and the detection wavelength was 267 nm. The retention time for Pioglitazone was found to be 8.08 min. The method was validated for precision, accuracy, linearity range, robustness, system stability, as per ICH guidelines Q2(R1).

Meenaxi M. Maste

Nikhil S. Gawas

Utkarsh Shashtri

Poonam Shelar

RP-HPLC Method Development and Validation for Pioglitazone in Bulk and Marketed Formulation

批量和市售制剂中吡格列酮的RP-HPLC方法开发与验证

In this research, a new quinoline derivative, 7-((2-aminoethyl)amino)-5-bromo-6-hydroxy-1- methylquinolin-1-ium-3-sulfonate (QEt) as well as six complexes of Co(II), Ni(II), Cu(II), Zn(II), Cd(II) and Hg(II) with this ligand [M(QEt-1H)2].nH2O (M: Co, Cu, Zn, Cd, Hg), [Ni(QEt-1H)Cl].2H2O were synthesized. The molecular formulas and structures of the complexes were determined using measurement as IR, EDX, ESI-MS, 1H NMR spectra and thermal analysis. The bioactivity tests shown that the ligand and CuQEt complex have limiting effects to microorganisms, complexes CoQEt, ZnQEt, CdQEt and HgQEt exhibit antibacterial activities with low IC50 values, from 0.5 to 56.0 μg/mL and be most effective to Bacillus subtilis. Especially HgQEt inhibits effectively to almost types of bacteria.

Mai Phuong Chi

Nguyen Thi Quy

Le Thi Hong Hai

Synthesis, Structural Characterization, Antimicrobial Activity of Complexes of Co(II), Ni(II), Cu(II), Zn(II), Cd(II) With 7-((2-Aminoethyl)Amino)-5-Bromo-6-Hydroxy-1-Methylquinolin-1- Ium-3-Sulfonate

合成、结构表征及Co(II)、Ni(II)、Cu(II)、Zn(II)、Cd(II)与7-((2-氨基乙基)氨基)-5-溴-6-羟基-1-甲基喹啉-1-ium-3-磺酸盐配合物的抗菌活性

Publication Information	Publisher: Scholars Research Library，Publishing cycle: ，Journal Type: journal，Open Access Journals: No
Basic data	Year of publication: 2010，Proportion of original research papers: ，Self Citation Rate:， Gold OA Rate:

Der Pharma Chemica

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Quantitative Structure-Activity Relationship and Molecular Modeling Studies on a series of constrained (L-)-S-adenosyl-L-homocysteine (SAH) analogues acting as DNA methyltransferase inhibitors.

Synthesis, characterization and antibacterial activity of Schiff base of Cu (II), Ni (II) and Co (II) complexes

GC.MS Analysis and Immuo Modulatory Activities of Punica granatum (Cortex) and Zingiber officinales (rhizome)

RP-HPLC Method Development and Validation for Pioglitazone in Bulk and Marketed Formulation

Synthesis, Structural Characterization, Antimicrobial Activity of Complexes of Co(II), Ni(II), Cu(II), Zn(II), Cd(II) With 7-((2-Aminoethyl)Amino)-5-Bromo-6-Hydroxy-1-Methylquinolin-1- Ium-3-Sulfonate

Quantitative Structure-Activity Relationship and Molecular Modeling Studies on a series of constrained (L-)-S-adenosyl-L-homocysteine (SAH) analogues acting as DNA methyltransferase inhibitors.

Synthesis, characterization and antibacterial activity of Schiff base of Cu (II), Ni (II) and Co (II) complexes

GC.MS Analysis and Immuo Modulatory Activities of Punica granatum (Cortex) and Zingiber officinales (rhizome)

RP-HPLC Method Development and Validation for Pioglitazone in Bulk and Marketed Formulation

Synthesis, Structural Characterization, Antimicrobial Activity of Complexes of Co(II), Ni(II), Cu(II), Zn(II), Cd(II) With 7-((2-Aminoethyl)Amino)-5-Bromo-6-Hydroxy-1-Methylquinolin-1- Ium-3-Sulfonate