Derpharmachemica

The city of Salé produces about 24 millions m3 /year of wastewater. The majority of this water is discharged directly into the Atlantic coast and Bouregreg estuary without any treatment. To preserve the quality of the receiving waters. treating wastewater and reusing it in agricultureproves very interesting. The objective of this study is thus to investigate the treatment and recycling of wastewater in agriculture. We are particularly interested in studying the growth of the stem and the average number of leaves in order to prove the positive effects of reusing treated wastewater in agriculture as compared to untreated wastewater. To achieve this objective. we have investigated the irrigation of the broad bean by three types of water: Untreated wastewater (UW). Well water (WW) and biologically treated wastewater (TW).

Series of new heterocyclic compounds, Theinopyridines, Pyrazolopyridines and pyrazolopyrimidines derivatives were obtained by the reaction of sodium salt of 1-(4,5-diphenyl-1H-pyrrol-3-yl)ethanone with aminopyrazole derivatives, cyanothioacetaamide and cyanoacidhydrazide. Theobtained compounds were confirmed by spectroscopic analysis such as Infrared Radiation (IR) and Proton Nuclear Magnetic Resonance (1HNMR) and mass spectra. The newly synthesized compounds screened for antimicrobial activity against Gram-positive, Gram-negative bacteria and fungi. Pyrazolopyridines and Pyrazolopyrimidines showed anti-microbial, anti-bacterial and anti-fungal activities.

UV Spectrophotometric methodhas beendeveloped for estimation of lamivudine in bulk and tablet dosage form by using water as solvent. Method developed is Area Under Curve (AUC) method. For analysis of lamivudine by AUC method the wavelength range selected was 265nm to 275 nm because the linearity was obtained within this area with good reproducibility of results . Lamivudine shows absorbance maxima (λmax) at 271 nm scanned in UV range of 400 nm to 200 nm. Lamivudine obeys Beer’s law in the concentration range of 10-60 µg/ml.

The study is carried out to test the catalytic efficiency of Cu-ZSM-5 zeolite catalyst on the reaction of Aza Michael under solvent-free conditions, at room temperature this reaction is most exploited in organic chemistry, b-amino -esters, ketones, nitriles are useful for the preparation of several natural bioactive products, antibiotics, and chiral auxiliaries, through the use of the porous material catalyst (zeolite Cu-ZSM-5), and the reaction of Aza Michael addition a series of amines on α, β-unsaturated methyl acrylate, we have synthesized new cc or c-heteroatomproducts, these compounds is an attractive area of researchers in synthetic organic chemistry, and we have developed new synthesismethodologies for the preparation of these products. The reaction was carried out with favorable conditions: ambient temperature, and without solvent, that the products, which are synthesized, gave us a high yield, and excellent chemo selectivity.

Reactions of 2-chloro-N-(3-cyano-4,5,6,7-tetrahydro-1-benzothiophen-2-yl)acetamide with substituted 5-phenyl-1,3,4-oxadiazole-2 thiol gave N- (3-cyano-4,5,6,7-tetrahydro-1-benzothiophen-2-yl)-2-aryl-[(5-phenyl-1,3,4-oxadiazol-2-yl)sulfanyl]acetamide were synthesized and assessed for their efficacy as antitubercular agents against tuberculosis H37Rv. The structural assignments of the new products were done on the basis ofInfrared radiation (IR), Proton nuclear magnetic resonance (1H-NMR) and elemental analysis.

Knocking out type2 diabetes by new insulin independent renal glucose transporters as targets, reducing the side effects related to high rise in glucose levels is a more efficient way to manage diabetes. Sodium-glucose co-transporter 2 (SGLT2) inhibitors block reabsorptionof glucose back into the blood and stimulate secretion in urine in a way controlling blood glucose levels. Areas discussed: We emphasize in this review an overview of type 2 diabetes. New insulin independent targets, SGLT family inhibitors and their mechanism of action are briefly discussed. Molecular modeling studies carried out for new analogues of SGLT2 were indicated and also about current marketed SGLT drugs their safety issues are briefly outlined. Conclusion: SGLT2 inhibitors are very promising drugs for near future, where insulin sensitization is a problem. A combination of drugs related to insulin dependent pathway and also independent pathway like SGLT2/SGLT1 drugs will be more effective in glycemic control...

Antioxidant property and interaction with Deoxyribonucleic Acid (DNA) of the following four quinones: Mansanone-D, Mansanone-H, Sissoidenone and 4-methoxy dalbergione, were investigated at pH=7.4 using cyclic voltammetry technique. The parameters like bindingconstant, binding site size and binding free energy value were also determined from voltammetric data. On comparison of binding constant and binding site size among all Quinones, Mansanone-H reveals strong binding capacity (1.04 x 109 ) with DNA than others. The negative sign of binding constants (ΔG) indicate the spontaneity of binding of Quinones with DNA. The electrochemical behavior of DPPH radical was investigated in Dimethyl Sulfoxide (DMSO) and used this radical to determine antioxidant activity of Quinones by cyclic voltammetry method. The scavenging effect of the radical on Quinone was confirmed by the decrease in peak currents with increase in the concentration of Quinones. The binding constant and Gibbs free energy val...

The quality of pharmaceuticals is always a matter of global concern because counterfeit medications with substandard quality are increasingly detected worldwide, the reason for which can be that these drugs may not have been subjected to strict approval processes by relevant regulatory agencies. So, in order to ensure the requisite quality, it should be mandatory for the drug manufacturers to analyze their products during each level of manufacturing and processing. Moreover some multinational brands are so costly and thus unaffordable to common people and comparatively local brands of same generic are available at much lower prices. But to select one product from several generic drugproducts of same active ingredients is the cause for concern for the common people. So, every effort should be done to make these drugs chemically and pharmaceutically equivalent in every aspect as the branded drugs which can only be possible if proper quality control guidelines are being followed during ...

Cytotoxic evaluation using Peripheral Blood Mononuclear Cells (PBMCs) was achieved by a novel series of (E)-1-(4-chlorobenzyl)-N'- benzylidene-5-bromo-1H-indole-2-carbohydrazide 6(a-j). Among the series, the compounds 6b, 6c, 6f, 6h and 6j were found to be active compared to other analogues. These compounds showed excellent dose dependent cytotoxicity on PBMCs, whereas, 6j showed reduction inactivity. The in silico pharmacokinetic parameter study such as ADME and toxicity of the synthesized compounds were evaluated using ACD/Ilab and ADMETSAR@MDDM methods. The synthesized molecules 6a, 6b, 6c, 6f, and 6g are in acceptable range and less toxic in nature.

The study was set out to investigate the possibility of using blood groups as predictive indices for diseases associated with lipid metabolism. Methods: Lipid profiles were examined in 100 apparently healthy male (40) and female (60) subjects of different ABO blood groups aged between 18-30 years from Imo State University. Of these, 20 were blood group A, 30 were B blood type, 4 were AB blood type, and 46 were blood group O. Lipid profile parameters were determined according to enzymatic assay using a commercial kit from Randox Laboratories, United Kingdom and calculation using Friedewald’s equation. Blood group was determined by monoclonal ABO blood grouping reagent.

The chemical composition of essential oil, isolated from Thymelaea microphylla by hydrodistillation, was analysed by GC and GC/MS. A total 30 compounds representing 99.91% of the oil were identified in Dreaat population. The essential oil of T. microphylla is Characterized by a high rate of Tridecanal (31.24%), Nonanal (11.43%), Pentadecen 2-one (6Z) (7.93%) and the Citronellol (6.80%). Antioxidant capacity was determined using the method of 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical. The extracts essential oil showed a good antioxidant activity. Disc diffusion method was used to evaluate the antibacterial activity on five different strains. The oil showed a significant effect against Gram-negative and Gram-positive bacteria. 

Fluoroquinolones are an essential class of antibacterial, and widely used in clinical application. This article concerns the spectroscopic and theoretical investigation of Ofloxacin. The experiment results were performed with Infra-Red (IR) spectroscopy, Ultra-Violet (UV) visiblespectroscopy and Nuclear Magnetic Resonance (NMR) spectroscopy. Theoretical calculations were performed with Gaussian 09W and Gauss View 5 software Packages. The structure, conformational stability, geometry optimization and vibrational frequencies of Ofloxacin (OFL) have been investigated using density functional theory DFT-B3LYP methods with the 6-31++G(d,p) basis set. The Mulliken atomic charges of the title molecule were also performed using the DFT method. The presented spectroscopic investigation on OFL shows the good agreement between observed spectra and theoretical predictions of the drug. In IR spectra, the difference in intensities is seen may be due the intramolecular Hbonding in experimental stud...

A big problem in intensive care units (ICU) is caused by antibiotic resistant bacterial nosocomial infections. Acinetobacter are among the mostchallenging bacterial pathogens and to help in formulating antibiotic policy for better management of patients with bacterial diseases. The data showed that 93.3% of bacterial isolates were resistant to ampicillin while 80% and 66.7% of bacterial isolates were resistant to ceftazidime and sulphamethoxazole/trimethoprim, respectively. Identification of multi-resistant isolates according to morphological and biochemical characteristics, Acinetobacter baumannii found to be the most frequent pathogen representing 66.7% followed by Acinetobacter calcoaceticus and Acinetobacter lwoffii with 20% and 13.3% percentages, respectively. The main objective of this study was studying the susceptibility of multi-drug resistant isolates to different ten essential oils derived from different parts of ten medicinal plant species traditionally used in Egyptian f...

An ethnobotanical survey of plants has been carried out in Targuist area (North of Morocco), it aimed to collect information on the medical and cosmetic uses of plants. By using 3500 questionnaires, ethnobotanical survey was conducted during two periods (2016 and 2017), withtraditional herbalists and users of these plants. The analysis of results identified 90 plants distributed in 43 families with a dominance of the lamiaceae (15.28%). The survey revealed that leaves were the most used part of the plants (43%) and the majority preparation used was a decoction (36.6%). Digestive diseases represent the most cited diseases (31%).

Binary complexes of Ca(II), Zn(II) and Mn(II) with L-proline was investigated pH-metrically in 1,2-propanediol-water mixtures by maintainingan ionic strength of 0.16 mol.L-1at 303.0 K. The best-fit chemical models for present study are ML+ , MLH2+ and ML2H + for Ca(II), Zn(II) and Mn(II) ions are established from modelling studies using computer program MINIQUAD75. Some errors influence the magnitudes of stability constants and its order is alkali > acid > ligand > metal. The graphical representation of log β against 1/D of the medium shows that dominance of electrostatic interactions. Distribution diagrams of the various species of the binary complexes in relation to pH at different variations (0.0-60.0% v/v) of propylene glycol-water mixtures were presented. 

The optimized molecular structures, vibrational frequencies, corresponding vibrational assignments and atomic NBO charges of a biologicallyimportant molecule namely, pyrazino[2,3-d] pyrimidine have been carried out through density functional theory (B3LYP) level employingseveral basis sets. The results of vibrational frequencies and optimized geometric parameters were found in good agreement with the experimental data, which indicate that is planar and more stable. Moreover, the possible electrophilic and nucleophilic reactive sites were predicted by local reactivity descriptors and MEP map to describe the presence of intermolecular bonding and the hydrogen bonding interaction. In addition, the design format of our molecule present an opportunity to reveal the electron density profile by using the FMOs analysis and other electronic structure parameters such as ionization energy (I), Electron affinity (A), Global hardness (η), Chemical potential (μ), Electrophilicity index(ω),

A highly efficient synthesis of Baylis-Hilman derivatives has been achieved via a vinylalumination of isatins at room temperature. The resultingoxindole scaffolds were obtained in moderate to high yields. The main advantages of this manuscript are short reaction time, operationally simple, purification of products by non-chromatographic method

The accumulating pharmacological importance of drug resistant pathogens has lent auxiliary urgency to new anti-tubercular compound development. In this regard, a novel series of pyrrolo [1,2-a]pyrazine incorporated indolizine derivatives have been synthesized, characterizedby using spectral data and screened for in vitro antimycobacterial activity. The anti-tubercular activity of the synthesized compounds (7a-p) was determined by microplate alamar blue assay and the outcomes were screened against Mycobacterium tuberculosis H37Rv strain. Compounds 7a-p exhibited good to potent anti-tubercular activity when compared with the standard first line anti-tuberculosis drugs (ciprofloxacin, pyrazinamide and streptomycin). Some of the tested compounds exhibited highest inhibitory activity at 1.6 µg/ml minimal inhibition concentration.