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The presence of bulky groups can turn agonists into antagonists. The presence of bulky groups can also make antibiotic molecules more difficult for bacterial enzymes to degrade.
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How can the conformation restriction of drug molecules be restricted?
This can be done by forming a ring structure or using rigid functional groups.
What is the name given to a drug when developed?
It is named according to the rules set by organic chemistry based on the groups of molecules it contains.
What are the advantages and disadvantages of conformation restriction of drug molecules?
Its activity will increase as there is a greater chance that the drug molecules will be of the right conformation. Its selectivity will also increase as there is less chance that the drug molecules will be of the wrong conformation. However, drug molecules with restricted conformation may take a longer time to synthesise as they tend to be more complex in structure.
Why do mole drug molecules have both water-soluble and oil-soluble functional groups?
The drug has to be water soluble to dissolve as gastrointestinal fluid is aqueous. The drug also has to be oil soluble as only the lipid soluble non-ionized form can readily diffuse across the lipid membrane.
How can drugs with the COOH be made more lipophilic?
The COOH group can be changed to a tetrazole group to increase the drug's lipophilicity. Both groups have a similar pKa value so the ionisation of the molecules should be similar.
What are drug business groups called?
pharmaceuticals
How can penicillin be structurally modified to overcome bacterial resistance?
In the bicyclic system, a bulky group can be added to position 6. This creates a steric shield which leads to steric hindrance. The beta-lactam ring is hence more protected and the drug can become more resistant to beta-lactamases of bacteria.
How cisplatin treat cancer?
Cisplatin is an anti-cancer drug consisting my a a platinum atom, two chlorine atoms and two amine groups. The two chlorine groups are substituted for water molecules in the body. The drug works by forming co-ordinate bonds with guanine bases in DNA, this prevents the process of DNA replication and hence it stops malignant tumours frow growing and spreading.
What are the phases of drug metabolism?
There are two phases of drug metabolism: Phase I - Functionalizes the drug molecule. In this phase, there are addition or modification of functional groups in order to make them more susceptible to phase II of metabolism. Phase II - Conjugates the molecule. In this phase, the functional handles of the molecule can be conjugated to highly hydrophilic molecules in order to facilitate the excretion.
If someone could not digest maltose what type of drug would you develop for them?
A drug that cleaves the two glucose molecules
How many molecules of diazepam are in 200 mg of the drug?
4.2x10^20
How can adrenergic drugs be structurally modified to be beta 2 selective?
The amino group of the adrenergic drug can be substituted with a bulkier amino substituents to enhance beta activity. OH groups can also be added to positions 3 and 5 of the benzene ring of the drug to cause beta 2 selectivity.
