Medicinal Chemistry Terms

Conrad Lewis
Flashcards by Conrad Lewis, updated more than 1 year ago
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1 Chemistry Flashcards on Medicinal Chemistry Terms, created by Conrad Lewis on 12/16/2015.
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absorption the movement of a drug from its site of administration to the bloodstream
active pharmaceutical ingredient (API) the chemical in an administered drug that is responsible for its biological activity
adverse effect an undesired effect of a drug
alkaloid a molecule found in a natural source with a basic nitrogen and a level of structural complexity
allosteric site a site on an enzyme or receptor that is not bound by a substrate or response-causing ligand. Noncompetitive inhibitors (enzymes) and noncompetitive antagonists (receptors) bind at allosteric sites.
alpha-helix (α-helix) a type of secondary structure in which the protein backbone assumes a spiral conformation
amide linkage the amide bond formed between individual amino acid residues in a protein backbone
analgesic pain killer
analogues compounds related to a lead and prepared in an attempt to optimize the desired properties of the lead
apparent volume of distribution (Vd) a hypothetical volume of plasma that is required to contain a specified drug dose
area under curve (AUC) the area beneath a Cp-time curve. AUC is a measure of drug exposure.
arsenicals an early synthetic drug class that was used to treat syphillis and certainly protozoan infections
assay a general term for testing the biological activity of a molecule. An assay may be performed either in vivo or in vitro.
beta-sheet (β-sheet) a type of secondary structure in which the protein backbone assumes a fairly flat shape formed by a back-and-forth flow of the chain
binding energy the free energy of binding between a drug and its target based on the dissociation equilibrium constant between the drug and target (K)
bioavailability (F) the fraction of an drug dose that actually reaches the bloodstream from its site of administration 32f4605b-193f-4c74-80e0-00d7bd9727ac.GIF (image/GIF)
bioequivalence testing an abbreviated clinical trial used by generic manufacturers to show that a generic product is biologically similar to an existing branded drug
bioisosteres isosteres that specifically preserve electronic and hydrogen bonding characteristics when one group is exchanged with another
bolus an amount of drug that is administered, typically intravenously, in a single burst
Caco-2 cells a cell that is used in cell permeability assays
cell permeability the ability of a molecule to passively cross cell membranes. High cell permeability indicates that a molecule will likely be well absorbed from the digestive system.
central compartment blood plasma
Cheng-Prussoff equation an equation that can convert an IC50 value to a Ki value 558dfa9e-b896-4501-b464-5e549e2599af.GIF (image/GIF)
classical isosteres isosteres that specifically preserve steric bulk when one group is exchanged with another
clearance (CL) the removal of a drug from the bloodstream, normally by either excretion or metabolism. The variable CL has units of either mL/min or mL/min/kg.
combinatorial chemistry a method, often automated, for making large collections of molecules using varied building blocks around a molecular scaffold
compartment model a method for describing how a drug distributes into the various tissues of an organism
competitive inhibitor an enzyme inhibitor that binds at the active site of an enzyme. Competitive inhibitors decrease the affinity of an enzyme for its substrate, and therefore increases Km.
composition of matter a type of patent that covers new chemical substances, especially drugs
compound library a collection of molecules that can be used to test for biological activity against a protein target
concensus scoring the use of multiple scoring methods in an in silico screen to increase the relability of the resulting hits
cytochrome P-450 (CYP) a superfamily of enzymes, mostly associated with the liver, that perform many oxidative metabolic reations on drugs
depolarization the flow of ions across a cell membrane from the side with high concentration to the side with low concentration
desensitization an abnormally low response to a drug, often because of downregulation of a receptor
directed combinatorial chemistry the use of combinatorial chemistry to generate libraries focused upon the SAR around a lead
distribution the transport of a drug to and from its site of action by the bloodstream
distribution phase the time period during which an absorbed drug reaches its full volume of distribution
docking the computer simulation of a molecule's binding to a target protein
downregulation a decrease in receptor expression by a cell in response to a continuous, high-level stimulation of the receptor
drug-like a description of a compound with a molecular weight between 400 and 500 g/mol and a lipophilicity (log P) of near 5
drug product the entire administered drug. For orally delivered drugs, the drug product includes the drug substance and all the binders, dyes, and fillers in the pill.
drug substance the active material within a drug product
drug-target residence time the half-life of a drug-receptor complex as it equilibrates between its bound and unbound state
elimination any process that causes a decrease in the concentration of a drug in the bloodstream. Both metabolism and excretion are elimination processes.
elimination phase the period of time after a drug has reached its full volume of distribution and is being cleared from the plasma
elimination rate constant (kel) a rate constant that describes rate of elimination for a drug. Elimination rate constants normally correspond to first-order processes and have units of inverse time.
endogenous ligand a ligand that is found naturally in the body
enzyme (E) usually a protein, a biological catalyst that converts a substrate to a product
enzyme-substrate complex (E-S) the aggregate substance formed by binding between an enzyme and its substrate
excretion the removal of waste from the body. For drugs, excretion is normally associated with the generation of urine by the kidneys through the filtration of blood.
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