Intro to Medicinal Chem

the science that deals with the discovery or design of new potential therapeutic agents and their development into useful medicines

Prototype having desired activity but also other undesirable characteristics, e.g., toxicity, other activities, insolubility, metabolism problems, oral bioavailability

polymer chains of amino acids that loop and fold to produce grooves, cavities, and clefts that are ideal sites for interaction with other molecules

How do molecules interact with proteins?

-interacts with the target consistently needed to achieve the desired effect

-amenable to synthetic modifications needed to improve properties

-Possesses, or can be modified to possess, physical properties consistent with its ability to reach the target after administration

conducting a biological assay on a large collection of compounds to identify compounds that have the desired activity. Initially, these compounds may bind weakly to the target and known as "hits."

Hits can be considered as ___ to leads

strength of the biological effect, i.e., how much (what concentration) of the compound required to achieve a defined level.

Administering less drug is desirable. T/F?

the process by which a drug reaches the bloodstream from its site of administration

to which "compartments" in the body the drug goes. For example, some drugs stay primarily in the bloodstream, while others distribute extensively into tissues.

the action of specific enzymes on a drug to convert it to one or more new molecules (called metabolites)

means by which the body eliminates an unchanged drug or its metabolites

the process of taking a compound identified from the drug discovery process through the steps to bring it to market: preclinical development, clinical development, and regulatory approval

What are the typical stages of modern rational drug discovery and development?

Which category do cis-trans isomers fall under?

-two mirror-image compounds that are non-superimposable

-identical physical properties

-non-distinguishable with the exception of their ability to rotate plan-polarized light