Explain why structure 4 is a more potent inhibitor (lower IC50 value) than inhibitor 3 and why structure 5 is a much weaker inhibitor (higher IC50 value) than 3 and 4.

Curren'S Math For Meds: Dosages & Sol
11th Edition
ISBN:9781305143531
Author:CURREN
Publisher:CURREN
Chapter9: Parenteral Medication Labels And Dosage Calculation
Section: Chapter Questions
Problem 6.4P
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A schematic representation of the enzyme IspD complexed to inhibitor 3, and a series
of inhibitors 3-5 are shown below.
Ala202
lle240
mwww
NH
NH
Val263
ОН
www
HN
N-
lle177
HN
'N'
CI
3 X = N
4 X = C-CN
5 X = C-COO IC50 274 µM
IC50 140 nM
IC50 35 nM
NH2
HN
Val266
N
-N
O-H---- N
HN
%3D
Arg157
HN
wwww
lle265
Explain why structure 4 is a more potent inhibitor (lower IC50 value) than inhibitor 3 and why
structure 5 is a much weaker inhibitor (higher IC50 value) than 3 and 4.
Transcribed Image Text:A schematic representation of the enzyme IspD complexed to inhibitor 3, and a series of inhibitors 3-5 are shown below. Ala202 lle240 mwww NH NH Val263 ОН www HN N- lle177 HN 'N' CI 3 X = N 4 X = C-CN 5 X = C-COO IC50 274 µM IC50 140 nM IC50 35 nM NH2 HN Val266 N -N O-H---- N HN %3D Arg157 HN wwww lle265 Explain why structure 4 is a more potent inhibitor (lower IC50 value) than inhibitor 3 and why structure 5 is a much weaker inhibitor (higher IC50 value) than 3 and 4.
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