By John G. Topliss (Eds.)
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Extra resources for Quantitative Structure–Activity Relationships of Drugs
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The equa tion is not very sharp and clearly reflects both the enormous diversity of the considered structures and the lack of sensitivity of a bacterial culture to molecular modification compared with an enzyme assay. Diagnostically it only provides a very crude picture of the receptor, as in Scheme 3. Amino preferred H y d r o p h o b i c i n t e r a c t i o n and Scheme 3. Reversible inhibition of L. casei (26). Although direct information about the receptor is crude, Eq. (27) is helpful in two ways.
18). Those compounds were relatively strong acids, having pK values such that they are more than 90% ionized at the pH of the test. 051 The equation provides good evidence that permeation of the bacterial cell is not rate limiting, except for the most acidic sulfonamides. This justifies the view of Cowles that ionized sulfonamides do not easily penetrate the cell. b. Correlations of MIC with Physicochemical Constants. Pro vided that strongly acidic members are excluded, essentially linear corre lations can be found with electronic parameters such as pK , σ, or N M R shift in sulfonamides of types XV and XVI (52,118).
31 The negative coefficient in R denotes that electron release is beneficial. The behavior is entirely analogous to that of sulfonamides, and the equa tion is thus diagnostic of competitive inhibition of dihydropteroate glutamate + A T P (Dihydrofolate synthase) Ο HN H N 2 A Ν. Τ CH NH CONHCH(C0 H)CH CH C0 H 2 2 2 Ν Η NADPH + H (Dihydrofolate reductase) + HN H N 2 S c h e m e 2. Final stages in tetrahydrofolic acid biosynthesis. 2 2 46 Μ. S. Tute synthase and charge derealization from the substituent to the S 0 group thus enhances activity.