From a medicinal chemistry (and a pharmacologist) perspective, functional groups provide specific properties and behaviors that allow drug molecules to exert their desired PD and PK effects. The key point here is that each individual group within a drug molecule can serve to provide one or more specific roles, tasks, or functions. The following table summarizes a series of drug discovery lead optimization for targeting a certain renal disease. Explain the basis for changing the R- functionality at the para- position. Please explain in as much detail as you need and by using scientific justifications, which one of the 4 candidates (526-529), presents the most viable investigational drug candidate, given the information provided below? `N' `N' R- Drug Code R IC50 (nM) Half-Life (t12), Minutes 526 CH;0 104 6 CF,0 CH;CH, 527 1110 95 528 11 <5 529 CH;CF, 14 96

Phlebotomy Essentials
6th Edition
ISBN:9781451194524
Author:Ruth McCall, Cathee M. Tankersley MT(ASCP)
Publisher:Ruth McCall, Cathee M. Tankersley MT(ASCP)
Chapter1: Phlebotomy: Past And Present And The Healthcare Setting
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From a medicinal chemistry (and a pharmacologist) perspective, functional groups provide
specific properties and behaviors that allow drug molecules to exert their desired PD and PK
effects. The key point here is that each individual group within a drug molecule can serve to
provide one or more specific roles, tasks, or functions. The following table summarizes a series
of drug discovery lead optimization for targeting a certain renal disease. Explain the basis for
changing the R- functionality at the para- position. Please explain in as much detail as you need
and by using scientific justifications, which one of the 4 candidates (526-529), presents the most
viable investigational drug candidate, given the information provided below?
N-
`N'
'N'
R-
Drug Code
R
IC30 (nM)
Half-Life (tı2), Minutes
526
CH;O
104
6
527
CF;0
1110
95
528
CH;CH,
11
<5
529
CH,CF,
14
96
Transcribed Image Text:From a medicinal chemistry (and a pharmacologist) perspective, functional groups provide specific properties and behaviors that allow drug molecules to exert their desired PD and PK effects. The key point here is that each individual group within a drug molecule can serve to provide one or more specific roles, tasks, or functions. The following table summarizes a series of drug discovery lead optimization for targeting a certain renal disease. Explain the basis for changing the R- functionality at the para- position. Please explain in as much detail as you need and by using scientific justifications, which one of the 4 candidates (526-529), presents the most viable investigational drug candidate, given the information provided below? N- `N' 'N' R- Drug Code R IC30 (nM) Half-Life (tı2), Minutes 526 CH;O 104 6 527 CF;0 1110 95 528 CH;CH, 11 <5 529 CH,CF, 14 96
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