The following structures were introduced as neuromuscular blocking agents. Structure B is derived from structure A. What was the main reason for incorporating additional ester groups? O To enhance hydrogen bonding interactions with the binding site. O To increase the polarity of the drug. O To decrease the stability of the drug O To alter the conformation of the molecule.
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- From a medicinal chemistry (and a pharmacologist) perspective, functional groups provide specific properties and behaviors that allow drug molecules to exert their desired PD and PK effects. The key point here is that each individual group within a drug molecule can serve to provide one or more specific roles, tasks, or functions. The following table summarizes a series of drug discovery lead optimization for targeting a certain renal disease. Explain the basis for changing the R- functionality at the para- position. Please explain in as much detail as you need and by using scientific justifications, which one of the 4 candidates (526-529), presents the most viable investigational drug candidate, given the information provided below? N- `N' 'N' R- Drug Code R IC30 (nM) Half-Life (tı2), Minutes 526 CH;O 104 6 527 CF;0 1110 95 528 CH;CH, 11 <5 529 CH,CF, 14 96A Structure B was derived from structure A. What was the main reason for incorporating the two ester groups? To decrease the stability of the drug. Hobbyk B To enhance hydrogen bonding interactions with the binding site. To increase the polarity of the drug. To alter the conformation of the molecule.Tricyclic, anti-depressant drugs were developed from the observation that some tricyclic, anti-psychotic drugs elevated a patient’s mood. Identify the structural features of a tricyclic drug that were found to affect its action as a pure anti-depressant or a mixed anti-psychotic/anti-depressant agent and comment on the structural modifications that can be made to such an anti-depressant drug whilst retaining the essential pharmacophore.
- Prepare a schematic diagram and present it. The Figure should illustrate the interactions made between the key components of total and non-specific binding reactions in drug bindings. In preparing this figure, it should reflect on the role of each of the components of the reaction mixtures, and why the subtraction of non-specific from total binding allows us to calculate specific binding. The Figure Legend should be brief but informative.What is the possible drug interaction in the following structure of phenoxybenamine? .N.Which letter represents the target site of furosemide (Lasix)?
- A decapeptide which could resist burns was isolated from an endemic plant from Mt. Mayon. Deduce the amino acid sequence of the decapeptide given the following informations. Mercaptoethanol gave two pentapeptides F1 and F2. Chymotrypsin treatment of F1 releases S and a tetrapeptide (C,K,F,M) while F2 gave a dipeptide (M,S) and a tripeptide (C,F,K) F1 when treated with CNBr released a free homoserine lactone and a tetrapeptide. Trypsin treatment of F1 gave a tripeptide and a dipeptide. F2 treated with carboxypeptidase released free M while with trypsin gave free K and a tetrapeptide.(1) Discuss the structure and function of ion channels and describe their importance in medicinal chemistry. (ii) Draw the molecular structure of tamoxifen and discuss, in detail, its mode of therapeutic activity. Use the protein databank (PDB entry: 3ERT) to help support your answer.What is the significance of the blue regions of the following molecule? Me Me Me H oppo Me steroid skeleton O Me Me None of the answers O They are prone to metabolism, thus limiting the lifetime of the drug O They introduce a dipole moment to the molecule allowing the correct alignment of binding groups when the molecule binds to the binding site O They represent the skeleton of acetylcholine O They are polar groups that increase water solubility
- Considering the general structure of penicillins, how are they rendered ineffective? Select one: O a B-Lactamase performs nucleophilic attack of the amide in the penicillin side chain Ob. B-Lactamase performs nucleophilic attack of the amide in the B-lactam ring and subsequently hydrolyzes this intermediate OC. B-Lactamase performs nucleophilic attack of the thiazolidone ring on the carbon next to the electronegative sulfur leading to a covalently inhibited B-Lactamase o d. All of these O e. None of theseb) Consider the following experimental results: Total hydrolysis of a nonapeptide gave: Ala,Arg, Glu,Leu,Lys,Met,Phe,Tyr,Val One fragment from CNBR treatment was: Tyr-Leu-Lys One fragment from Chymotrypsin treatment was Arg-Glu-Met-Tyr One fragment from Trypsin treatment was Val-Ala-Phe-Arg i. Deduce, with suitable explanations, the amino acid sequence of the nonapeptide.b) Consider the following experimental results: Total hydrolysis of a nonapeptide gave: Ala,Arg,Glu,Leu,Lys,Met,Phe,Tyr, Val One fragment from CNBr treatment was: Tyr-Leu-Lys One fragment from Chymotrypsin treatment was Arg-Glu-Met-Tyr One fragment from Trypsin treatment was Val-Ala-Phe-Arg ii. The reagent shown below is widely utilized in the sequencing of peptides. Treatment of the nonapeptide you deduced in part i. with this reagent yields a phenylthiohydantoin derivative, compound 1, and an octapeptide. Write a mechanism for the formation of compound 1. N=c=8
