hi i want help

hi i want help
1- A Suggest an indication area for the two medicines A1 and B1, and write down whether one or both are prodrugs or not B Begge substansene inneholder et heterosyklisk aromatisk ring -element. Skriv opp navnet på denne ringen isolert uten substituenter C Go through the functional groups in A1 and B1 separately and count hydrogen bond acceptors / do nors. i) Suggest from that an approximate range for log P for the two substances. ii) In light of this, suggest approximate water solubility of the two substances at pH 7. iii) Write down whether the water solubility will vary with pH or not. D Briefly discuss whether A1 and B1 are optically active as they are drawn, and on that bas is determine the R / S of the two substances. The answer must be substantiated briefly. E This task must be answered with digital hand drawing. Briefly discuss whether there is an area in each of the molecules that can be called a “pharmacophor”, ie an area in the molecules that is necessary for the activity of the drug. If necessary, use a digital hand drawing of this product. F This task must be answered with digital hand drawing. The two drugs A1 and B1 are treated separately in a mixture of ethanol and 0.1 M HCl for 2 hours and heating to 50 oC. i. In one of the two solutions, e.g. one hydrolysis product with a molecular weight of 32 daltons and in th e other a hydrolysis product with a molecular weight of 60 daltons. Write down which hydrolysis products are and in which reaction with A1 or B1 they occur. ii. In the case where one of the hydrolysis products has a molecular weight of 60 daltons, the remaining substrate converts to a new product with a molecular weight of 331 daltons. Make a digital hand drawing of this product G Give a brief definition of what an amino acid is, and use this to determine if A1 or B1 or both can be defined as amino acid derivatives. The answer must be briefly substantiated 2- a. Suggest possible drug group for substances 2 -1 to 2 -3. Where relevant, the mode of action / target should be specified. (Ex: «Inhibitor of XX», «YY agonist»). The answers must be justified on the basis of the substances’ chemical structure and structural activity conditions where this has been taught. In some cases, it may be natural to specify a specific subgroup. Answer briefly. b. Are any of these potential drug substances a p otential prodrug? The answer must be briefly substantiated. c. One of these potential drug substances can be metabolized to a low molecular weight toxic substance. Explain briefly how such a metabolism occurs, what the substance looks like and why this me tabolite is toxic. d. Will it theoretically be possible to reduce the toxicity of this metabolite by providing an additional substance? Suggest a possible additional substance. e. One of the above substances will be a very chemical reactive and thus poss ibly unsuitable as a drug substance. What substance is this? Why is this unsuitable? f. How do you think the following changes of substance 2 -2 will affect the duration of action of the drug substance: * -O-CH3 – group replaced with a -OC H2CH3 group? * The olefin (C = C) is saturated to become a -CH 2 CH 2 – chain 3- The synthesis of a drug substance is shown in the figure (attached as pdf). Ac means acetyl. Use as many technical terms as possible to describe the reactions below. Each question must be answered very briefly. A What type of reaction takes place in the synthesis of (II) from (I)? B Which by -product is formed in the synthesis of (III)? C What type of r eaction is the synthesis from (III) to (V)? What additional products would you expect in the reaction? D What function does KHCO3 have in the reaction for the synthesis of (VII)? The reaction is better if small amounts of potassium iodide are added. What fun ction do you think potassium iodide has in this reaction? E What type of reaction is the synthesis step (s) for the formation of (X)? F What type of reaction is the last step? G Which reagent do you want to use to make the sodium salt of the drug substance? Whic h reagent do you want to use to make the chloride salt of the drug substance? H Will any of the intermediates in the synthesis be active within the same drug group as the drug substance synthesized here? State very briefly if you expect the substances listed to have the same clinical properties (effect, side effect) as the drug substance. 4- Suggest possible drug group for the possible potent substances 4 -1-A to 4 -1-I. This section deals with the substances as such and not metabolites. State very briefly why you might consider certain substances to be inactiv e. Suggest a probable active metabolite from an inactive substance in point a. Which of the substances 4 -1-A or 4 -1-D probably has the longest half -life? Must be justified very briefly. Which of the substances 4 -1-H or 4 -1-I probably has the longest half -life? Must be justified very briefly. Which of the substances 4 -1-H or 4 -1-I probably has the best clinical effect? Must be justified very briefly. Suggest the action and drug group for substance 4 -2. The answer must be briefly substantiated. 5- A Suggest a common indication area for the drug group represented by all four structures A5 – D5. B Write down the most basic nitrogen atom in A5, use the figure numbering in the answer C According to the SAR for this drug group, it is a requirement that one of the groups must have an acidic character. Writ e down which group in structure A5 can be said to be angry. The answer must be substantiated briefly D The numbering of the ring positions is the same in all three structures A5 – C5. Explain briefly using this numbering why A5 is called a chlorothiazide while C5 is called a hydrochlorothiazide. E This task must be answered with digital hand drawing. When B5 is treated with 0.1 M HCl for 2 hours with gentle heating, the product C5 plus another product X is formed. Make a digital hand drawing for the structure of this product X and attach it t o the answer to problem 5 e) F This task must be answered with digital hand drawing. When the substituent R2 in structure D5 has a gross formul a -C5H5O and contains a heterocyclic ring, structure D5 becomes one of the most widely used diuretic drugs on the market today. Make a digital hand drawing for the structure of this product and attach it to the answer to problem 5 f). Write down which med icine has the name of the active pharmaceutical substance. Write down the name of the heterocyclic substance in isolation without substituents. Write down whether this ring element is aromatic or not. Write down whether this medicine is a “loop” diuretic o r not. Write down whether the structures A5 – C5 represent “loop” diuretics or not G One of the medicines A5 – D5 can be used together with medicines for cardiovascular disease. Write down which of the structures A5 – D5 it applies to 6- This task must be answered with digital hand drawing. Suggest possible drug group for substance 6 -1. Enter biological attack point. Justify the answers very briefly. Will s ubstance 6 -1 be stable in acidic or alkaline aqueous solution? Draw the chemical structure of any decomposition products and show how these appear. Draw the chemical structure of possible metabolites that may appear from 6 -1. Show in the drawing how the se appear. The metabolites should have a molecular weight below 100 Daltons. In substance 6 -2, X may be oxygen, methylene (CH2) or sulfur. Suggest drug group for substance 6 -2 where X is oxygen. Substance 6 -2 where X is oxygen is a prodrug. Draw as d etailed a drawing as possible that shows how this substance can be converted into active substance. Will 6 -2 where X is methylene (CH2) or sulfur be potent within the same drug group? The answer must be briefly substantiated. 7- This task must be answered with digital hand drawing Potential drug substances have the formula 7 -1 Draw a drawing showing the S -configuration around the stereogenic / chiral atom where R4 is for substa nce 7 -1-C. What antibacterial properties do you think the different substances 7 -1-A to 7 -1-D could have? The answers must be briefly substantiated. Draw the chemical structure of as many probable metabolites as possible from substance 7 – 1-A where the metabolites do not contain nitrogen or sulfur. Indicate in the drawing how these appear. The active substance from substance 7 -1-B has a molecular weight of M. A probable metabolite of this substance has a molecular weight of M + 30. Draw the chemical structure of this metabolite and sketch how it appears. Do you think the metabolite in point d above has an antibacterial effect? Justify the answer. 8- This task must be answered with digital hand drawing. Substance 8 -1 has a molecular weight of M. A possible decomposition product in aqueous acid has a molecular weight of M plus 18. Draw a drawing showing how this decomposition product can be formed. Another possible contaminant in substance 8 -1 has the s ame molecular weight as 8 -1. This contaminant is not a lactam, is not an ether and does not have an alkene (C = C) group. Draw a drawing showing the chemical structure of this substance and how this pollution can be formed. Substance 8 -2 is a possible d rug substance. Suggest a possible behavior for substance 8 -2. Potential in vivo effect of substance 8 -2 involves binding to specific well -known proteins. Draw as detailed a drawing as possible that shows how the effect can be described using chemical bo nds. Draw a drawing showing how substance 2 -2 in problem 2 binds to the receptor