Question

8. In the section "Designing the Drug Thalidomide", you learned that researchers create various analogues to determine which structural features are necessary for biological activity and which are responsible for side effects. The analogues were created using the molecule shown below. Using the information found in Tabkw 3, sraw the corresponding analogs #7, 8, and 11.

9. Thalidomide is known to be an inhibitor of TBF-a. TNF-a is a protein mediator, and when to much of this mediator is present, it can cause muscle weakness and body wasting as you read in the section "designing the drug thalidomide" and in the background. In table 3, the concentration of which 50% inhibition of TNF-a Production occurs in blood cells production occurs in blood cells (IC50 in uM) Is provided. Compare and/or Contrast the IC50 values of thalidomide Compared to the analog that Just have the addition of the aromatic ring (compound number six) Or the analog that contain nitrile or the analog that contain night trial (-CN; #7) or alkoxy (-OCH3 or -OCH2CH3; #8-11) substituents on the added aromatic ring.

10. Are alkoxy Substituents found in the analogues #8-11 electron donating or electron withdrawing grouos on the aromatic ring?

please help with these questions thank you! explanations as well

8. (3 pts.) In the section Designing the Drug Thalidomide", you learned that researchers create various analogs to determine which structural features are necessary for biological activity and which are responsible for side effects. The analogs were created using the molecule shown below. Using the information found in Table 3. draw the corresponding analogs #7, 8, and 11. O o NH2 O X X Analog #7 Analog #8 Analog #11 9. (2 pts) Thalidomide is known to be an inhibitor of TNF-a. TNF-a is a protein mediator, and when too much of this mediator is present, it can cause muscle weakness and body wasting as you read in the section Designing the Drug Thalidomide and in the background. In Table 3, the concentration at which 50% inhibition of TNF-a production occurs in blood cells (ICso in uM) is provided. Compare and/or contrast the ICse values of thalidomide compared to the analogs that just have the addition of the aromatic ring (compound #6) or the analogs that contain nitrile (-CN; #7) or alkoxy (-OCH3 or -OCH-CH3 #8-11) substituents on the added aromatic ring. 10. (1 pt.) Are alkoxy substituents found in the analogs #8-11 electron donating or electron withdrawing groups on the aromatic ring?

Answer 1

if you have any doubts feel free to ask me

CN Analog IC50 =150 MM N. # 7 O -OCH₂ or -NH₂ Analog 8 8 I 60=1200M Analog in -OCH, CH₂ "OCH₂ CH₂ I 50 = 56 MM "NH X / In analog 6 where there is no substitution on aromatic ring IC50=260MM ; This means that the concentration of drug should be 2600M to half it half have half of marimm inhibitory activity Now when x2 is a election with bawing group like CN, I C= 150 MM This means at low concentation of this it is showing higher inhibitory activity than without any substitution. When X and X is substituted with elechon - donating groups , value keep on decreasing as election donating activity increases. 30 when X, Foch, ch, and Y = OCH, CH₂ Il wo= 56MM. Hence this anolog lche best drug because at very low concenbation, it has maximum inhibitory activity drug the ICGO is 1

If you like please rate my answer.