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
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
Chapter10: Reconstitution Of Powdered Drugs
Section: Chapter Questions
Problem 7.2P
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