A proton-pump inhibitor expedition: the case histories of omeprazole and esomeprazole

-mercaptoethanol can reverse the inhibition of some glycolytic enzyme activities of Streptococcus mutans UA159 by benzimidazoles

“…C¸c chÊt benzimidazon vµ c¸c dÉn suÊt cña chóng nh− omeprazon (OM) hay lansoprazon (LAN), ®−îc sö dông réng r·i ®Ó kiÓm so¸t sù sinh axit qu¸ møc th«ng qua sù øc chÕ enzim H + /K + PATPaza cña c¸c tÕ bµo tiÕt axit [6,9]. C¸c chÊt nµy ®ang ®−îc sö dông réng r·i ®Ó ®iÒu trÞ c¸c bÖnh viªm loÐt d¹ dµy.…”

“…Thø ba, chóng rÊt kh«ng bÒn trong dung dÞch axit; thêi gian ph©n hñy cña chóng chØ kho ¶ng 2 phót ë pH = 1,0 vµ kho ¶ng 20 phót ë pH = 7,4. Do ®ã, benzimidazon lµ mét tiÒn chÊt (prodrug), cã thÓ tËp trung t¹i bé phËn bÞ axit hãa cña tÕ bµo ®Ých vµ ë ®ã, nã sÏ ®−îc chuyÓn thµnh d¹ng ho¹t ®éng (active form) [7,9]. C¬ chÕ t¸c ®éng cña benzimidazon nãi chung x ¶y ra b¾t ®Çu b»ng viÖc ®−îc proton ho¸ ®Ó t¹o thµnh sunphenamit, mét d¹ng ho¹t ®éng.…”

“…C«ng tr×nh nghiªn cøu cña Olbe vµ cs. [9] ®· ph¸t hiÖn thÊy c¸c t¸c nh©n khö nh− dithiothreton (DTT) hay glutathion (GSH) cã kh ¶ n¨ng ng¨n chAEn sù t¹o liªn kÕt S-S gi÷a benzimidazon vµ c¸c enzim ®Ých, v× thÕ cã thÓ lµm mÊt t¸c dông cña chóng.…”

Role of Phospholipids in Protection of the GI Mucosa

“…As a consequence, understanding the regulation of gastric acid section and the potential causes of gastric acid hypersecretion became a central research focus until 1970, with major scientific advances including the elucidation of the role of gastrin, acetylcholine, and histamine as physiological stimulants of acid secretion and the identification of luminal acid and somatostatin as physiological inhibitors [2]. Afterwards, the emphasis was on the development of pharmacological inhibitors of gastric acid secretion, with the clinically important discovery of highly effective H 2 receptor antagonists (H 2 RAs) followed by the even more efficacious proton pump inhibitors (PPIs) [3][4][5][6][7]. During this same period came the major discovery by Robert and associates of the role of prostaglandins in inhibiting gastric acid secretion, and more importantly in protecting the gastric mucosa from a damaging agents and ulcerogenic conditions (e.g., stress), a remarkable finding at the time, termed ''cytoprotection'' [8].…”

Modification of pharmaceutical substances for structure analysis

“…For example the absolute structure will either remain the same or becomes inverted in a defined way. The structure of timoprazole [3] will be presented. So far no crystals structures of this particular member of prazole family were published.…”