SCOPE:This course is designed to impart fundamental knowledge, and skills to design the structure and correlate with the functions of drugs. It includes details on Chemistry, Mechanism of action, adverse effects, uses of Chemotherapeutic Agents, and the synthesis of some important drugs. The course also covers the basics of modern drug design techniques, including QSAR and combinatorial chemistry. This subject will introduce students to structure-activity relationships, which help to predict and evaluate the therapeutic effects of different drugs. In alignment with the United Nations Sustainable Development Goals (SDGs), particularly: SDG 3(Good Health and Well-being), SDG 9(Industry, Innovation, and Infrastructure), SDG 12 (Responsible Consumption and Production) SDG 13 (Climate Action) this syllabus emphasizes the design and development of safer, effective, and environmentally responsible drugs. Students will explore modern drug discovery approaches including role of AI in drug discovery, computer-aided drug design (CADD), and prodrug strategies that aim to enhance therapeutic efficacy while minimizing ecological and health risks.The course helps to equip the students with the necessary knowledge and skills for the synthesis and analysis of new synthetic molecules. In addition to the foundational knowledge of drug design and synthesis, this course provides students with a comprehensive understanding of pharmacokinetics and pharmacodynamics, enabling them to assess how drugs interact with the body at a molecular level. The curriculum also provides a commitment to continuous learning and staying updated with advancements in the field of medicinal chemistryCOURSE OUTCOMES: Upon successful completion of this course, students shall be able to; KNOWLEDGE K1: Memorize the chemistry of drugs concerning their biological activityK2: Describe the concept of rational drug design, prodrug and different modern drug design techniques K3: Summarize knowledge in the chemistry of different anticancer, antibiotics, and different anti-viral agentsK4: Outline the AI tools and platforms used in medicinal chemistry.K5: Sketch the synthesis of therapeutic useful drug molecules using available synthetic pathwaysK6: Illustrate the SAR of some important drug classes concerning their biological activitySKILLS1: Prepare compounds of medicinal interest using available synthetic and new pathwaysS2: Analyse the effects of various functional groups in the therapeutic activity of drugsS3: Calculate the percentage purity of synthesized medicinally important compounds by performing assays per pharmacopoeial procedureS4: Estimate the amount of drug present in the synthesized compoundsS5: Apply the significance of physicochemical parameters in the therapeutic actions of drugsS6: Employ standard operating procedures (SOPs) and Good Laboratory Practices (GLP) while performing experiments ATTITUDEA1: Participate in group discussions for the design of a new synthetic pathway of therapeutic agentsA2: Appreciate the relevance of Structural Activity Relationships in the biological action of drugs A3: Explore opportunities for continuous learning and staying updated with advancements in the field of medicinal chemistryA4: Accept the significance of Medicinal Chemistry in the healthcare systemA5: Follow a safe, green, and eco-friendly approach in developing the synthetic scheme of medicinal compoundsA6: Appreciate self-motivation and the ability to engage in self-directed learning COURSE CONTENTS: UNIT-1 Modern concept of rational drug design 9 HrsA brief introduction to Quantitative Structure-Activity Relationship (QSAR) (3 hrs)Combinatorial chemistry and computer-aided drug design(CADD) (2 hrs)Prodrugs: Basic concepts and application of prodrugs (2 hrs)Role of Artificial Intelligence (AI) in Modern Drug Discovery and Medicinal Chemistry (2 hrs)A study of the development of the following classes of drugs, including Classification SAR, synthesis of important drugs (Superscripted by *), Structure not necessary (Superscripted by $), chemical nomenclature, uses, newly approved drugs under each category and brand names of important marketed products.UNIT- II Anti-infective agentsAntifungal Agents 4 HrsAzoles: SAR of azole antifungals, Econazole, Miconazole, Ketoconazole, Fluconazole, Clotrimazole*, Voriconazole$. Posaconazole$, Isavuconazole$ (2 hrs)Antifungal Antibiotics: Amphotericin$, Nystatin$, Griseofulvin (1 hr)Miscellaneous: Tolnaftate*, Micafungin$ (1 hr)Urinary tract anti-infectives 2 HrsSAR of quinolone antibacterial agents (1 hr)Nalidixic acid, Norfloxacin, Ciprofloxacin*, Ofloxacin, Nitrofurantoin*, Methanamine, fosfomycin (1 hr) Antitubercular agents 3 HrsSynthetic anti-TB agents: Isoniazid*, Ethionamide, Pyrazinamide, Paraaminosalicylic acid*, Ethambutol (2 hrs)Anti TB antibiotics: Rifampin$, Capreomycin$, Streptomycin$ XDR, and MDR TB (1 hr)Antiviral agents and Anti-AIDS agents 6 HrsViral life cycle, Viral diseases Amantadine, Rimantadine (1 hr)Acyclovir*, Ganciclovir, Valcyclovir Iodoxuridine*, Zidovudine, Lamivudine$, Didanosine*, Efavirenz$, Nevirapine (4 hrs)New Antiviral Drugs for Treatment of Viral diseases: Remdesivir$,Nirmatrelvir$, Ritonavir$, Molnupiravir$, Nitazoxanide$, Ribavirin$ and Ivermectin$ (1 hr) Antiprotozoal agents 2 HrsIntroduction to protozoal diseases and causative organisms (1 hr) Metronidazole*, Diloxanide Furoate*, Dehydroemetine$, Nifurtimox (1 hr) Anthelmintics 2 HrsBenzimidazoles: Mebendazole, Albendazole*, Piperazine, Diethyl carbamazine*. Antimalarials 4 HrsEtiology of malariaQuinoline Antimalarials: SAR of Quinoline Antimalarials (1 hr) Chloroquine phosphate*, Amodiaquine, Pamaquine, Primaquine*, Proguanil, Cycloguanil, Pyrimethamine (2 hrs)Artimisine derivatives (1 hr). UNIT-III Sulfonamides and Sulfones 4 HrsClassification of sulphonamides, SAR of Sulfonamides (1 hr) Sulfadiazine*, Sulfamethoxazole, Sulfacetamide*, Sulfasalazine (2 hrs) Folate Reductase Inhibitors: Trimethoprim*,Synergistic Action of Cotrimoxazole. Sulfones: Dapsone* (1 hr) UNIT-IVAntibiotics 7 HrsClassification of antibiotics, Chemistry of penicillin (1 hr)Beta-lactam antibiotics: Penicillins. Penicillin G, Ampicillin, Amoxicillin, Cloxacillin (1 hr) Beta-lactamase inhibitors: Clavulanic Acid$, Thienamycin$, Cephalosporins: Cephalexin, Cefadroxil, Cefuroxime (2 hrs)Aminoglycosides: Neomycin$, Amikacin$, Gentamicin$ (1 hr)Tetracycline: Chemistry and SAR of tetracycline, Chlortetracycline$, Doxycyclin$(1 hr).Macrolides: Erythromycin$, Azithromycin$Miscellaneous: Bacitracin, Mupirocin, Chloramphenicol*(1 hr). UNIT-V Antineoplastic agents 7 HrsAlkylating agents: Mechanism and SAR of alkylating agents, Cyclophosphamide*, Mechlorethamine*, Chlorambucil* (2 hrs).Antimetabolites: Mercaptopurine*, Fluorouracil, (1 hr)Methotrexate Antibiotics: Daunorubicin$, Doxorubicin$, Dactinomycin$, Bleomycin$(1 hr) Plant products: Etoposide$, Taxol$, Vincristine$ and Vinblastine$Miscellaneous: Cisplatin, Interferons (1 hr).Newer Anticancer Drugs: Lurbinectedin$, Rituximab$, Cetuximab$, decitabine$, Pemigatinib$, Talazoparib$, Olaparib (2 hrs) UNIT-VI Cardiovascular agents:Antianginal agents and vasodilators 2HrsNitro vasodilators: Isosorbide Dinitrate, Nitroglycerin*, Pentaerythritol tetranitrate*, Nicorandil Antiarrhythmic agents: 3 HrsClass I: Quinidine, Procainamide*, Phenytoin*, Lidocaine* Class II: Beta-blockers- Propranolol*Class III: Amiodarone, BretyliumClass IV: Calcium Channel Blockers: Verapamil, DiltiazemAntihypertensive agents: 4HrsBeta-blockers- Atenolol*, Metoprolol ACE inhibitors: Captopril*, Enalapril, Fosinopril Angiotensin antagonists: Telmisartan, Losartan Calcium channel blockers: Nifedipine*, Amlodipine, Felodipine Adrenergic agents: Clonidine*, Methyldopa. Adrenergic antagonists:Prazosin, Reserpine$. Vasodilators: Hydralazine, MinoxidilDiuretics: 3HrsCarbonic anhydrase inhibitors: Acetazolamide* Thiazides: SAR of thiazide diuretics Chlorthiazide, Hydrochlorothiazide. Loop diuretics: Furosemide*, Ethacrynic acid. Potassium sparing Diuretics: Spironolactone, Triamterene, Amiloride. Osmotic Diuretics: Mannitol.e) Antihyperlipidemic agents: 2HrsTypes of hypolipoproteinaemia, Clofibrate*, Fenofibrate, Cholestyramine, Lovastatin, Simvastatin, Atorvastatin, Probucol.UNIT-VII Anticoagulants and Antiplatelet agents: 1 Hr Warfarin*, Dicoumarol*, Anisindione, Aspirin, Clopidogrel UNIT-VIII Hypoglycaemic agents: 3HrsSulfonylureas: Tolbutamide*, Chlorpropamide*, Glipizide Biguanides: Metformin*. Metaglinides: Nateglinide Thiazolidinediones: Pioglitazone,Rosiglitazone.Glucosidaseinhibitors: Acarbose$, Voglibose$ Miscellaneous: MiglitolUNIT-IX Thyroid and Antithyroid agents 2 HrsBio-synthesis of Thyroid hormone (1 Hr)L-thyroxine, L- Threonine, Propylthiouracil, Methylthiouracil, Methimazole*, Carbimazole (1 Hr) UNIT- X Anticonvulsants 2HrsClassification of anticonvulsants: Phenytoin*, Ethosuximide*, Trimethadione, Carbamazepine, Valproic acid UNIT-XI Hypnotics and sedatives 3 HrsClassification of hypnotics and sedatives: Phenobarbitone*, Diazepam, Alprazolam, Zolpidem, Chlordiazepoxide, Triclofos sodium, SAR of barbiturates, and benzodiazepines
