Medicinal Chemistry

chemical sciences

advanced

K_W01 ‒ 23 → knowledge

K_U01 ‒ 32 → cognitive and noncognitive skills

K_K01 ‒ 11 → social competence

The aim of the course is to familiarize the student with the basic concepts of medicinal chemistry. Modern methods of drug design and development will be discussed, as well as ways to deal with problems arising during these processes (problems with solubility and bioavailability). Methods used for the synthesis of drugs and their analogues (classical organic synthesis, combinatorial chemistry, mechanochemistry) will be thoroughly discussed.

Basic literature:

G. Thomas, Medicinal Chemistry An Introduction, John Wiley & Sons, 2007

Auxiliary literature:

G. Patrick, An Introduction to Medicinal Chemistry, Oxford University Press

EU1 - characterizes modern methods in drug design and development

EU2 - characterizes core methods in drug synthesis

EU3 - analyzes structure-activity relationship

For lecture and exercises:

EU1:

A - verification indicates that the student without noticeable imperfections characterizes modern methods in drug design and development

B+ - verification indicates that the student almost correctly characterizes modern methods in drug design and development and does not fulfil the higher grede requirements

B - verification indicates that the student substentially characterizes modern methods in drug design and development and does not fulfil the higher grede requirements

C+ - verification indicates that the student substentially but inconsitently lcharacterizes modern methods in drug design and development and does not fulfil the higher grede requirements

C - verification indicates that the student in most test cases lcharacterizes modern methods in drug design and development and does not fulfil the higher grede requirements

D - verification indicates that the student does not characterize modern methods in drug design and developments and does fulfil the higher grede requirements

EU2:

A - verification indicates that the student without noticeable imperfections characterizes core methods in drug synthesis

B+ - verification indicates that the student almost correctly characterizes core methods in drug synthesis and does not fulfil the higher grede requirements

B - verification indicates that the student substentially characterizes core methods in drug synthesis and does not fulfil the higher grede requirements

C+ - verification indicates that the student substentially but inconsitently characterizes core methods in drug synthesis and does not fulfil the higher grede requirements

C - verification indicates that the student in most test cases characterizes core methods in drug synthesis and does not fulfil the higher grede requirements

D - verification indicates that the student does not characterize core methods in drug synthesis and does fulfil the higher grede requirements

EU3:

A - verification indicates that the student without noticeable imperfections nalyzes structure-activity relationship

B+ - verification indicates that the student almost correctly nalyzes structure-activity relationship and does not fulfil the higher grede requirements

B - verification indicates that the student substentially nalyzes structure-activity relationshipand does not fulfil the higher grede requirements

C+ - verification indicates that the student substentially but inconsitently nalyzes structure-activity relationshipand does not fulfil the higher grede requirements

C - verification indicates that the student in most test cases nalyzes structure-activity relationship and does not fulfil the higher grede requirements

D - verification indicates that the student does not nalyze structure-activity relationship and does fulfil the higher grede requirements

The final grade x is determined by the value st(w) defined as

st(w)= 5, if 4,5 < w; st(w)= 4.5, if 4.25 < w ≤ 4.5; st(w)= 4, if 3.75 < w ≤ 4.25; st(w)= 3.5, if 3.25 < w ≤ 3.75; st(w)= 3, if 2.75 < w ≤ 3.25; st(w)= 2, if w ≤ 2.75

by the n-grades, i.e., numeric values of grades N(A)=5, N(B+)=4.5, N(B)=4, N(C+)=3.5, N(C)=3, N(D)=2, and by the rule:

● if all the n-grades for the associted classes are at least 3 and y is their average, then x is given by x=IN(st((y+z)/2)), where IN is the inverse function

of N, and z is the weighted average of n-grades given to all verifications with weights 2 assigned to exams, and weights 1 assigned to other forms of

verification

● if one of the grades given to the assaciate classes is either D or F, then x=D.