You know it’s an angiotensin converting enzyme inhibitor use any treatment of hypertension diabetes neuropathy and some types of chronic heart failure it prevents the conversion of the peptide hormone in detention one the intention to impugn swells so constriction which causes an increase in blood pressure in our place the first member of the group known as dicarboxylic
Containing is anita it’s on wh os list of essential medicine and he saw the most important medication needed in a basic health system in a repair has been proven to protect the function of the kidneys in hypertension heartily and remedies in an apprentice pregnancy category d there is evidence that suggests another pair will cause injury and death to a developing
Fetus pregnant women are not advice to take this medication enalapril is secreted embracement and not recommended for use while breastfeeding the most common side effect of enalopril include increase in serum cretinous dizziness low blood pressure and dry cough the most serious side effect is ngo edema that often affect the face and lips which endangering the
Patient’s airways ngo edema can occur at any point during treatment with enalopril but kamandi occur after the first few doses secretly developed the first inhibitor kept apace but it had adverse effects such as metallic taste this is the structure of this drug it consists of two carboxylic acid groups on this side the carboxylate ion binds to charged nitrogen of
Amino acid in binding site while at the other side the carboxylic group make direct interaction with catalytic seeing ion it also consists of carbonyl group that form straight hydrogen bonds in ac a binding site while on the site secondary amine contribute to the molecule slowly populous city and for oral availability characteristic fin a little group here we mix
The hydrophobic side chain of phenol amino in angiotensin wine while methyl group here mimics the side chain of alanine and it react with hydrophobic first one the row leading ring also part of this structure carboxylic acid carbon ooh a mine and benzene in the body of another cream is hydrolyzed extensively to anela pretty primarily by nearest races and excreted
And change ionization of the adjacent reversely in enalapril a greatly enhanced the basicity of the secondary amine such as the pka of the amine in this compound is seven point eight three whereas in another plane it is only five point two plus in small interesting the end in another pilot will be primarily ionized and from a veteran with edges in carboxylate but
The eminent enalapril will be primarily enalapril an inhibitor which have to iron escobar silly groups in enalapril a one of the carboxylic group is involved in the chelation mr. chile think abou silly oxygens may direct coordination to zinc penta coordinated geometry they appeared to my meat the nucleophilic water in the carboxyl oxygen of the substrate in the
Tetrahedral intermediates during enzymatic reaction where the other one internet we are dreaming group or other amino acid the phenyl is the side chain from hydrophobic interaction with s1 sub site of the enzyme while the metal feet to s1 pocket and increase the binding affinity of the drug the carbonyl group also form hydrogen we angiotensin-converting enzyme
Binding site this is how the carpet inside she looked like from 3d view data structure can be view for our 3d views and you can and pocket the trap or temperature also can be view for map of leaky important interaction using a software which is can sketch the treasure of enalopril a before and after minimization can we design the minimization also can be obtained
Using 3d structures which are thick string emboss and space field structure region bonus after inheriting bond owner of another pilot hpa is a heron receptor which is the electron negative vector it provides in actual reach at them to receive the hydrogen bond svd is a hydrogen bond donor that provides a hydrogen for hydrogen bonding based on the structure of
Another pilot there are six hydrogen bond acceptor and three hydrogen bond donor based on a henderson has publication ph is equal to pka plus an extra over and iron extra from a drunk bank we know that the pka of a strongest acid it is three point one three whereas for the from the space it is seven point eight four by substituting the value of ph and pk into the
Henderson-hasselbalch equation the percentage ionization of strongest acd is 99.99% whereas for the strongest base e is seventy two point nine one percent so we can conclude that nl aprilia is soluble in both acidic and basic we can predict the solubility of enalopril act by using lemke’s formula nl aprilia is a poly functional molecule we know that the total number
Of carbons in it is eighteen carbons so by calculating the carbon solubilizing potential of each functional group we conclude that the drug is water in solid by looking at the physical chemical parameters and then the period fulfill the pinsky’s rule of five it’s supposed to be orally active however it has a lower abaya availability because the ionization of adjacent
Carboxylic in analog that quickly increases the basicity of secondary amine therefore in the small intestine the amine in another pilot will be primary ionized – from tjuta ion with the adjacent epoxy li the formation of jitter ions lowers the rl activity of an elaborate this explains why another pilot has a low or a bio availability enalapril is a completing prodrome
Which hydrolyzed into enalopril by carboxy asterisk enzyme enalapril a was developed partly to overcome the limitation of captopril the sulphide real moiety was replaced by carboxylate my team however there are additional modification that can be made which require in its structure base design to achieve a similar potency to captopril enalapril i however had a
Problem on its own the consequence of the structural modification may have in favorable ionization characteristics to allow sufficient potency for oral administration
Transcribed from video
far 212 group 8 : enalapril By Shakirah Rosli
