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The Lipinski’s rules indicate poor absorption when:   The molecular weight is > 500 Da The number of hydrogen-bond donors is greater than 5. The number of hydrogen-bond acceptors is greater than 10. The partition coefficient [measured as log(P) = log10 {[drug] n-octanol / [drug] water}] is greater than 5.   27.A. Indicate whether or not the molecule shown below (fluconazole) follows the Lipinski’s rules. Analyze each rule one by one, indicating which are the hydrogen-bond donors and hydrogen-bond acceptors and calculate log (P). According to your analysis, will fluconazole have good or bad absorption. MW = 306.271 g/mol  Solubility in water = 1 mg /ml  Solubility in octanol > 60 mg/ml

The Lipinski’s rules indicate poor absorption when:   The molecular weight is > 500 Da The number of hydrogen-bond donors is greater than 5. The number of hydrogen-bond acceptors is greater than 10. The partition coefficient [measured as log(P) = log10 {[drug] n-octanol / [drug] water}] is greater than 5.   27.A. Indicate whether or not the molecule shown below (fluconazole) follows the Lipinski’s rules. Analyze each rule one by one, indicating which are the hydrogen-bond donors and hydrogen-bond acceptors and calculate log (P). According to your analysis, will fluconazole have good or bad absorption. MW = 306.271 g/mol  Solubility in water = 1 mg /ml  Solubility in octanol > 60 mg/ml

Chemistry
Chemistry
10th Edition
ISBN:9781305957404
Author:Steven S. Zumdahl, Susan A. Zumdahl, Donald J. DeCoste
Publisher:Steven S. Zumdahl, Susan A. Zumdahl, Donald J. DeCoste
Chapter1: Chemical Foundations
Section: Chapter Questions
Problem 1RQ: Define and explain the differences between the following terms. a. law and theory b. theory and...
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The Lipinski’s rules indicate poor absorption when:

 

  • The molecular weight is > 500 Da
  • The number of hydrogen-bond donors is greater than 5.
  • The number of hydrogen-bond acceptors is greater than 10.
  • The partition coefficient [measured as log(P) = log10 {[drug] n-octanol / [drug] water}] is greater than 5.

 

27.A. Indicate whether or not the molecule shown below (fluconazole) follows the Lipinski’s rules. Analyze each rule one by one, indicating which are the hydrogen-bond donors and hydrogen-bond acceptors and calculate log (P). According to your analysis, will fluconazole have good or bad absorption.

MW = 306.271 g/mol

 Solubility in water = 1 mg /ml

 Solubility in octanol > 60 mg/ml

 

N= F Fluconazole e
Transcribed Image Text:N= F Fluconazole e
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