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Minani Theobald
University of Rwanda
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Q1. What bring the innovation deficit of the new chemical entities?
Increased demand on safety for drugs
This involve in increasing the trial number then
make most drug reaching to market
Low hanging fruit” have been picked.
The cost taken by the drug discovery to obtain final
product
Q2.During drug design process, there are targets involve in SAR, and
what are they?
Membrane Proteins
Nucleic acids [DNA and RNA]
Enzymes and Hormones
Etc.
Q.3 Why does the drug discovery process is called the wasteful game?
Q.4 List the steps of drug discovery process
Hunch
literature precedent
cell model
animal model
pharmacology in animal model
Pharmacology in human disease.
Screening
Structure based drug design
o Crucial point for reliable high-throughput screening
results is the robustness and quality of the biological
test assays.
o Molecular modeling
o Quantitative structure-activity relationships QSAR
o Structural biology (structure-based drug design) SAR
Q15.what should you do if the compound do not fulfill the requirement for
successful drug development
QQ. State three different ways in which computers are used in the design of
new drugs.
Physicochemical parameters involved in drug activity
quantitative structure activity relationship (QSAR)
quantum chemistry models to determine the most promising
substance of a series
Q24.2. Give the technique can be performed in designing the following drugs
a) GIT drug
b) Drug for meningitis
c) Epileptic drug
d) Peripheral nerves drug
e) Iv injection drug
f) Topical drug or dermal drug
g) Transdermal drug
Q25.what is QSAR
The change in the polarity and ionization of compounds can be
altering their substituents
Q26.you are designing a drug with improving absorption then you find the
functional group you need to remove or mask involves in binding , How can
you overcome this issue?
o Adding non-polar molecules such as alkyl
Q30.metabolic blockers
Q31. List the techniques involve in metabolism improvement. Discuss each
o Steric shields
o Electronic effects of Bioisosteres
o Stereoelectronic modification
o Metabolic Blocker
o Removal of susceptible metabolic groups
o Group Shifts
o Ring Variation
Q35.Regarding toxicity
Q36.what is prodrug
Q37. What are the purposes of prodrug in both pharmaceutical drug designing
and drug formulation processes?
The drug has to be tested to ensure that it is not only safe and
effective, but can be administered in a suitable fashion.
o This involves preclinical and clinical trials covering toxicity,
drug metabolism, stability, formulation, and
pharmacological tests.
a) Explain why old tablets of aspirin that have been left in moist
air smell of vinegar.
b) Explain why aspirin is not very soluble in water.
c) Explain why aspirin is much more soluble in sodium
hydroxide solution than it is in water.
d) Write a chemical equation to show how soluble aspirin is
produced.
e) Explain what happens when soluble aspirin enters the
stomach.
References
1.University Of Rwanda Lecturer’s notes updates 2016-17