This video includes mechanism of action, chemistry and SAR of various Proton Pump Inhibitors (PPIs). It is very Useful for Final Year B.Pharm /GPAT/NIPER/GATE/M.Pharm Students.
Hello everyone welcome to my youtube channel chemical rama myself my ashram assistant professor department of pharmaceutical chemistry she ha got institute of pharmaceutical sciences today we are going to discuss proton pump inhibitors so the general form a loophole for proton pump inhibitors is shown here it contains a benzimidazole ring a pyridine ring and
These two hetero cycles are fused together by a sulfur oxide linker basically proton pump inhibitors are used to treat different types of peptic ulcers as well as gas oh esophageal reflux disorders based on their structure proton pump inhibitors can be split into two groups they all have substituted pyridine part the first group of proton pump inhibitors are
Linked to various benzimidazole whereas the second group of proton pump inhibitors are linked to a substituted a made as o pyridine ring the various structures of proton pump inhibitor are omeprazole rebecca’s own lance oprah’s old and pant oprah’s own all these drugs they act as pro drugs and they are activated by strongly acidic conditions which are found in the
Canaliculi of parietal cells activation of proton pump inhibitor involves three step first step is protonation of the benzimidazole ring second step is rearrangement to form sulfinic acid and third step is formation of disulfide with gastric h plus k plus 80 paise now let us understand this mechanism through structural form first step is protonation so the lone
Pair of electrons on nitrogen atom they are going to attack on the second carbon of the imidazole ring this leads to formation of a spiro intermediate and there is loss of the aromatic character of this imidazolium but at the same time this imidazoles ring can gain its aromatic character by transfer of the lone pair of electrons at your and at the same time this
Self oxide ring is going to break leading to formation of sulfonamide intermediate this sulfonamide intermediate will undergo an intra molecular rearrangement to form pyridinium sulfonamide structure and this pyridinium sailfin amide structure reacts with proton pump and forms a disulfide bomb leading to a reversible inhibition so this is all about the mechanism
Of inhibition of proton pump inhibitors the various drugs are first drug which was introduced was timo preserve in 1975 the mope resolve was found to inhibit acid secretion irrespective of its stimulus whether intracellular or extracellular studies on team appraisal revealed that enlargement of thyroid gland due to inhibition of irena p as well as there was a
Trophy of thymus gland literature search showed that some substituted mercaptans imidazoles had no effect on iodine uptake and introduction of such substituent’s into team oprah’s old resulted in an elimination of the toxic effects without reducing the anti security refunds so omeprazole was launched into the market in 1979 it was the first class of truck which was
Introduced under proton pump category it contains an v methoxy substituent on the benzene dissolving and this imparts more stability at neutral ph it is a one s-21 resume drug with a bad bone structure of team oprah soul but it has two methyl or two methyl substituent and two mythic c substituents to methoxy groups are present at sixth position of the benzimidazole
Thing and other at the fourth position of the pyridine ring whereas the two methyl groups they are present at third position and fifth position of typical eating drink the next produce is soma preserve this omeprazole is an s isomer of omeprazole which was developed as a magnesium salt in 1987 by astra and it was found to be having less inter patient variability
Compared to omicron zone another drug that is lance oprah soul it was introduced in 1991 in europe and in u.s. in 1995 it has no substitutions on the benzimidazole thing you can see or there is no substitution is present on this benzema dissolving on the pyridine it has two substituents the first is methyl group which is present at third position and the second
Substituent is tri fluoro ethoxy group which is present at the fourth position dex lens of rizzoli it was again launched as a follow-up of lance oprah’s all in 2009 and it is an rnn shimmer of lens of russell paint oprah soul it was the first repaired in 1985 by small-scale chemists and it has a dye fluoro oxy group on the benzene vidas old ring you can see on
This is that fluoro oxy benzini dissolving and it also has two methyl groups which are present at third and fourth position of the bigot evening reveille plays ol rebel resolve was introduced in 1999 in usa like lens oprah’s own it also does not have any substituent on the benzene at all something but it contains methyl group at third position of the building as
Well as there is presence of methoxy prop oxy substitution this is methoxy prop fox’s substitution at the fourth position grab a prasad is marketed as a sodium salt and the last drop in this category is anata presume tonetta preserve is an a made as oh pyridine proton pump inhibitor it has a plasma half-life of webinars due to the presence of a medes opie reading
Moiety the rate of metabolism is reduced and there is a longer plasma residence time it has various substituent’s that is it contains two methoxy groups one at position six on the amidah so pyridine ring and the other is present at fourth position of the pyridine ring it also has two methyl substituent which are present at position 3 and position 5 of stop avedon
Ring viability of tentative razón is double for the s10 data presume so thank you for patient listening and happy learning like share and subscribe my channel cam karuna
Transcribed from video
Proton Pump Inhibitors By Mayuuresh Raut