Exam 1 Flashcards
Relationship of structure and activity
Chemical structure influences biological activity through Physicochemical properties
Similar molecules _____ exert similar biological activities
Usually
11 reasons for developing a new drug
No current treatment Vulnerable drug Lack of site selectivity Absorbed too quickly Water insoluble Formulation problems Poor absorptions Chemically unstable drug Intolerance or irritation Poor doctor or nurse Poor patient acceptance
8 places where drugs come from
Combinatorial chemistry Random screening Natural products Chemogenomics Privileged motifs Literature and patients Ligand design Endogenous ligands
Hits/leads relationship from new drugs
New drugs come from several places and hits are biologically active to make leads. Leads make clinical candidates
Hypothetical drug development formula
Potency, efficacy, selectivity, absorption, distribution, metabolism, excretion, protein binding
Once a drug reaches the target, the two must _____ and _____ to begin the process to produce the desired effect
Recognize and bind
Most target sites are
Proteins
Is the binding of the drug to the reversible?
Usually reversible
Properties of drug molecules
Low molecular weight
Not too lipohilic
Not too hydrophobic
Presence of functional groups
Properties of durggable targets
Usually a protien
Leads to a biological response
Doesn’t cause toxicity at therapeutic dose
Most drug target are _____, and majority of the ligand interactions are steroselective
Chiral
Typically, biological activity resides mostly in one _______ over the other
Enantiomer
Pfeiffer’s rule
Preference of one enantiomer over the other often increases with an increase in receptor affinity
On target toxicity
Type of adverse effect taht results from pharmaceutical drug exposure is commonly due to interactions of the drug with its intended target
