Derpharmachemica

In the present synthesis work, we were synthesized viable bio active nitrogen and oxygen atom containing heterocyclic compounds like pyrazole, pyrazolone, coumarin, azo coumarin, and naphthyl coumarin. A metal catalyst free reaction to afford the targeted compounds (1-7) in goodyields. All three types of coumarins were synthesized in one step ecofriendly approach under solvent free condition. The beauty of this work easily available primary material, gentle conditions, smooth operation and economical cost. The synthesized compound structures were confirmed by advance spectroscopic techniques and elemental analysis. Besides, compounds also evaluated for their in vitro antimicrobial activity

Acinetobacter baumannii is a ubiquitous Gram-negative bacillus bacterium that is frequently found in the nosocomial infections. Regard to the rapid development of resistance against various antimicrobial agents due to the high ability of natural genetic transformation, A. baumannii is resistance to many of the antibiotics. Toxin-antitoxin system is one of the virulence agents in A. baumannii that can be involved in the emergenceof drug resistance. HicB as a toxin system is an ideal target for the design of new classes of antimicrobial agents against A. baumannii. The goals of this work was to model the complete tridimensional structure of the HicB protein using computational methods and to assess structural and functional of it. The consistency of modeled structure was confirmed by different servers to high accuracy for modeling and dynamics simulation. The molecular dynamic simulation and virtual screening results indicate that HicB is a stable protein from A. baumannii. These result...

Phenyl imidazole propionate derivative which shows wide range of biological activities was synthesized. The yield of imidazole ring formation i.e. conversion of 1-isopropyl 3-(2-oxo-2-phenylethyl)2-(4-methoxybenzyl)malonate (1) to tert-butyl 3-(4-methoxyphenyl)-2-(4-phenyl-1Himidazole-2-yl)propanoate (2) was improved from 35% to 87%. Statistical model based screening and optimization DOE study were carried outto derive the most favorable design space and optimal operating condition for the process parameters. The model of optimization study was created using central composite design. Model-validation was performed which showed excellent reproducibility with high degree of precession. Use of ammonium chloride as a catalyst to improve the yield of imidazole ring formation reaction was also explored for the first time

Allergic asthma is a complicated disorder where multiple stimuli activate various signalling pathways resulting in the synthesis of a wide array of inflammatory proteins. Among the diverse transcription factors in the human genome, Nucleus Factor Kappa B (NFκB) and p38 Mitogen Activated Protein (MAP) kinases play a crucial role in the pathophysiology of allergic asthma. Salicylic acid derivatives, 5-Amino Salicylic Acid(5-ASA) and Sodium Salicylate (SS) have been evidenced to inhibit NFκB in vitro model. 5-ASA has demonstrated significant antiasthmatic activity in preclinical murine models. In the present study, 5-ASA and SS were screened in silico against a definite set of proteins, namely Inhibitor of Kappa Beta (IκB), p38 α, β, γ and δ using Glide and Prime modules of Schrodinger suite. The two drug candidates were attributed to the MTT assay in RAW 264.7 mouse monocyte macrophage cells for their in vitro cytotoxicity. From the hits obtained in silico, IκB and p38γ were further e...

A reversed phase high performance liquid chromatography was developed for estimation and determination of two actives pharmaceutical ingredient Udenafil (Zydena) and Dapoxetine (Priligy). In presence of pregabalin as internal standard. The chromatographic conditions wereapplied according to ICH-guidelines using Thermo Hypersil BDS–C18 (250 mm × 4.6 mm, 5.0 µ) the mobile phase containing acetonitrile: 0.2% triethyl amine in pure water (H2O) the adjusted pH was 4.4 using ortho- phosphoric acid (75: 25) with flow rate amount approximately 1 ml/min using UV detection at 246 nm. Limit of detection was established to be 0.015 μg/ml and Limit of Quantification (LOQ) was found to be 0.025 μg/ml for udenafil and the Limit of Detection (LOD) of dapoxetine HCl 0.020 μg/ml. according to ICH-guidelines and statistical treatment of date the date for this method was linear with correlation coefficient R2 > 0.99 which prove that the method is convenient and applicable for the investigation and st...

A series of novel 1,3,5-triazine derivatives bearing various aryl amine, 2-amino pyrazine and 4-hydroxy coumarin moieties as substituents have been synthesized by an easy and conventional method using sequential nucleophilic substitution of chlorine atoms of cyanuric chloride. Thereaction of cyanuric chloride with 4-hydroxy coumarin in acetone using alkaline medium at 0-5°C was afforded compound 3 in good yield. Followed by reaction 3 with 2-amino pyrazine and then various aromatic amines have afforded target compounds 6a-n in good yields. All the newly synthesized compounds were characterized by using spectroscopic analysis and then examined for their ability to inhibit the two Grampositive bacteria (Bacillus subtilis and Staphylococcus aureus) Gram-negative bacteria (Escherichia coli and Pseudomonas aeruginosa) and one fungal species (Aspergillus niger) for biological interest.

The outer rinds or peels of many fruits are not eaten and are thrown as a waste. Similarly in food industry, processing of fruits results in the formation of agro waste in high amounts and is common in the form of peels. This waste has to be managed efficiently as they pose seriousproblems to environment. Till now agro waste is used as livestock feed or as fertilizer but recently strategies have been developed to explore the bioactive components from the peels as well as their therapeutic benefits. Many scientific investigations reported the isolation of constituents with promising antioxidant, antimicrobial, antiproliferative activities from the peels of various fruits.