Cyclooxygenases play a vital role in inflammation and are responsible for the production of prostaglandins.Two cyclooxygenases are described,the constitutive cyclooxygenase-1 and the inducible cyclooxygenase-2,for whi...Cyclooxygenases play a vital role in inflammation and are responsible for the production of prostaglandins.Two cyclooxygenases are described,the constitutive cyclooxygenase-1 and the inducible cyclooxygenase-2,for which the target inhibitors are the non-steroidal anti-inflammatory drugs(NSAIDs).Prostaglandins are a class of lipid compounds that mediate acute and chronic inflammation.NSAIDs are the most frequent choices for treatment of inflammation.Nevertheless,currently used anti-inflammatory drugs have become associated with a variety of adverse effects which lead to diminished output even market withdrawal.Recently,more studies have been carried out on searching novel selective COX-2 inhibitors with safety profiles.In this review,we highlight the various structural classes of organic and natural scaffolds with efficient COX-2 inhibitory activity reported during 2011-2021.It will be valuable for pharmaceutical scientists to read up on the current chemicals to pave the way for subsequent research.展开更多
Benzaldehyde lyase(BAL)is an enzyme which was originally found from Pseudomonas fluorescens biovar I.It has long been used in the formation of a C-C bond.BAL can exclusively yield(R)-enantioselective products from the...Benzaldehyde lyase(BAL)is an enzyme which was originally found from Pseudomonas fluorescens biovar I.It has long been used in the formation of a C-C bond.BAL can exclusively yield(R)-enantioselective products from the synthesis ofα-hydroxy ketones and has so far been explored as an important enzyme to prepare the corresponding intermediate of pharmaceuticals.Due to its substrate spectrum and stereospecificity,this enzyme extends the synthetic potential for carboligations appreciably.In this review,we highlight the biotransformation applications of BAL in recent years,some of which have achieved intriguing results and provided the theoretical basis for drug development and industrial purpose in the future.展开更多
文摘Cyclooxygenases play a vital role in inflammation and are responsible for the production of prostaglandins.Two cyclooxygenases are described,the constitutive cyclooxygenase-1 and the inducible cyclooxygenase-2,for which the target inhibitors are the non-steroidal anti-inflammatory drugs(NSAIDs).Prostaglandins are a class of lipid compounds that mediate acute and chronic inflammation.NSAIDs are the most frequent choices for treatment of inflammation.Nevertheless,currently used anti-inflammatory drugs have become associated with a variety of adverse effects which lead to diminished output even market withdrawal.Recently,more studies have been carried out on searching novel selective COX-2 inhibitors with safety profiles.In this review,we highlight the various structural classes of organic and natural scaffolds with efficient COX-2 inhibitory activity reported during 2011-2021.It will be valuable for pharmaceutical scientists to read up on the current chemicals to pave the way for subsequent research.
基金The author would like to thank Dr.K.Kaliyaperumal,Dr.M.Fredimoses and Dr.B.Sachin for their careful revisions of this work.
文摘Benzaldehyde lyase(BAL)is an enzyme which was originally found from Pseudomonas fluorescens biovar I.It has long been used in the formation of a C-C bond.BAL can exclusively yield(R)-enantioselective products from the synthesis ofα-hydroxy ketones and has so far been explored as an important enzyme to prepare the corresponding intermediate of pharmaceuticals.Due to its substrate spectrum and stereospecificity,this enzyme extends the synthetic potential for carboligations appreciably.In this review,we highlight the biotransformation applications of BAL in recent years,some of which have achieved intriguing results and provided the theoretical basis for drug development and industrial purpose in the future.
