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Material Type: Exam; Professor: Gates; Class: Medicinal Chemistry; Subject: Chemistry; University: University of Missouri - Columbia; Term: Unknown 2007;
Typology: Exams
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A. = 1/K (^) D B. Any compound used to cure, mitigate, prevent, or diagnose a disease or physical malady C. Endogenous ligand for a receptor D. Strength varies as 1/r 6 (r = distance) E. = [D][R]/[D•R] F. Can provide a three-dimensional picture of a macromolecular drug target G. Strength varies as 1/r 2 (r = distance) H. Stable bond at room temp. Worth 85 kcal/mol I. Stable bond at room temp. Worth 8.5 kcal/mol J. Interaction of drug with its biological target K. Quantitative system to assay receptors L. Core set of functional groups required for biological activity within a structural group of molecules M. Often thermoneutral a vaccum N. Absorbtion, distribution, metabolism, excretion, and toxicity O. Favored by electron withdrawing groups P. Quantitative structure-activity relationship Q. Qualitative stereochemistry assessment ratio R. Strongest when bond angle is 180˚
O O
Cl Cl Cl CHN 2 O
N H
HN
O
O
CN
HN N
NH (^2)
NC NH
I NH
H 3 C NH
-0.4 0.2 0.
Activity = 1.1 Activity = 2.1 Activity = 3.
-0.2 0.0 0.
Log P Values From Leo, A.; Hansch, C.; Elkins, D. Chem Rev. 1971 , 71 , 525. Table courtesy of Prof. Richard B. Silverman Compound log Poct Compound log Poct Compound log Poct CH3OH -0.66 CH2=CHCOOH 0. O CH (^3)
CCl3COOH 1. H 3 C C CH (^3)
BrCH2COOH 0.41 CH2=CHCH2OH 0.17 CH3CH2CH2CH2OH 0. ClCH2COOH 0.47 CH3CH2CHO 0.38 CH3CH2OCH2CH3 0. FCH2COOH -0.12 CH3CO2Me 0.18 CH3CH2OCH2CH2OH -0. ICH2COOH 0.87 CH3CH2COOH 0.33 CH3CH2NHCH2CH3 0. CH3CN -0.34 CH3OCH2COOH -0.
N H
CH3CHO 0.43 CH3CH2CH2Br 2.10 CH3CH2CH2CH2CH2F 2. CH3COOH -0.17 CH3CH2CH2NO2 0.65 PhCH2OH 1. HOCH2COOH -1.11 CH3OCH2OCH3 0.00 PhCH2NH 1. CH3CH2Br 1.74 CH3OCH2CH2OH -0.
NH
CH3CH2Cl 1.54 Me3N 0.27 PhCH2COOH 1. CH3CH2I 2.00 CH3I 1.69 PhOCH2COOH 1. CH3CONH2 -1.46 CH3NO2 -0.33 2.
HN O NH
Me2NH -0.
NH
O
O
O
N H
-CH 2 - (x ) 0.50 -CH 3 (x ) 0. Branching -0.20 -H 2 C=CH-CH=CH 2 - (x ) "two thirds of benzene"
H 2 C=CH- (x ) "one third of benzene"