Piroxicam

Piroxicam

Piroxicam blocks COX enzymes, reducing prostaglandin synthesis to relieve pain and swelling. It is an NSAID for long-term management of arthritis, pain, and inflammation. Chemical Formula: C₁₅H₁₃N₃O₄S Mechanism of Piroxicam: Non-selective COX inhibitor Long half-life (~50 hrs) Uses of Piroxicam: Chronic inflammatory conditions (OA, RA) Once-daily dosing Side Effects: GI irritation/ulceration Photosensitivity Headache Notes: Long-acting … Read more

Phenacetin (Withdrawn)

Phenacetin (Withdrawn)

Phenacetin (Withdrawn) was withdrawn due to nephrotoxicity and carcinogenic risks linked to long use. It was once used as an analgesic and antipyretic for pain and fever relief. Chemical Formula: C₁₀H₁₃NO₂ Mechanism of Phenacetin (Withdrawn) : Central COX inhibition Mild analgesic and antipyretic Uses of Phenacetin (Withdrawn): Formerly used for fever and pain Side Effects: … Read more

Synthesis of Oxazole

Synthesis of Oxazole

Synthesis of Oxazole involves methods like Robinson-Gabriel synthesis, Fischer oxazole synthesis, and cyclization of α-acylaminoketones. Robinson–Gabriel Synthesis (Classical method) Reactants: α-acylaminoketones Reagents: Acidic dehydrating agents (e.g., P₂O₅, POCl₃) Reaction: R–CO–CH₂–NH–CO–R’ → Oxazole (via cyclodehydration) Mechanism: Intramolecular cyclization Dehydration Aromatization Bredereck Synthesis Reactants: α-haloketone + formamide Reaction: CH₃COCH₂Cl + HCONH₂ → 2-methyl-oxazole Good for substituted oxazoles … Read more

Reactions of Oxazole

Reactions of Oxazole

Reactions of Oxazole include electrophilic substitution at the 5-position, nucleophilic substitution at the 2-position, and ring-opening reactions. Electrophilic Aromatic Substitution (EAS) The ring is electron-deficient (due to N and O), so EAS is more difficult than in pyrrole, furan, or imidazole. Most reactive site: C-5, due to resonance stabilization of the intermediate. Examples: Nitration (HNO₃/H₂SO₄) … Read more

Pyridine

Pyridine is a nitrogen-containing heterocyclic compound essential in pharmaceuticals, agrochemicals, and organic synthesis. Chemical Formula of Pyridine: C₅H₅N Physical Properties of Pyridine: Property Value Appearance Colorless liquid Odor Fish-like, unpleasant Boiling Point ~115 °C Melting Point ~-41 °C Solubility Miscible with water and organics Basicity (pKa of conjugate acid) ~5.2 (moderately basic) Medicinal Uses: Pyridine … Read more

Reactions of Thiazole

Reactions of Thiazole

Reactions of Thiazole include electrophilic substitution, metalation, oxidation, and reduction pathways significant in medicinal chemistry. Reactions of Thiazole Electrophilic Aromatic Substitution (EAS) Like oxazole, C-5 is the most reactive site. Easier than oxazole due to lower electronegativity of sulfur. Examples: Bromination: Thiazole + Br₂ → 5-bromothiazole Nitration: HNO₃/H₂SO₄ → 5-nitrothiazole Friedel–Crafts acylation: Rare, can occur … Read more

Synthesis of Thiazole

Synthesis of Thiazole

Synthesis of Thiazole explains key routes like Hantzsch, Gabriel, and cyclization strategies with reagents, mechanisms, and applications. Hantzsch Thiazole Synthesis (Classical and widely used) Reactants: α-haloketone + thioamide Conditions: Reflux in ethanol or basic medium Reaction: CH₃COCH₂Cl + NH₂–CS–NH₂ → Thiazole derivative Mechanism: Nucleophilic attack by thioamide Cyclization Elimination of HCl Gabriel Synthesis Uses α-haloketone … Read more

Thiazole

Thiazole

Thiazole is a sulfur and nitrogen heterocyclic ring important in drug design, vitamins, and medicinal chemistry. Chemical Formula of Thiazole: C₃H₃NS Physical Properties of Thiazole: Property Value Appearance Colorless to pale yellow liquid Boiling Point ~116 °C Melting Point ~-30 °C Solubility Soluble in organic solvents Basicity Weakly basic Medicinal Uses: Found in many biologically … Read more

Acetaminophen (Paracetamol)

Acetaminophen (Paracetamol)

Acetaminophen (Paracetamol) relieves pain and fever, widely used as an OTC analgesic-antipyretic. It inhibits central prostaglandin synthesis with minimal anti-inflammatory effect. Chemical Formula: C₈H₉NO₂ Mechanism of Acetaminophen (Paracetamol): Weak COX inhibition in CNS No peripheral anti-inflammatory effect Acts on serotonergic & endocannabinoid systems (minor) Uses of Acetaminophen (Paracetamol): Fever Mild to moderate pain Preferred in … Read more

Naproxen

Naproxen

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

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