A series of novel phenadoxone derivatives without mu2 receptor activity (mu2 activity is responsible for physical dependence) proposed to be developed as analgesics is shown below. Addition of which heterocyclic substituent R to phenadoxone is LIKELY to cause the MOST binding of the corresponding derivative to plasma proteins? Use the additivity of approximate estimates of logP to answer this question. phenadoxone derivatives R= A. Azetidine B. Thiophene C. Oxetane D. Furan E. Pyrrole -NH
A series of novel phenadoxone derivatives without mu2 receptor activity (mu2 activity is responsible for physical dependence) proposed to be developed as analgesics is shown below. Addition of which heterocyclic substituent R to phenadoxone is LIKELY to cause the MOST binding of the corresponding derivative to plasma proteins? Use the additivity of approximate estimates of logP to answer this question. phenadoxone derivatives R= A. Azetidine B. Thiophene C. Oxetane D. Furan E. Pyrrole -NH
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Step 1: Introduction:
In the quest for developing novel analgesics, researchers are exploring various chemical modifications to existing compounds to enhance their effectiveness. In this context, a series of phenadoxone derivatives has been proposed, with the objective of minimizing physical dependence, which is typically associated with mu2 receptor activity. One critical aspect to consider in drug development is the binding of these derivatives to plasma proteins, as it can impact their pharmacokinetics and therapeutic potential. To address this concern, we will evaluate the impact of different heterocyclic substituents on the likelihood of binding to plasma proteins, using approximate estimates of logP values.
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