Design, Synthesis, Characterization, and Computational Studies on Benzamide Substituted Mannich Bases as Novel, Potential Antibacterial Agents

A series of benzamide substituted Mannich bases (1–7) were synthesized. The synthesized derivatives were authenticated by TLC, UV-Visible, FTIR, NMR, and mass spectroscopic techniques and further screened for in vitro antibacterial activity by test tube dilution method using amoxicillin and cefixime as standard drugs. The compounds 5, 6, and 7 were found to be the most active antibacterial agents among all the synthesized compounds. The physicochemical similarity of the compounds with standard drugs was assessed by calculating various physicochemical properties using software programs. The percent similarity of synthesized compounds was found to be good and compound 1 was found to have higher percentage of similarity. The compounds were subjected to QSAR by multilinear regression using Analyze it version 3.0 software, and four statistically sound models were developed with R2 (0.963–0.997), Radj2 (0.529–0.982), and Q2 (0.998–0.999) with good F (2.35–65.56) values

Extraction, characterization and evaluation of Eruca sativa against streptozotocin-induced diabetic nephropathy in rat

The present study was aimed to evaluate petroleum ether and hydroalcohol extracts of Eruca sativa seeds in the treatment of diabetic nephropathy in the rat model. GC-MS analysis of petroleum ether extract revealed the presence of fatty acids and erucic acid. Quercetin and kaempferol were isolated from the hydroalcohol extract. Diabetes was induced in rat by streptozotocin (65 mg/kg i.p.) 15 min after nicotinamide (230 mg/kg, i.p.) administration. Both the extracts at different doses produced a significant attenuation in the elevated serum glucose level. Elevated renal parameters, lipid and anti-oxidant enzyme levels were restored in a dose-dependant manner. Moreover, both extracts produced significant reduction in the formation of advanced glycation end products in the kidney. These findings suggest that E. sativa might inhibit the progression of diabetic nephropathy and could be a therapeutic agent for the management of diabetic nephropathy. Video Clip of Methodology: Extraction of compounds from seeds: 3 min 45 sec   Full Screen   Alternat

Schiff Bases: A Versatile Pharmacophore

Schiff bases are condensation products of primary amines with carbonyl compounds gaining importance day by day in present scenario. Schiff bases are the compounds carrying imine or azomethine (–C=N–) functional group and are found to be a versatile pharmacophore for design and development of various bioactive lead compounds. Schiff bases exhibit useful biological activities such anti-inflammatory, analgesic, antimicrobial, anticonvulsant, antitubercular, anticancer, antioxidant, anthelmintic, antiglycation, and antidepressant activities. Schiff bases are also used as catalysts, pigments and dyes, intermediates in organic synthesis, polymer stabilizers, and corrosion inhibitors. The present review summarizes information on the diverse biological activities and also highlights the recently synthesized numerous Schiff bases as potential bioactive core.</jats:p

Mannich Bases: An Important Pharmacophore in Present Scenario

Mannich bases are the end products of Mannich reaction and are known as beta-amino ketone carrying compounds. Mannich reaction is a carbon-carbon bond forming nucleophilic addition reaction and is a key step in synthesis of a wide variety of natural products, pharmaceuticals, and so forth. Mannich reaction is important for the construction of nitrogen containing compounds. There is a number of aminoalkyl chain bearing Mannich bases like fluoxetine, atropine, ethacrynic acid, trihexyphenidyl, and so forth with high curative value. The literature studies enlighten the fact that Mannich bases are very reactive and recognized to possess potent diverse activities like anti-inflammatory, anticancer, antifilarial, antibacterial, antifungal, anticonvulsant, anthelmintic, antitubercular, analgesic, anti-HIV, antimalarial, antipsychotic, antiviral activities and so forth. The biological activity of Mannich bases is mainly attributed to , -unsaturated ketone which can be generated by deamination of hydrogen atom of the amine group

1,3,4-Oxadiazole Derivatives: Synthesis, Characterization, Antimicrobial Potential, and Computational Studies

We report the synthesis and biological assessment of 1,3,4-oxadiazole substituted 24 derivatives as novel, potential antibacterial agents. The structures of the newly synthesized derivatives were established by the combined practice of UV, IR,1H NMR,13C NMR, and mass spectrometry. Further these synthesized derivatives were subjected to antibacterial activity against all the selected microbial strains in comparison with amoxicillin and cefixime. The antibacterial activity of synthesized derivatives was correlated with their physicochemical and structural properties by QSAR analysis using computer assisted multiple regression analysis and four sound predictive models were generated with goodR2,Radj2, and Fischer statistic. The derivatives with potent antibacterial activity were subjected to molecular docking studies to investigate the interactions between the active derivatives and amino acid residues existing in the active site of peptide deformylase to assess their antibacterial potential as peptide deformylase inhibitor.</jats:p

In vitro antioxidant properties and inhibitory effect of extracts and fractions of Plectranthus glandulosus leaves on copper sulfate (CuSO4)-induced oxidation in human low-density lipoprotein

Oxidation of LDL has been suggested to be an initial step in the development of atherosclerosis. This research work deals with the evaluation of antioxidant potential of Plectranthus glandulosus leaves extracts and fractions as well as its protective effects against human LDL oxidation. A preliminary quantitative phytochemical screening was carried out. Antioxidant potential was evaluated employing in vitro hydrogen peroxide, nitric oxide scavenging assays and TAOC test. The human LDL oxidation induced by CuSO4 inhibition test was also performed. Plectranthus glandulosus leaves exhibited the presence of 18.3% of saponines, 25.6% of terpenoids and 36.2% of flavonoids. EAF exhibited highest hydrogen peroxide and nitric oxide scavenger activity (IC50 13.63µg/ml and 24.59 µg/ml respectively). Ascorbic acid exhibited an IC50 value of 15.39µg/ml in hydrogen peroxide assay and 22.96 µg/ml in nitric oxide scavenging activity. EAF exhibited a higher TAOC (optical density 0.186±0.00) than that of ascorbic acid (0.162±0.001) at the concentration of 25µg/ml while at 200µg/ml N-BUTF exhibited a higher optical density (1.261±0.001) than that of ascorbic acid (1.065±0.001). EAF lengthened the lag time of the CD formation up to 150mins at the concentration 1mg/ml. TBARS formation inhibition at the concentration 0.5mg/ml, were no significant different between n-butanol (68.55%) ethyl acetate fraction (68.21%) and quercetin 67.69%). Plectranthus glandulosus is a promising prospect as an anti-atherosclerotic agent and needs a detailed study to establish the same. Key words: Plecthrantus glandulosus; oxidation; LDL; atherosclerosis, antioxidant

An allied approach for in vitro modulation of aldose reductase, sorbitol accumulation and advanced glycation end products by flavonoid rich extract of Coriandrum sativum L. seeds

Traditional herbal medicines are attaining more popularity and are being widely practiced. Coriandrum sativum L. is one of the oldest herbal medicinal plants valued for its nutritional and medicinal properties. Present investigation was focussed on evaluation of attenuating potential of flavonoid rich extract of C. sativum (FCS) seeds against pathogenic markers of diabetic complications i.e. advanced glycation end products (AGEs), sorbitol and aldose reductase (ALR); by using in-vitro methods. Gas chromatography–mass spectrometry (GC–MS) and Infrared spectroscopy of FCS revealed the presence of different flavonoids.Results demonstrated that FCS has produced 79.80% inhibition of AGEs formation. Additionally, FCS was effective against sorbitol accumulation and ALR inhibition with IC50 values of 221 μg/ml and 6.08 μg/ml respectively. Molecular docking was conducted against three binding site for ALR, RAGEs and sorbitol dehydrogenase to explore their binding interactions with identified flavonoids. The constituents F2, F4 and F6 have shown good binding interactions with all the receptors. The visualisation of the docked complexes revealed the occurrence of hydrophobic forces and hydrogen bonding in receptor and docked constituents.The results were in support with experimental inhibitory activities of FCS against these biomarkers and provide a considerable basis for the identification and development of new inhibitors. Keywords: C. sativum, FCS, AGEs, Sorbitol, AL

Chemistry behind Serum Albumin: A Review

This review informs about the chemical composition of plasma proteins majorly albumin and globulin. Blood proteins, also called plasma proteins, are found in blood plasma. While, serum proteins are present in the human body in very high quantities for other proteins. Hundreds of proteins are dissolved in the plasma but only two major protein groups are present i.e. Albumin and Globulin. Albumin is a very important component (55% of blood proteins) and it is made by the liver. There is an immediate correlation between albumin turnover and body size. Globulin is formed from different proteins called alpha, beta, and gamma types (38% of blood proteins) but a number of the globulins are mainly made by the liver, while others are made by the immune system. The average serum protein level existing in the human body is 6 to 8g/dl but 3.5 to 5.0g/dl is making up only albumin and globulin makes up 2/3gl. Different aspects of the proteins are discussed below

Coriandrum sativum seeds extract mitigate progression of diabetic nephropathy in experimental rats via AGEs inhibition.

Inthe present study, we have demonstrated the phytochemical composition of petroleum ether extract of C. sativum (CPE) seeds by using chromatographic, spectroscopic as well spectrometric analysis. CPE was evaluated for its possible role in mitigation of diabetic nephropathy (DN) in Streptozotocin (STZ)-nicotinamide (NAD) induced type 2 diabetes model. Administration of CPE at doses of 100, 200, and 400 mg/kg for 45 days has produced significant attenuation of elevated biochemical parameters including serum glucose, lipid and creatinine levels. CPE has also reserved albuminuria and elevated creatinine clearance in treated diabetic rats. Advanced glycation end products (AGEs) formation in kidneyswas also considerably reduced along with noteworthy increase in level of superoxide dismutase (SOD), glutathione (GSH), and decrease in lipid peroxidation in terms of thiobarbituric acid reactive species (TBARS). Molecular docking studies were also employed to reveal out the possible mechanism. In conclusion, using STZ-NAD model, we have successfully predicted that by assets of bioactive constituents CPE might inhibit the progression of DN. C. sativum may act as potential adjuvant for antidiabetic therapy and needs to be investigated further