Naproxen blocks COX enzymes, reducing prostaglandins to relieve pain, fever, and swelling. It is an NSAID used for arthritis, muscle pain, menstrual cramps, and inflammation. Chemical Formula: C₁₄H₁₄O₃ Mechanism of Naproxen: Reversible COX-1/COX-2 inhibitor Uses of Naproxen: Arthritis, ankylosing spondylitis Dysmenorrhea Fever, inflammation Side Effects: GI discomfort Cardiovascular risk (less than some NSAIDs) Fluid … Read more
Ibuprofen blocks COX enzymes, decreasing prostaglandin synthesis to ease pain and swelling. It is an NSAID used for pain, fever, arthritis, and inflammation relief. Chemical Formula: C₁₃H₁₈O₂ Mechanism of Action: Reversible COX-1 and COX-2 inhibitor Reduces prostaglandin synthesis → ↓ pain, fever, inflammation Uses: Mild to moderate pain Fever Dysmenorrhea Osteoarthritis, rheumatoid arthritis Side Effects … Read more
Ketorolac blocks COX enzymes, reducing prostaglandins to provide strong analgesic and anti-inflammatory effects. It is a potent NSAID for short-term management of moderate to severe pain. Chemical Formula: C₁₅H₁₃NO₃ Mechanism of Action: Potent non-selective COX inhibitor Primarily analgesic, weak anti-inflammatory Uses of Ketorolac: Moderate to severe acute pain (short-term, post-op) Alternative to opioids Side Effects … Read more
Diclofenac inhibits COX enzymes, reducing prostaglandin synthesis for strong anti-inflammatory action. It is widely used to treat pain, osteoarthritis, rheumatoid arthritis, and inflammation. Chemical Formula: C₁₄H₁₁Cl₂NO₂ Mechanism of Action: Potent COX-2 > COX-1 inhibitor Inhibits PG synthesis and may inhibit LOX and lipoxygenase enzymes (minor) Uses of Diclofenac: OA, RA, ankylosing spondylitis Post-op pain, dysmenorrhea … Read more
Oxazole is a five-membered aromatic heterocyclic compound containing one oxygen and one nitrogen atom, important in pharmaceuticals. Chemical Formula of Oxazole: C₃H₃NO Physical Properties: Property Value Appearance Colorless liquid Boiling Point ~69–70 °C Melting Point ~-2 °C Solubility Soluble in organic solvents Basicity Weakly basic Medicinal Uses of Oxazole: Used as a bioisostere of oxadiazoles … Read more
Reactions of Imidazole include electrophilic substitution at C-4/C-5 and nucleophilic substitution at C-2. Reactions of Imidazole Tautomerism: Prototropic tautomerism: 1H-imidazole ⇌ 3H-imidazole In practice, 1H-tautomer is more stable and dominates. Electrophilic Substitution Reactions (EAS): EAS occurs readily at position-4 or 5 due to high electron density. Nitration: Milder conditions than for benzene. Forms 4- or … Read more
Synthesis of Imidazole includes Debus synthesis and Radiszewski method using glyoxal, aldehyde, and ammonia. Synthesis of Imidazole Debus–Radziszewski Synthesis (most commonly used) Reactants: Aldehyde (e.g., formaldehyde) 1,2-dicarbonyl compound (e.g., glyoxal) Ammonia (or primary amines) Reaction: Glyoxal + NH₃ + CH₂O → Imidazole + H₂O Mechanism: Schiff base formation Cyclization via nucleophilic attack Aromatization by dehydration … Read more
Imidazole is a five-membered aromatic heterocycle with two non-adjacent nitrogen atoms, widely used in drugs. Chemical Formula of Imidazole: C₃H₄N₂ Physical Properties of Imidazole: Property Value Appearance White crystalline solid Melting Point ~90–91 °C Boiling Point ~257 °C Solubility Very soluble in water and polar solvents Basicity More basic than pyrazole Medicinal Uses: Present in … Read more
Reactions of Pyrazole mainly include electrophilic substitution at the 4-position and oxidation or reduction pathways. Reactions of Pyrazole Tautomerism: Pyrazole exhibits prototropic tautomerism between N-1 and N-2. 1H-pyrazole ⇌ 2H-pyrazole This affects reactivity at the nitrogen atoms and the electron density distribution on the ring. Electrophilic Substitution Reactions (EAS): Due to the electron-rich ring, EAS … Read more
Synthesis of Pyrazole involves methods like Knorr synthesis using 1,3-dicarbonyl compounds and hydrazines. Condensation of 1,3-Dicarbonyl Compounds with Hydrazine (most common method) Reactants: 1,3-diketones (e.g., acetylacetone) Hydrazine (NH₂NH₂) or substituted hydrazines Reaction: CH₃COCH₂COCH₃ + NH₂NH₂ → 3,5-Dimethylpyrazole + H₂O Mechanism: Formation of hydrazone at one carbonyl Intramolecular cyclization Elimination of water → Pyrazole ring Advantages: … Read more