Freeman, David S.

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University of Montana

University of MontanaScholarWorks at University of MontanaSyllabi Course SyllabiSpring 1-2003PHAR 422.01: Medicinal Chemistry IIDavid S. FreemanUniversity of Montana - MissoulaLet us know how access to this document benefits you.Follow this and additional works at: https://scholarworks.umt.edu/syllabiThis Syllabus is brought to you for free and open access by the Course Syllabi at ScholarWorks at University of Montana. It has been accepted forinclusion in Syllabi by an authorized administrator of ScholarWorks at University of Montana. For more information, please contactscholarworks@mso.umt.edu.Recommended CitationFreeman, David S., "PHAR 422.01: Medicinal Chemistry II" (2003). Syllabi. 4285.https://scholarworks.umt.edu/syllabi/4285PHARMACY 422 MEDICINAL CHEMISTRY II 2003 SPRING SEMESTERINSTRUCTOR: David Freeman, Office -  SB 308 Office Phone: 243-4772 Home Phone: 728-6551E-mail: dfreeman@selway.umt.eduEXAMS AND GRADING:First Exam: Friday, February 28, 1 p.m. - 50 pointsSecond Exam:Friday, March 21, 1 p.m. - 70 points Third Exam: Monday, April 28,1 p.m. - 80 pointsFinal Exam: -100 points10 Point Quizzes: Best 5 or 6 out of 6 scores - 50 or 60 pointsTotal Points: 350 to 360 A = 90-100% B = 80-89% C = 70-79% D = 65-69%* All EXAMS are comprehensive* All exams and quizzes must be taken at scheduled times* Instructor must be informed BEFORE missing a scheduled exam periodand MUST be based on GOOD REASONS* Missed exam periods must be made up within 2 days* No make up quizzesSTUDENT PERFORMANCE OBJECTIVES:1. Know the chemical structures of important neurotransmitters or hormones and the biochemical pathways for their syntheses and metabolism2. Know the major biochemical events triggered by the activation of receptors important for drug action3. Given the chemical structure of a drug, know its pharmacologic or therapeutic class4. Given the chemical structure of a drug, know important chemical features (acid/base or lipophilic properties, chemical groups affecting absorption, distribution, or metabolism, chemical groups affecting potency or receptor interaction, chemical groups affecting storage or formulation)that contribute to the drug's pharmacological activity5. Given the chemical structure of a drug, know important chemical changes that will predictably alter the pharmacological properties (potency, duration of action, etc.) of the drug6. Given the chemical structure of a drug, know the important biological receptors it interacts with and the biochemical events produced by these interactions7. Given the common or generic name of a drug, know its pharmacologic or therapeutic class, some of its important chemical properties (structural skeleton or chemical class, acid/base, etc.), the receptors it interacts with and the biochemical events produced by these interactionsTEXTBOOK: Goodman & Gilman's "The Pharmacological Basis of Therapeutics", Tenth EditionReading In TextI. Antihyperlipidemic Agents972-977 A. Review of the Biochemical Processing of Lipids1. Storage of cholesterol and triglycerides2. Lipid transport and blood lipoproteins3. Abnormal Lipid Metabolism and pathophysiologyB. Chemistry and Biochemical Mechanisms of Agents984-987 1. Agents inhibiting cholesterol synthesis (HMG CoA Reductase Inhibitors)* LOVASTATIN PRAVASTATIN SIMVASTATIN FLUVASTAT1N ** ATORVASTATIN CERIVASTATIN *989-990 2. Bile acid binding resins ‘CHOLESTYRAMINE COLESTIPOL COLESEVELAM*991-994 3. Agents altering blood lipoprotein patterns* NICOTINIC ACID CLOFIBRATE GEMFIBROZIL FENOFIBRATE *995 4. Prospectus - New agents in developmentReadingIn TextII. Antihypertensive DrugsA. Overview of the Biochemical and Physiological Factors Responsible for HypertensionB. Chemistry and Biochemical Mechanisms of Agents 883-885 1. Alteration of the sympathetic nervous system877-881 2. Alteration of the central nervous system*METHYLDOPA CLONIDINE GUANABENZ GUANFACINEGUANADREL*885-889 3. Vasodilators * HYDRALAZINE MINOXIDIL NITROPRUSSIDE *893, 810-813 4. Alteration of renin-angiotensin system817-819 a. Angiotensin converting enzyme inhibitors (ACE inhibitors)820-824 * CAPTOPRIL ENALAPRIL LISINOPRIL FOSINOPRIL BENAZEPRIL** MOEXIPRIL PERINDOPRIL QUINAPRIL RAMIPRIL TRANDOLAPRIL 829-833 b. Angiotensin receptor antagonists* LOSARTAN CANDESARTAN IRBESARTAN VALSARTAN ** TELMISARTAN EPROSARTAN *833-834 5. Prospectus - New agents in developmentIII. Anticoagulant, Thrombolytic, and Antiplatelet Agents1519-1521 A. Biochemical Processes of the Blood Clotting Systems1530-1531 B. Prothrombin time and clotting testsC. Chemistry and Biochemical Effects of Agents1. Calcium chelators * EDTA CITRATE *1521-1522 2. Heparin and its derivatives* HEPARIN ARDEPARIN DANAPAROID DALTEPARIN ** ENOXAPARIN TINZAPARIN FONDAPARINUX * a. Antagonist * PROTAMINE SULFATE *1526-1528 3. Oral Anticoagulantsa. Natural product and model agent* BISHYDROXYCOUMARIN *b. Synthetic agents * WARFARIN *1531-1533 4. Thrombolytic agents ‘ STREPTOKINASE t-PA UROKINASE*1534-1536 5. Antiplatelet/Antithrombotic agents* ASPIRIN TICLOPIDINE CLOPIDOGREL EPTIFIBATIDE * ‘ DIPYRIDAMOLE TIROFIBAN ABCIXIMAB *6. Inhibitors of fibrinolysis* AMINOCAPROIC ACID APROTININ TRANEXAMIC ACID *IV. Agents Useful for Treating Heart FailureA. Cardiac Glycosides 933-935 1. Cardiac ion channels and mechanism of action of Glycosides916-918 2. Definitions, Sources, and Chemistry* DIGOXIN DIGITOXIN OUABAIN*927 B. Phosphodiesterase Inhibitors * AMRINONE MILRINONE *928-929 C. Prospectus - New treatments for heart failureV. Antianginal Agents843-848 A. Organic Nitrates - Chemistry and Mechanisms* NITROGLYCERIN ISOSORBIDE DINITRATE ISOSORBIDE MONONITRATE 853-858 B. Calcium Channel Blockers - Mechanisms1 .‘ VERAPAMIL DILTIAZEM MIBEFRADIL *2. Dihydropyridines: ‘ NIFEDIPINE NIMODIPINE NISOLDIPINE ** AMLODIPINE NICARDIPINE FELODIPINE ISRADIPINE *Reading In TextVI. Diuretic Agents757-763 A. Overview of the Biochemical Functioning of the Nephron763-766 B. Chemistry and Mechanisms of Carbonic Anhydrase Inhibitors * ACETAZOLAMIDE *767-768 C. Chemistry and Mechanisms of Osmotic Diuretics * MANNITOL *769-772 D. Chemistry and Mechanisms of "Loop" or High-Ceiling Diuretics* FUROSEMIDE BUMETANIDE TORSEMIDE ETHACRYNIC ACID *773-776 E. SAR and Chemistry of Thiazides‘ HYDROCHLOROTHIAZIDE CHLOROTHIAZIDE METHYCLOTHIAZIDE QUINETHAZONE*777-781 F. Potassium-sparing diuretics * SPIRONOLACTONE TRIAMTERENE AMILORIDE 784 G. Prospectus - New diuretics in developmentVIII. Analgesic-Antipyretic-Antiinflammatory and Antigout Agents670-679 A. Chemistry, Biochemistry, and Overview of EicosanoidsB. Nonsteroidal Antiinflammatory Drugs (NSAIDs)687-692 1. Mechanisms of action692-694 2. Adverse effects696-699 3. Salicylates * ACETYLSALICYLIC ACID DIFLUNISAL ** OLSALAZINE SULFASALAZINE *703-704 4. Para-aminophenols * ACETAMINOPHEN *705-709 5. Acetic acid derivatives * INDOMETHACIN SULINDAC ** TOLMETIN KETOROLAC DICLOFENAC ETODOLAC *710-713 6. Propionic acid derivatives * IBUPROFEN NAPROXEN** FENOPROFEN KETOPROFEN OXAPROZIN *713-714 7. * PIROXICAM MELOXICAM NABUMETONE*714-715 8. Selective COX-2 Inhibitors * CELECOXIB ROFECOXIB VALDECOXIB *740 C. Inhibitors of Leukotriene Biosynthesis and Receptor Antagonists* ZILEUTON ZAFIRLUKAST MONTELUKAST *716-717 D. Gold compounds * AUROTHIOGLUCOSE AURANOFIN ** GOLD SODIUM THIOMALATE *718 E. Disease Modifying Antirheumatoid Drugs (DMARDs)‘ METHOTREXATE LEFLUNOMIDE ETANERCEPT INFLIXIMAB* ‘ SULFASALAZINE HYDROXYCHLORAQUINE PENICILLAMINEAZATHIOPRINE*F. Antigout agents719-720 1. Decreased granulocyte activity ‘ COLCHICINE*721-722 2. Inhibit uric acid synthesis * ALLOPURINOL *722-724 3. Uricosuric Agents * PROBENECID PHENYLBUTAZONE SULFINPYRAZONE726-727 G. Prospectus - New antiinflammatory treatmentsIX. Opioid Analgesic Agents569-574 A. Biochemistry of Endorphins, Enkephalins, and Their Receptors578-579 B. Natural Product and Model Agent * MORPHINE *587-590 C. SAR, Stereochemistry, and Chemical Properties1. Chemical features of morphine2. N-Substituents producing agonist, partial agonist, or antagonist effects3. Synthetic agents‘ HEROIN HYDROMORPHONE CODEINE MEPERIDINE LEVORPHANOL** BUTORPHANOL METHADONE FENTANYL PENTAZOCINE ETORPHINE * ‘ NALOXONE NALTREXONE DEXTROMETHORPHAN*X. Methylxanthines743-746 A. Chemistry and Biochemical Mechanisms

PHAR 422.01: Medicinal Chemistry II

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PHAR 422.01: Medicinal Chemistry II

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