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- 2. Flavopiridol was the first semi-synthetic cyclin-dependent kinase inhibitor to be tested in clinical trials. Research has shown that co-administration of flavopiridol with drugs such as the taxanes had synergistic cytotoxic effects against a variety of tumour cells. HO но, HO O 1114 CI 2.1 Is flavopiridol a natural product? Explain your answer.Q1. Eticlopride is a dopamine antagonist, which can block dopamine receptor sites and influence levels of dopamine. The molecule is involved in a number of intermolecular interactions with amino acids in the G protein-coupled receptor. о но ČI Eticlopride i) Draw a suitable diagram to indicate where the following amino acids might interact with the molecule: phenylalanine; valine; histidine; tyrosine. In your answer, please draw the amino acids and show the interaction. ii) For each interaction you have shown, state the nature of that interaction (e.g. H- bonding, pi-pi etc.)3a. 3b. 3c 3d. 3e. CO₂ clavulanic acid CH₂-OH H Answer the following questions about clavulanic acid. Does clavulanic acid inhibit D-alanyl-D-alanine transpeptidase? Does clavulanic acid contain a ß-lactam? Does clavulanic acid contain a thiazolium ring? What is the result of the treatment of penicillinase with clavulanic acid? Does clavulanic acid form a covalent acyl-enzyme intermediate with penicillinase?
- 4 How does aqueous Silver nitrate, AGNO3, works against neonatal conjunctivitis (inflammation of the outer eye) due to neonatal bacterial infection? It hydrolyzes protein in bacteria to amino acids and inactivate it. O It denatures the protein bacteria and kills them. It mutates the genetic make-up of bacteria and transforms them to useful proteins. It oxidizes side chains of cysteine residues to cystine.1. The antibacterial activity of flavonoids was tested against the bacterial strain, Escherichia coli. The minimum inhibitory concentration at which 50% of the compounds were inhibited (MIC50) are presented in the table below for some of the compounds. Table 1: Antibacterial activity of flavonoids tested against E. coli Compound Kaempferol Quercetin Compound X Luteolin Tangeritin 5,6,7,4'- Tetramethoxyflavone Genistin Genistein MIC50 (μg/mL) 25.50 35.76 36.72 67.25 137.10 156.34 238.94 320.88 1.1 What subgroups of flavonoids do these belong to.1. The antibacterial activity of flavonoids was tested against the bacterial strain, Escherichia coli. The minimum inhibitory concentration at which 50% of the compounds were inhibited (MIC50) are presented in the table below for some of the compounds. Table 1: Antibacterial activity of flavonoids tested against E. coli Compound Kaempferol Quercetin Compound X Luteolin Tangeritin 5,6,7,4'- Tetramethoxyflavone Genistin Genistein MIC50 (µg/mL) 25.50 35.76 36.72 67.25 137.10 156.34 238.94 320.88 1.3 Would myricetin have higher or lower antibacterial activity compared to quercetin? Justify your answer by using the results provided.
- 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 curve2. How might the compound shown below work as a mechanism-based inhibitor of phosphoglucomutase? Use structural drawings to explain your answer. CI s=0 OH НО ОНOther Guide Questions: 1. How is turnover number of an enzyme related to Vmax? 2. How can competitive and non-competitive inhibition be distinguished in terms of Km ? 3. Distinguish between the molecular mechanisms of competitive and non-competitive inhibition. 4. Why is a Lineweaver-Burk Plot useful in analyzing kinetic data from enzymatic reactions ? 5. What properties of metal ions make them useful cofactors? 6. Why necessary or advantageous for the body to make zymogens? 7. Briefly describe the role of nucleophilic catalysis in the mechanism of the chymotrypsin reaction. 8. Please make a derivation of the Michaelis-Menten equation.
- Provide an electron pushing mechanism for the conversion shown below. Abbreviate the enzyme catalyst active site groups (BH* and B:) as needed. Which purine base is used? NH₂ Enz H₂O 'N NHX 10 (select) v molecules of penicillinDescribe how the following function as drugs: (a) AZT (b) cisplatin (c) daunomycin