1) The following compounds all belong to the same broad class of antibacterial drugs. Rank them in orderfrom most potent (1) to least potent (3) based on their intrinsic activity at enzyme inhibition (e. g. , an invitro assay). Explaining your reasoning is an important part of getting full credit. 2) A patient with a bacterial infection was treated with penicillin derivative D, (shown below) but theinfection persisted. When treated with a combination of D and E, the infection was cured, although E byitself was inactive. Can you explain why this occurred and suggest a single penicillin drug that would beeffective for treating this specific infection?3) Compound F is a potent and non-selective -agonist called isoproterenol. A similar compound with asingle meta-hydroxy group and replacement of the N-isopropyl with a methyl group gives a drug (G) withonly 1 agonist activity and no activity. If the pattern of hydroxy groups is switched from 1,2 inisoproterenol to 1,3, compound H is prepared. H has selective 2 agonist activity and when dosed inhumans, has a much longer duration of action. Please be very specific in your answers to the followingquestions: a) What are two reasons why G does not have activity?b) Why does adding another meta-hydroxy group (H) return activity?c) Why does H have a longer duration of action?4) Describe each of the follow compounds as having the potential to act as either, 1) non-selective antagonist, 2) short acting -antagonist, 3) 2-agonist or 4) long acting -antagonist. Do not wastetime looking these compounds up (I made them up), I want you to use your knowledge of the subject tomake the determination. 5) The compound shown below has almost no activity when tested in an in vitro assay. When dosed inhumans, many find it to be an excellent pain reliever while others find it to be ineffective. What’s going, bevery specific with your explanation including any analogous compounds you may wish to compare thiswith?6) Congratulations on your fine work as a medicinal chemist at the ACME Pharmaceutical Company! Yourwork in the hypotension group (lowering blood pressure) has come up with a great new drug candidateshown below: While this compound was efficacious in lowering blood pressure in clinical trials, it was seen that inpatients that had infections and were treated with sulfmethoxazole, the infection persisted. On the otherhand, those infected patients treated with penicillins were cured from the infection. Please explain. 7) Based on your knowledge of the different classes of drugs we have studied in the second half of thisclass, please answer the following questions based on the structure shown below. This drug has very littlemetabolism and is excreted mostly as the molecule shown. a) What class or type of drugs would you most associate this drug with? What features lead you to thisconclusion?b) What part of the body would this drug not be effective in? Why?c) What clinical indication might this drug be prescribed for? Why?8) Your success at ACME is known throughout the company and your supervisor places you on a leaddiscovery program. The aim of this project is to identify a potent (IC 50 <,<, 1 M) and reversible inhibitor ofa particular enzyme. You have a discussion with your friendly biochemist also on the project and togetheryou decide to set up a screen to look for fragments. The project churns along and after screening ACME’sfragment file, the following compounds and their corresponding activities are identified: CompoundIC5023 M1,120 M525 MCompoundIC50150 M1. 2 M67 MAll of these compounds are believed to bind in the active site of the enzyme. Be specific in explaining astrategy to move forward including a compound to prepare (you don’t need to synthesize it). 9) You’ve been so successful at ACME that you have been moved to the antibacterial program with thehope that you can provide a winner there as well. In your first project looking at an SAR program aroundthe cephalosporin Cefuroxime, you prepare the compound shown below. Your biologist calls you screaming with great news, in the in vitro assay, this compound is over 100 timesmore active than the Cefuroxime standard. “Of course” you reply, I planned this happen. Please explainthis to your biologist. 10) Please rank the following drugs for their analgesic activity when dosed in an IV formulation. 1=mostactive and 4=least active. Explain your reasoning.