Design, Synthesis and Antibacterial Evaluation of some new 3,5-Diphenylcyclohex-2-en-1-one Derivatives

The moiety of cyclohexene has been showed highly antibacterial activity. New compounds were synthesized from diphenylcyclohexenone via reaction with a variety of reagents to afford branched chain of 1,3-diphenylcyclohexene or fused heterocyclic systems including pyrazole, chromen and pyrrole derivatives. Cyclic ketoketene s,s-acetal can be prepared by reaction with CS2/MeI under PTC conditions which in turn used as starting material for the synthesis of pyrazolyl and benzothiszolyl derivatives. Most of new synthesized compounds were characterized by using spectral data and were screened for their antibacterial activity

Synthesis of New Potential Chemotherapeutic Agents Incorporating Naproxen Sub-Structure

A Series Of Potential Biologically Active Compounds Have Been Synthesized Through The Derivatization of Carboxyl Group In Naproxen Core Structure Involving The Conversion The Naproxen To Its Methyl Ester Then To TheAcid Hydrazide. The Acid Hydrazide Of Naproxen Was Incorporated With Hydrazones, Diamide Linkage, Oxadiazole, Pyrazolone, Triazole, Quinazoline And Indole Containing Motifs. The Targeted Compounds Have Been Achieved In A Very Good Yield Under Conventional Heat And Irradiation Conditions. All Compounds Have Been Characterized By Ir, 1h-Nmr, 13c-Nmr And Mass Spectra.Keywords: Naproxen; Anti-Inflammatory; Nsaid's

Synthesis of New Potential Chemotherapeutic Agents Incorporating Naproxen Sub-Structure

A Series of Potential Biologically Active Compounds Have Been Synthesized Through the Derivatization of Carboxyl Group in Naproxen Core Structure Involving the Conversion the Naproxen to its Methyl Ester then to the Acid Hydrazide. The Acid Hydrazide of Naproxen was incorporated with Hydrazones, Diamide Linkage, Oxadiazole, Pyrazolone, Triazole, Quinazoline and Indole Containing Motifs. The Targeted Compounds have been achieved in a very good yield under Conventional Heat and Irradiation Conditions. All Compounds have been characterized by Ir, 1h-Nmr, 13c-Nmr and Mass Spectra

Eco-Friendly Synthesis, Biological Evaluation, and In Silico Molecular Docking Approach of Some New Quinoline Derivatives as Potential Antioxidant and Antibacterial Agents

A new series of quinoline derivatives 5–12 were efficiently synthesized via one-pot multicomponent reaction (MCR) of resorcinol, aromatic aldehydes, β-ketoesters, and aliphatic/aromatic amines under solvent-free conditions. All products were obtained in excellent yields, pure at low-cost processing, and short time. The structures of all compounds were characterized by means of spectral and elemental analyses. In addition, all the synthesized compounds 5–12 were in vitro screened for their antioxidant and antibacterial activity. Moreover, in silico molecular docking studies of the new quinoline derivatives with the target enzymes, human NAD (P)H dehydrogenase (quinone 1) and DNA gyrase, were achieved to endorse their binding affinities and to understand ligand–enzyme possible intermolecular interactions. Compound 9 displayed promising antioxidant and antibacterial activity, as well as it was found to have the highest negative binding energy of -9.1 and -9.3 kcal/mol for human NAD (P)H dehydrogenase (quinone 1) and DNA gyrase, respectively. Further, it complied with the Lipinski’s rule of five, Veber, and Ghose. Therefore, the quinoline analogue 9 could be promising chemical scaffold for the development of future drug candidates as antioxidant and antibacterial agents

A Simple Synthesis of Some New Thienopyridine and Thienopyrimidine Derivatives

A number of pyridothienopyridine (2, 3), pyridothienopyrimidine (6, 10), pyridothienotriazine (13), pyrimidothienopyrimidine (15, 16, 17a,b) and thienoimidazo-triazines (18) were obtained via interaction of 3-amino-5-phenylamino-2,4-dicarbonitrile (1) with different reagents

A model for calculating bottom-hole pressure from simple surface data in pumped wells

© 2020, The Author(s). Bottom-hole flowing pressure and pump intake pressure (PIP) are important parameters to optimize the performance of oil wells. In recent years, downhole sensors are becoming widely used in electrical submersible pump systems to measure these pressures. However, it is still rare to use downhole sensors in sucker rod and progressive cavity pumped wells. In this study, two correlations were developed to calculate bottom-hole flowing pressure and PIP from readily available field data. The two correlations do not require measurements of buildup tests, but they rely on measuring the dynamic fluid level and estimating fluid gradient correction factor using either (1) the tubing gas flow rate or (2) the annular gas flow rate. Then, the PIP is calculated by the summation of either (1) the tubing pressure plus the tubing gaseous liquid column pressure or (2) the casing pressure, annular gas column pressure and the annular gaseous liquid column pressure. The correlations were developed using 419 field data points (389 points for training and 30 for testing) of wide range for each input parameter. Using the training data, the mean absolute percentage deviation (MAPD) between the calculated and measured PIPs is 25% and 20% for the first and second correlations, respectively. However, the testing data showed MAPD of 33% and 12% for the first and second correlations, respectively. The accuracy of these correlations is significantly higher than that of the previously available methods, and the correlations require simpler input. Such study is an original contribution to calculate the PIP with improved accuracy and without downhole pressures sensors

Synthesis and Reactions of Five-Membered Heterocycles Using Phase Transfer Catalyst (PTC) Techniques

Phase transfer catalysts (PTCs) have been widely used for the synthesis of organic compounds particularly in both liquid-liquid and solid-liquid heterogeneous reaction mixtures. They are known to accelerate reaction rates by facilitating formation of interphase transfer of species and making reactions between reagents in two immiscible phases possible. Application of PTC instead of traditional technologies for industrial processes of organic synthesis provides substantial benefits for the environment. On the basis of numerous reports it is evident that phase-transfer catalysis is the most efficient way for generation and reactions of many active intermediates. In this review we report various uses of PTC in syntheses and reactions of five-membered heterocycles compounds and their multifused rings

A-Alkenoyl Ketene S,S- and N,S-Acetals As Starting For Unexpected and Novel Synthesis of N-Heterocycles

A series of N-heterocycles such as diazaspiro-[4.5]decane,  pyrazolo[4,3-d][1,2]-diazepine, imidazo[3,2,1ij][1,8]naphthyridine derivatives or  pyrazolo[3,4-b]pyridin-4-ol were synthesized using a-alkenoyl-, a,a-dialkenoyl ketene-(S,S)-acetals 2a-d, 3a-c or a-dialkenoyl ketene-(N,S)-acetal 12 as starting materials. The biological activity of some new synthesized compounds have been investigated.&nbsp