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- The addition of a nucleophilic group like a thiol (-SH), or an unprotonated amino group (-NH₂) to an a,ß-unsaturated ketone is important for understanding how NAPQI reacts with glutathione, N-acetylcysteine, or protein amino acid side chains containing -SH or -NH2 groups. In this problem we will add mercaptoethanol to p-benzoquinone. p-Benzoquinone will be a simple model of NAPQI. +H H a single uncharged addition product This reaction will proceed in steps. First the H-S-R will add to the unsaturated ketone to give a charged addition product. Next, a simple proton transfer will form an uncharged adduct in which the 6-membered ring contains one carbonyl and a second enolic hydroxyl. The keto form next will tautomerize to its more stable enol form, and in doing so the 6-membered ring becomes aromatic with 6-π electrons. See page 14 of the lecture notes for Lecture 9 How ADME affects preclinical Drug Design February 24, 2023, where I have shown the mechanism for this addition and give the…During acidosis of a protein, shown below, salt bridges are broken, resulting in denaturation. Which choice shows the products of alkalosis?are involved in the regulation of glucose metabolism and in control tissue swelling by the control of inflammation, while regulating cellular salt balance between Na+ and K+. a.glucocorticoids, mineralocorticoids b. mineralocorticoids, glucocorticoids c. androgen, estrogen d. estrogen, androgen Which of the following represents an aldonic acid? OH OH но, но OH но —н но Но HO HO H но но H H- -OH -OH H OH H FOH H- -OH- OH HO но HO. OH II III IV V Refer to the structures. Which of the following compounds will react with acetyl chloride to give an amide and ester, respectively? NH2 ÇOOH CH3 он CHO II II IV V The six groups of enzymes are the following: I. Oxidoreductases II. Transferases III. Hydrolases IV. Isomerases V. Lyases VI. Ligases Fill in the blanks: catalyze hydrolysis while catalyze bond formation.
- The following three derivatives of succinimide are anticonvulsants and have found use in the treatment of epilepsy, particularly petit mal seizures. Ph Ph `N' `N' ČH3 ČH3 Methsuximide Ethosuximide Phensuximide Following is a synthesis of phensuximide. CN Ph CN Ph CN 1. NaOH, H2O 2. HC, Н20 NaOEt KCN Ph-CHO cOOEt H cOOEt NC COOEt 3. Нeat Ethyl cyanoacetate (A) (B) Benzaldehyde Ph Ph Ph CH;NH2 НООС СООН Et0oC COOEt `N' (C) (D) ČH3 Phensuximide Methsuximide is formed by a similar pathway to that shown for phensuximide. Draw the structure of the compound that reacts with ethyl cyanoacetate in the synthesis of methsuximide.A) The biotransformation of this drug: Choose all that apply. CH3 CH3 OH H,C он он HO H,C. Phase I Phase II Reductive reaction Oxidative reaction Hydrolysis reaction glucuronic acid conjugation sulfate conjugation O methylation O acetylation product becomes less water soluble Porducts become more water soluble excretion of the products mostly happens in kidney excretion of the product mostly happens in feces B) What is the enzyme and coenzyme/cosubsrate ?The following three derivatives of succinimide are anticonvulsants and have found use in the treatment of epilepsy, particularly petit mal seizures. Ph. Ph `N' ČH3 ČH3 Methsuximide Ethosuximide Phensuximide Following is a synthesis of phensuximide. CN Ph CN Ph CN NaOEt KCN 1. NaOH, H2O Ph-CHO 2. HС, Н20 COOET H cOOEt NC COOEt 3. Нeat Ethyl cyanoacetate (A) (B) Benzaldehyde Ph. Ph Ph CH3NH2 НООС СООН EtOOC COOET `N' (C) (D) ČH3 Phensuximide In the conversion of (B) to (C), draw the structure of the product of step 1.
- 27) Hydrolysis of an ester: O II CH,-C-O-CH2-CH2-CH, + H20 28) Acid/ Base reaction of an amine CH3-CH2-NH2 H2CO3 29) Hydrolysis of an amide 11 CH3-CH2-CH2-CH2-CH2-C-NH-CH2-CH2-CH, + H20 OMIC Moleculesamidase NH2 HO, NH K ta Cadangkan kaedah vang cecuai.untuk uian onzim amidase るidentify which has the lowest pka value. use aromatcity concepts to explain why.
- 1. Biogenic Amines are inactivated primarily by a. Sulfonation b. Glucoronidation c. Aromatic hydroxylation d. Methylation 2. A drug can exert its pharmacological effect only if it is a. Protein bound b. Protein unbound c. Free drug d. Both B & C e. Both A & C 3. In order for the drug to be ready and available for absorption, it must be release first from its dosage form with the exception of: a. Capsule b. Tablet c. Solution d. Suspension 4. All of the following are true, except a. Solubility increase with decrease particle size b. Solubility increase with increase surface area c. Solubility increase with increase particle size d. Solubility decrease with decrease surface area 5. The rate in which the drug appears in the bloodstream is also known as a. Half-life b. Potency c. Bioavailability d. Area under the curveWhich of the following substituent is an ortho/para-directing activator and an ortho/para-directing deactivator? a amino group b halogen group c nitro group d carboxyl groupWhat product will result from the reaction shown? CHO amino alcohol amino acid imine CH3CH₂CH₂CH₂NH₂ enamine hydroxylamine H, A