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Download (4Mb) - Etheses - Saurashtra University

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Part-IAim of Present WorkR 2 OR 3 R 4R 2 OR 3 R 4R 2 OR 3 R 4NH + (Slow)NNNSOHNSONNHSOHNHNHR 11 2R 1R 13-H 2 OR 2 OR 3 R 4R 2 OR 3 R 4NNNNHSS-Cys 813 -EnyNNSHS-Cys 813 -EnyR 1R 15Covalently bound species4Figure 2. Reaction mechanism proposed for the acid transformation of pyridinylmethylsulfinylbenzimidazoles (PMSB’s) to sulfenamide.Therefore, there is a need to develop better analogs of the existing PPI’s in which theformation of this disulfide intermediate can be avoided, so as to obtain reversible Protonpump inhibition & thus overcome the drawbacks of the currently available PPI’s.2.1 Structural changes done so farEarlier, medicinal chemists worldwide have tried a variety of changes in the skeleton ofPMSB moiety based on the principles of the isosteric/bioisosteric replacement of thegroup as well as the heterocyclic ring system to achieve subtle changes in the nature ofthis PMSB nucleus, which may alter its irreversible binding (inhibition) to the protonpump to a reversible one.58

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