Lead Compound Identification: Natural Sources

Combinatorial chemistry A method to create vast numbers of chemical compounds for drug discovery. Lead Compound A molecule with desired pharmacological activity, serving as a starting point for drug development. Dr. Saki Raheem A professional involved in drug discovery or related research. Organic Chemistry The branch of chemistry dealing with carbon-based compounds. Historical Progression of Therapeutics Evolution of medical treatments from plant, microorganism, marine, and animal sources. Natural Products Compounds derived from natural sources like plants, microorganisms, marine life, and animals. Alkaloids Nitrogen-containing organic compounds found in plants with pharmacological effects. Ephedrine An alkaloid used in herbal remedies with stimulant properties. Quinine An alkaloid from cinchona bark used to treat malaria. Morphine An alkaloid from opium with potent pain-relieving properties. Chloroquine An antimalarial drug replacing quinine with fewer side effects. Procaine A local anesthetic developed from cocaine simplification. Artemisinin An antimalarial compound derived from the sweet wormwood plant. Plasmodium falciparum A dangerous malaria-causing parasite transmitted by mosquitoes. Dichlorodiphenyltrichloroethane (DDT) 1/6 A pesticide used to eradicate mosquitoes and reduce malaria prevalence. Van der Waals Forces Weak intermolecular forces influencing molecular interactions. Pharmacophore The 3D arrangement of atoms responsible for a drug's biological activity. Mirror Image Isomer A molecule with a reversed spatial arrangement of atoms compared to another. Prophylactic A preventive agent administered to avoid disease occurrence. Ciclosporin An immunosuppressant derived from a soil fungus, used post-organ transplants. Lipstatin An inhibitor of pancreatic lipase from Streptomyces, a lead compound for anti-obesity drugs. Curacin A An antitumor compound isolated from a marine cyanobacterium. Magainins Antibiotic polypeptides extracted from the skin of the African frog Xenopus laevis. Halichondrin B An antitumor agent derived from marine sources. Eribulin An antitumor agent used in cancer treatment. Xenopus laevis African frog species used for research on novel agents Epibatidine Potent analgesic compound from Ecuadorian poison frog skin Epipedobates anthonyi Species of Ecuadorian frog known for skin extracts Bungarus fasciatus Snake species known for toxins like ±bungarotoxin 2/6 Tetrodotoxin Non-peptide toxin from puffer fish, highly potent Teprotide Compound isolated from Brazilian viper venom Captopril Antihypertensive drug developed from Teprotide ACE inhibitors Drugs like cilazapril and captopril targeting angiotensin-converting enzyme Neurotoxins Toxins like those from Clostridium botulinum causing food poisoning Conotoxin Peptide toxin from marine cone snail, e.g., Ziconotide Ziconotide Synthetic form of conotoxin used for chronic pain treatment Clostridium botulinum Bacterium producing neurotoxins causing muscle spasm prevention 3,5-dicaffeoylquinic acid derivatives Compounds derived from (-)-quinic acid with specific substitutions at 3 and 5 positions. Tetrahedron Letters A scientific journal where the synthesis of Halichondrin B was published. BnO Benzyl ester functional group in the chemical structure. OBn Hydroxyl group attached to a benzyl ester in the chemical structure. TBSO Tert-butyldimethylsilyl ether functional group in the chemical structure. (-)-quinic acid A specific form of quinic acid used as a starting material in chemical synthesis. 3,5-di-O-caffeoylquinic acid A compound derived from quinic acid with two caffeoyl groups at positions 3 and 5. 3/6 A compound derived from quinic acid with two feruloyl groups at positions 3 and 5. 3,5-di-O-feruloylquinic acid A compound derived from quinic acid 3,5-(3,4-dimethoxycinnamyl)quinic acid with specific dimethoxycinnamyl groups at positions 3 and 5. Reagents and conditions Specific methods and chemicals used in the chemical synthesis process. Combinatorial Chemistry A method involving systematic synthesis of diverse molecules by combining building blocks. High Throughput Screening (HTS) Efficient drug testing method providing accurate results on small quantities of substances. Solid-Phase Techniques Chemical reactions where starting materials are attached to a solid support for sequential reactions. Merrifield Solid Phase synthesis A method for peptide synthesis where starting material is attached to a solid support. Anchor/linker Molecular unit covalently attached to a polymer chain on a solid support for chemical reactions. Resins Materials used as solid supports in solid-phase synthesis, such as polystyrene beads. Mix and split strategy A method in combinatorial synthesis where starting materials are divided, mixed, and recombined to generate diverse molecules. Lead compound A compound identified as a starting point in drug design for further optimization. Dipeptides 16 possible combinations of two amino acids 4/6 Parallel synthesis Each dipeptide made in a separate flask Combinatorial synthesis Generating dipeptides using mix and split procedures Analogues Variants of a lead compound for optimization Solid-phase synthesis Chemical reactions on a solid support like resin Directed combinatorial library Synthesizing specific structures in a library Unbiased combinatorial library Producing a variety of structures in a library Semisynthetic drugs Prepared from natural products with modifications Total synthesis Creating natural product analogs from scratch Lead compounds isolation Extracting compounds from various natural sources Solid-phase techniques Chemical reactions on solid supports like beads Oligomer production Molecule growth in one direction only Template production Synthesis proceeding in different directions Natural products Rich source of lead compounds for drug discovery Structure-activity relationships Study of how chemical structure affects biological activity Active compounds Compounds with significant biological effects Less active compounds Compounds with lower biological effects Biological activity Effects of a compound on living organisms Side effects 5/6 Unintended effects of a drug or compound Natural product-derived compounds Compounds in clinical trials from natural sources Molecular structures synthesis Creating structures on solid support like beads Wide range of starting materials Variety of compounds used in synthesis Starting with beads Initiating chemical reactions on solid supports Different structures attached to beads Each bead carrying a unique chemical structure Mix and split procedures Method to generate diverse compound mixtures Lead compound optimization Improving activity and properties of lead compounds 6/6