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F12MCM Medicinal Chemistry > Definitions > Flashcards

Definitions Flashcards

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1
Q

Agonist

A

An endogenous substance or drug that can interact with a receptor and initiate a physiological or a pharmacological response characteristic of that receptor.

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2
Q

Antagonist

A

A drug or compound that opposes the physiological effects of another. At the receptor level, it is a chemical entity that opposes the receptor-associated responses normally induced by another bioactive agent.

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3
Q

Antimetabolite

A

A structural analog of an intermediate (substrate or coenzyme) in a physiologically occurring metabolic pathway that acts by replacing the natural substrate, thus blocking or diverting the biosynthesis of physiologically important substances.

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4
Q

Baceteriocidal

A

A bacteriocidal compound is one whose mechanism of action leads directly to cell death.

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5
Q

Bacteriostatic

A

A bacteriostatic compound is one that stops a bacterium growing or reproducing but does not kill it directly.

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6
Q

Bioassay

A

A procedure for determining the concentration, purity, and/or biological activity of a substance by measuring its effect on an organism, tissue, cell, enzyme or receptor preparation compared to a standard preparation.

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7
Q

Bioisostere

A

A compound resulting from the exchange of an atom or a group of atoms with another, broadly similar, atom or group of atoms. The objective of a bioisosteric replacement is to create a new compound with similar biological properties to the parent compound. The bioisosteric replacement may be physiochemically or topologically based.

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8
Q

Carrier-linked prodrug

A

A prodrug that contains a temporary linkage of a given active substance with a transient carrier group that produces improved physiochemical or pharmacokinetic properties and that can be easily removed in vivo, usually by hydrolytic cleavage.

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9
Q

Catabolism

A

Consists of reactions involving endogenous organic substrates to provide chemically available energy and/or to generate metabolic intermediates used in subsequent anabolic reactions.

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10
Q

Catabolite

A

A naturally occurring metabolite.

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11
Q

Codon

A

The sequence of three consecutive nucleotides that occurs in mRNA which directs the incorporation of a specific amino acid into a protein or represents the starting or termination signals of protein synthesis.

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12
Q

Coenzyme

A

A dissociable, low-molecular weight, non-proteinaceous organic compound (often nucleotide) participating in enzymatic reactions as acceptor or donor of chemical groups or electrons.

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13
Q

Congener

A

A substance co-generated or synthesised by essentially the same synthetic chemical reactions and the same procedures.

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14
Q

Co-operativity

A

The interaction process by which binding of a ligand to one site on a macromolecule influences binding at a second site.

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15
Q

Distomer

A

The enantiomer of a chiral compound that is the less potent for a particular action.

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16
Q

Drug

A

Any substance presented for treating, curing or preventing disease in human beings or in animals. May also be used for making a medical diagnosis or for restoring, correcting or modifying physiological functions.

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17
Q

Drug targeting

A

A strategy aiming at the delivery of a compound to a particular tissue of the body.

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18
Q

Efficacy

A

Describes the relative intensity with which agonists vary in the response they produce even when they occupy the same number of receptors and with the same affinity.

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19
Q

Enzyme

A

A macromolecule, usually a protein, that functions as a (bio)catalyst by increasing the reaction rate.

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20
Q

Eutomer

A

The anatiomer of a chiral compound that is the more potent for a particular action.

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21
Q

Genome

A

The complete set of chromosomal and extrachromosomal genes of an organism, a cell, an organelle or a virus; the complete DNA.

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22
Q

Homologue

A

Used to describe a compound belonging to a series of compounds differing from each other by a repeating unit.

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23
Q

Hormone

A

A substance produced by endocrine glands, released in very low concentration into the bloodstream, and which exerts regulatory effects on specific organs or tissues distant from the site of secretion.

24
Q

Isosteres

A

Molecules or ions of similar size containing the same number of atoms or valence electrons.

25
Q

Lead discovery

A

The process of identifying active new chemical entities, which by subsequent modification may be transformed into a clinically useful drug.

26
Q

Lead generation

A

The term applied to strategies developed to identify compounds which possess a desired but non-optimised biological activity.

27
Q

Lead optimisation

A

The synthetic modification of a biologically active compound, to fulfil all stereo electronic, physiochemical, pharmacokinetic + toxicologic required for clinical usefulness.

28
Q

Mechanism-based inhibitor

A

A compound that is processed by an enzyme as a normal substance until a highly reactive intermediate is generated that forms a permanent covalent bond to the enzyme and/or coenzyme irreversibly inhibiting the enzyme.

29
Q

Metabolism

A

Comprises the entire physical and chemical processes involved in the maintenance and reproduction of life in which nutrients are broken down to generate energy and to give simpler molecules (catabolism) which by themselves may be used to form more complex molecules (anabolism).

30
Q

Metabolite

A

Any intermediate or product resulting from metabolism.

31
Q

Me-too drug

A

A compound that is structurally very similar to already known drugs, with only minor pharmacological differences.

32
Q

Mutagen

A

An agent that causes a permanent heritable change into the DNA of an organism.

33
Q

Mutual prodrug

A

The association in a unique molecule of two, usually synergistic, drugs attached to each other, one drug being the carrier for the other and vice versa.

34
Q

New chemical entity (NCE)

A

A compound not previously described in the literature.

35
Q

Non-classical isostere

A

**See bioisostere

36
Q

Nucleic acid

A

A macromolecule composed of linear sequences of nucleotides that perform several functions in living cells.

37
Q

Nucleoside

A

A compound in which a purine or pyrimidine base is bound via a N-atom to C-1 replacing the hydroxy group of either 2-deoxy-D-ribose or of D-ribose, but without any phosphate groups.

38
Q

Nucleotide

A

A nucleoside in which the primary hydroxy group of either 2-deoxy-D-ribose or of D-ribose is esterified by orthophosphoric acid.

39
Q

Oligonucleotide

A

An oligomer resulting from a linear sequence of nucleotides.

40
Q

Orphan drug

A

A drug for the treatment of a rare disease for which reasonable recovery of the sponsoring firm’s research and development expenditure is not expected within a reasonable time.

41
Q

Partial agonist

A

An agonist which is unable to induce maximal activation of a receptor population, regardless of the amount of drug applied.

42
Q

Peptidomimetic

A

A compound containing non-peptidic structural elements that is capable of mimicking or antagonising the biological actions of a natural parent peptide.

43
Q

Pharmacokinetics

A

The study of absorption, distribution, metabolism + excretion of bioactive compounds in a higher organism.

44
Q

Pharmacophore

A

The ensemble of steric and electronic features that is necessary to ensure the optimal supra molecule interactions with a specific biological target structure and to trigger its biological response.

45
Q

Placebo

A

An inert substance or dosage form which is identical in appearance, flavour and odour to the active substance or dosage form. It is used as a negative control in a bioassay or in a clinical study.

46
Q

Potency

A

The dose of drug required to produce a specific effect of given intensity as compared to a standard reference.

47
Q

Prodrug

A

Any compound that undergoes biotransformation before exhibiting its pharmacological effects.

48
Q

Quantitative structure activity relationships (QSAR)

A

Mathematical relationships linking chemical structure and pharmacological activity in a quantitative manner for a series of compounds.

49
Q

Receptor

A

A molecule or a polymeric structure in or on a cell that specifically recognises and binds a compound acting as a molecular messenger.

50
Q

Second messenger

A

An intracellular metabolite or ion increasing or decreasing as a response to the stimulation of receptors by agonists.

51
Q

Site-specific delivery

A

An approach to target a drug to a specific tissue, using prodrugs or antibody recognition systems.

52
Q

Structure-activity relationship (SAR)

A

The relationship between chemical structure and pharmacological activity for a series of compounds.

53
Q

Structure-based design

A

A drug design strategy based on the 3D structure of the target obtained by x-ray or NMR.

54
Q

Teratogen

A

A substance that produces a malformation in a foetus.

55
Q

Transition-state analogue

A

A compound that mimics the transition state of a substrate bound to an enzyme.

56
Q

Xenobiotic

A

A compound foreign to an organism.

F12MCM Medicinal Chemistry (3 decks)

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