Term
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Definition
| Absorption, Distribution, Metabolism, Excretion, Toxicity |
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Term
| Structure-activity relationship (SAR) |
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Definition
| Modifying the effect of bioactive compounds to test their effect |
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Term
Stronger Bond =
Weaker Bond = |
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Definition
| Longer time in binding -> Inc. Duration of action |
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Term
| Strongest intermolecular bonds |
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Definition
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Term
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Definition
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Term
| Van der waals occur between ____ regions |
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Definition
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Term
| Dipole-Dipole vs Ion-Dipole |
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Definition
Dipole-dipole is partial charge attracted to partial charge.
Ion-dipole is charge attracted to a partial charge. |
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Term
| Induced dipole movement occurs in |
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Definition
| Aromatic rings (with quatenary ammonium ion) |
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Term
| Alkanes is capable of what type of bonding? |
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Definition
| Only van der waal (immisscible in water) |
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Term
| Alkane chemically stable in vivo vs in vitro |
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Definition
In vivo - Usually stable
In vitro - Usually stable |
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Term
Alkane's solubility with
a) water
b) nonpolar |
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Definition
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Term
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Definition
In vivo - stable
In vitro - prone to oxidation --> peroxidation |
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Term
Alkene soluble in
a) water
b) non polar? |
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Definition
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Term
| Hydration, epoxidation, peroxidation, reduction |
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Definition
Hydration -Addition of water to double bond
Epoxidation - removal of DB to form epox
Peroxidation-removal of DB to form O-O
Reduction - Removal of double bond C-C |
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Term
Cycloalkanes
Characteristic
Stability in vitro/vivo
Solubility in polar/nonpolar |
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Definition
a) flammable
b) stable and inert
c) Lipophilic, hydrophobic |
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Term
Aromatic Hydrocarbon
1. Name them
2. Characteristic
3. Form peroxide even though DB?
4. Metabolism?
5. Solubility
5. |
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Definition
1. Benzene, naphthalene, antrhacene, phenanthrene
2. Flammable
3. No
4. Aromatic hydroxylation
5. van der waal (not water soluble) |
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Term
| Metabolism of aromatic hydrocarbons |
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Definition
1. Hydroxylation -OH
2. conjugation -OSH3 or Glucuronide conjugate |
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Term
Halogens
1. Bond interaction
2. Solubility
3. Increase in Haolgens =?
4. In vitro/ In vivo
5. Effect on halflife |
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Definition
1. Van der waal
2. Lipophilic, poor solubility in water
3. Less flammable, more lipophilic, more toxic
4. Stable in both, but hard to get rid of in the body because lipophillic and thus increase toxicity.
5. Increases half life |
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Term
Alcohol
1. Bond Interaction
2. Solubility
3. In vivo / in vitro |
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Definition
1. Hydrogen, permanent dipole
2. Water soluble
3. Primary ->aldehyde -> acetic acid
2ndary -> ketone
Tertiary stable in vivo
In Vitro - Stable |
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Term
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Definition
1. Metabolized by P450 abdAlcohol dehydrogenase. Primary -> aldehyde -> acetic acid
2. Conjugation |
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Term
Phenol
1. Acidity vs cyclohexanol
2. Bonding
3. Na + K increase/decrease solubility
4. Heavy metal +/- solubility
5. Treating phenol salt with acid will |
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Definition
1. Mildly acidic, cyclohex = neutral
2. H bonds IN ADDITION to ion-dipole
3. Increase
4. Decrease
5. regenerate phenol |
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Term
| Stability of phenol in vitro |
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Definition
| Exposure to oxygen will form quinones (highly colored( |
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Term
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Definition
And phases
1. Hydroxylation (as with all aromatic)
2. Oxidized
3. Conjugation (name the 2?)
4. methylation |
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Term
Ethers
1. Solubility
2. In vitro/vivo
3. |
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Definition
1. poor water solubility
2. Vitro - peroxide forms
Vivo - stable |
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Term
Aldehydes + Ketones
1. Solubility
2. Vitro/Vivo |
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Definition
1. Water soluble (POLAR)
2. Vitro - Ketone Stable where as aldehyde is not (reacts with 02 to acid)
3. |
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Term
Aldehyde/Keton +Alcohol with acid =
Ketals/Acetals + acidic pH = |
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Definition
Hemiacetal/hemiketal + alcohol -> acetal/ketal
Convert back to ketones/aldehyde |
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Term
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Definition
1. oxidation (mostly)
2. sometimes reduction to alcohol |
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Term
Amines
1. Roles (2)
2. Strength of H bond vs O
3. Solubilty of primary, secondary, tert
4. EDG vs EWG and effect on amines |
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Definition
1. Solubilize the drug to free base or water soluble salt of amine
2. Weaker
3. Prim > Sec > Tert
4. EDG +basicity - acidity
EWG +acidity - basicity |
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