Non-Steroidal Anti-inflammatory Drugs (NSAIDs): Synthesis of Ibuprofen, Naproxen and Nabumetone

This review paper covers the major synthetic approaches attempted towards the synthesis of some Non-Steroidal Anti-Inflammatory Drugs (Naproxen, Ibuprofen and Nabumetone)

Design, Synthesis and Acute Anti-Inflammatory Evaluation of New Non-Steroidal Anti-Inflammatory Agents Having 4-Thiazolidinone Pharmacophore

Naproxen suffers from general side effects of NSAIDs, owing to the presence of free carboxylic group. The study was aimed to retard the adverse effects of gastrointestinal origin. New series of 4-thiozolidinones derivatives of naproxen were synthesized Va-f. The structures of synthesized compounds have been established on the basis of their spectral FT-IR and 1H NMR data. In vivo acute anti-inflammatory effects of the synthesized compounds were evaluated in rats using egg-white induced edema model of inflammation. The tested compounds and the reference drug produced significant reduction of paw edema with respect to the effect of propylene glycol 50%v/v (control group). Compounds Va-e exhibited potent anti-inflammatory effect than naproxen (50mg/kg, i.p.) at 180-240 min., while compound Vf exhibited lower anti-inflammatory effect. Keywords: Naproxen, 4-Thiazolidinone, Anti-inflammatory activity

The study of antibacterial activity of Hibiscus sabdariffa flowers extracts

The aqueous and methanol extracts obtain from flowers Hibiscus sabdariffa have been investigated for their antibacterial activity. Antibacterial activity was determined by using agar well diffusion method at concentrations of (500, 250, 125, 62.5) mg/ml, against Staphylococcus aureus, Escherichia coli, Salmonella typhi, Klebsiella pneumonia, Enterococcus spp., Acinetobacter spp., Pseudomonas aeruginosa, Shigella dysenteriae, Proteus vulgaris. Hibiscus sabdariffa extracts demonstrated antibacterial effects of methanol and aqueous extracts against bacteria used in this study at different levels. Only E. coli was not susceptible to aqueous extract at all concentrations were used

Synthesis, anti-inflammatory, molecular docking and ADME studies of new derivatives of ketoprofen as cyclooxygenases inhibitor

The synthesis of new selective COX-2 enzyme is an approach for obtaining potent, anti-inflammatory drugs that have fewer side effects. Ketoprofen has a very low selectivity toward COX-2 enzyme and has a serious GIT side effects because it induces gastric ulcer. A new series of 4-thiazolidinones bearing ketoprofen moiety was designed, synthesized, and then evaluated as a new inhibitor of cyclooxygenase-2 (COX-2). Characterization and identification of the synthesized compounds were established by determination of 1H-NMR spectra,13C-NMR spectra, FT-IR spectroscopy, and physical properties. These newly synthesized compounds have been evaluated in vivo for their anti-inflammatory efficiency and in silico selectivity toward COX-2 throughout molecular docking by using GOLD.suite.v.5.6.2. All the tested. compounds via molecular. docking showed significant. activities when compared. With ketoprofen and diclofenac as references drugs, the results were consistent with the study of in in vivo acute. anti-inflammatory activity. Also, ADME studies had been accomplished in order to predict the absorption sites, bioavailability, topological polar surface Area (TPSA), and also drug-likeness.  The ADME results reported that. All the synthesized. compounds can be absorbed by the GIT

Molecular modelling, Synthesis and Antiproliferative Evaluation of New Phenyldiazenyl)-Pyrazol Schiff Base Derivatives

Lung cancer is the most prevalent worldwide. In addition, it is also the most common cause of cancer-related deaths worldwide, with around 1.8 million new cases annually. With a 5-year survival rate of fewer than 20%. Cytotoxic medicines are commonly employed in cancer treatment. Although the medicine improves patients' quality of life, several disadvantages diminish its efficacy. This necessitates developing new effective strategies that target tumors with minimal adverse effects. This research aims to overcome these issues by synthesizing a new series of phenyldiazenyl)-pyrazol schiff base derivatives by utilizing the molecular docking (GOLD) suite program and the pharmacokinetic properties determination by utilizing (Swiss) ADME suite; The most appropriate-fitting compounds were subsequently produced and confirmed using spectrum analysis (FTIR, 1HNMR, and 13 CNMR). MTT in vitro assay were performed to assess of antiproliferative activities against A549 lung cancer cell lines. The antiproliferative study showed that compound 3a had an inhibitory concentration (IC50 of 17.37 µM) on lung cancer cells (A549), which was significantly higher inhibitory activity than Erlotinib (IC50 = 25.06 µM). While compound 3b had an inhibitory activity comparable to the reference drug's, The IC50 values for compounds 3c, 3d, and 3e were 47.48, 45.56, and 33.05 µM, respectivel

Molecular modeling, synthesis, and antiproliferative evaluation of new isoxazole ring linked by Schiff bases and azo bond

Lung cancer is the most common malignancy worldwide, with approximately 1.8 million new cases yearly. Cytotoxic drugs are frequently used in cancer treatment. Even though the medicine enhances patients' quality of life, several drawbacks diminish its efficacy. Drug resistance and many disadvantages associated with chemotherapeutic drug side effects continue to be significant factors limiting the efficiency of cancer treatment. This necessitates developing new effective strategies that target tumors with minimal adverse effects. This research aims to overcome these issues by synthesizing a new series of compounds with an isoxazole ring attached by Schiff bases and azo bonds based on molecular docking with the (Genetic Optimization of Ligand Docking) program and estimating the pharmacokinetic properties with the Swiss ADME. The greatest-fitting compounds were then manufactured and verified by spectral analysis (FT-IR, 1H NMR, and 13C NMR), in vitro MTT assay for assessment of antiproliferative activities against A549 lung cancer cell lines showed that compounds 5a and 5b had an inhibitory concentration half-maximal inhibitory concentration (IC50) (17.34 and 18.32 μM), respectively, which was significantly lower than the inhibitory concentration of erlotinib (IC50 = 25.06 μM)

Synthesis, characterization and antimicrobial study via new heterocyclic derivatives of trimethoprim

<p>New compounds of trimethoprim heterocyclic derivatives were synthesized. These compounds were synthesized through the condensation reaction between trimethoprim with bromoacetic acid to yield compound <b>1</b>. Several Schiff bases <b>2</b>–<b>7</b> have been synthesized by the condensation different aromatic aldehydes with compound <b>1</b>. Compound <b>8</b> were formed from the reaction of sodium nitrite and acetyl acetone in presence of conc. hydrogen chloride to obtain the hydrazono derivative; then, Cyclocondensation of compound <b>8</b> with hydrazine hydrate, phenyl hydrazine and dinitrophenyl hydrazine respectively to yield compounds <b>9</b>–<b>11</b> in ethanol affording the pyrazoline derivatives. This work involves the synthesis of some 1,2,3-Triazoles derived from compound <b>1</b> by the action of sodium azide on the diazonium chloride salt to yield 5-azido-8-(3,4,5-trimethoxybenzyl)imidazo[1,2-c]pyrimidin-3(2H)-one <b>12</b>. Finally, by reaction of 12 with acetyl acetone and ethyacetoacetate; respectively in sodium ethoxide/ethanol as a solvent to form compounds <b>13</b>, <b>14</b>. The structures of the compounds <b>1</b>–<b>14</b> were characterized by elemental analysis, spectral data and antimicrobial evaluation of the some newly synthesized compounds and found that the synthesized compounds are active against tested Gram positive and Gram negative bacteria like <i>Staphylococcus aureus, Bacillus subtilis, Escherichia coli</i> and <i>Proteus.</i> </p