(d) Compare the structure of the ẞ-lactam antibiotic shown in Figure Q10(d) with that shown in Figure Q10(a) in terms of how it affects the following properties; (i) Spectrum of activity. (ii) Resistance to ẞ-Lactamases. (iii) Oral bioavailability. H3C -NHH COOH (3 marks) (3 marks) (3 marks)
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- (a) What is the difference between the hormones progesterone and testosterone? (b) Draw the structure of a a steroid nucleus. (c) Give the products obtained from complete base hydrolysis in the following reaction: O || CH,−O−C−(CH2)14–CH3 O CH–0–C−(CH2)14—CH3 + 3 NaOH O CH,−0–C−(CH2)14–CH32. 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.Explain the following terms with one suitable example for each :(i) A sweetening agent for diabetic patients(ii) Enzymes(iii) Analgesics
- Explain the following terms with one suitable example for each: (i) A sweetening agent for diabetic person (ii) Enzymes (iii) AnalgesicsTrypsin is a serine protease that has a KM of 15 mM. At an initial substrate concentration of 250 µM insulin, trypsin is found to degrade insulin at a rate of 0.6 µM/min. If the concentration of trypsin in solution was 4.326 µM, what is the kcat of trypsin in s-1?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.
- Raloxifene is a drug used in the treatment of osteoporosis in postmenopausal women and those on glucocorticoids. In a study conducted by Izgelov et al. (2018), the two metabolites derived from raloxifene are shown and their intestinal metabolism are discussed. он Raloxifene 6-Glucuronide HO Raloxifene onge HQ. OH OH OH Raloxifene 4'-Glucuronide Determine the isomer configuration of the labelled double bond (shown in red) from the structure of raloxifene by writing the letter of the configuration in the provided box below. STRICTLY write the letter only.Which of the following bases are strong enough to deprotonate C6H5OH(pKa = 10) so that equilibrium favors the products:(a) H2O; (b) NaOH; (c) NaNH2; (d) CH3NH2; (e) NaHCO3; (f) NaSH; (g)NaH?Assume the following two molecules exhibit identical bioactivity and pharmacokinetics. In considering which to promote to lead status in a drug discovery program, which would be the more desirable choice? S bag O Compound B Compound A A NHMe B S N Me ΝΗ
- AH = - 1.2 kcal/mol; Kp = 16 nM OH 1 HO AH = - 6.0 kcal/mol; N. Kp = = 76 nM OH 2 HOl. AH = - 5.5 kcal/mol; Kp = 0.5 nM OH (iii) By considering the enthalpies given, what do you think this suggests about the target (e.g. the binding pocket of an enzyme) that the molecule binds to?Below is the structure of eicosapentaenoic acid (EPA) which is an omega-3 fatty acid. What would be the IUPAC (International Union of Pure and Applied Chemistry) designation (the nomenclature emphasized in lecture) for EPA? omega-3 20:4 (A5,8,11,14) 20:5 (43,6,9,12,15) 20:0 20:5 (A5,8,11,14,17) ◄ Previous Il app.honorlock.com is sharing your screen. Stop sharing Hide Your Webcam2. 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 ОН