Medicinal chemistry at Faculty of Pharmacy of UVPS Brno Medicinal Chemistry I: 2nd year summer semester Lectures: General topics: ● history ● nomenclature ● physico-chemical properties and activity ● stuctural features and activity ● structure modifications: homlogy, analogy, isosterism... ● drugs biotransformation ● prodrugs ● drugs research, development, patents & good practices Special topics ● weak and strong analgesics & antiinflammatory drugs ● general & local anaesthetics, muscle realaxants ● CNS agents: antipsychotics, antineurotics, antidepressants, stimulants, cognitive enhancers, halucinogens ● sedatives, hypnotics, antiepileptics, antivomitics, antikinetics ● adrenergic receptors' agonists and antagonists Medicinal Chemistry I: 2nd year summer semester (February - May) Seminars: every Tuesday from 7.30 (compulsory!) ● introduction into the discipline ● syntheses and metabolism of selected weak analgesics and NSAIDs ● syntheses of some opiod receptors' ligands ● syntheses and metabolism of some local & general anaesthetics ● history and syntheses of platinum anticancer drugs ● syntheses of some adrenergics & anobesics ● syntheses and metabolism of some antipsychotics ● syntheses and metabolism of some antidepressants syntheses of selected adrenergic receptor antagonists ● final test ( credit) Medicinal Chemistry II: 3rd year winter semester Lectures ● antibiotics & other antibacterial chemotherapeutics: sulfonamides, quinolones, nitrofuranes, tetracyclins, β-lactameantibiotics: penicilines & cephalosporins, (poly)peptide antibiotics, aminoglycoside antibiotics, macrolide antibiotics etc. ● antitubeculotics & antileprotics ● antiviral agents ● antimycotics ● antiparasitics: antiprotozoal & vermicidal agents; insecticides ● liver protectants, cholagogues, cholelitholytics ● drugs controlling blood clotting ● antihyperlipidemics ● drugs improving heart perfusion, cardiotonics, coronary vascular dilators ● anti-hypertensive drugs ● anti-arrythmics, drugs for erectile dysfunction ● diuretics ● laxatives & antidiarrhoics ● antacids & anti-ulcerative agents: proton pump inhibitors, H2 -antihistamines, gastric cytoprotectants ● anticancer drugs ● insuline(s) & other antidiabetics ● hormones: derived from one amino acid, drugs for thyroid gland, peptide hormones, steroid hormones ● medicines for biologic therapy Medicinal Chemistry II: 3rd year winter semester (September - December) Laboratory practical classes ● every even Thursday from 11.15, compulsory ● synthesis of – an antibacterial drug (sulfacetamide) – a local anaesthetic (lidocaine) – an NSAID (acetylsalicylic acid) – an antiepileptic (phenytoin) – an antimicrobial preservative (methyl- or other paraben) ● products are characterized by a chromatography; the identity is confirmed by NMR or IR spectra ● determination of – pKa of a weakly acidic drug (phenytoin or nitrofurantoin)