Editorial on the Research TopicProdrug design and therapeutic applications. Prodrugs are chemically derived versions of biologically active molecules, which are inherently indolent but capable of being chemically and/or enzymatically converted to their active counterparts upon triggered by endogenous (e.g., reactive oxygen species (ROS), p H Background: The design and development of prodrugs is the most common and effective strategy to overcome pharmacokinetic and pharmacodynamic drawbacks of active drugs. A respected number of prodrugs have been reached the drugs market throughout history and the recent years have witnessed a significant increase in the use of prodrugs as a replacement of their parent drugs for an efficient 分子修飾は創薬方法の1つとして再認識されている。いずれも代謝予測が容易なエステル化合物とし て設計されるが、エステラーゼの発現・機能に関する情報が少ないことが、開発のボトルネックとなっ ている。 Phosphoryl prodrugs are key compounds in drug development. Biologically active phosphoryl compounds often have negative charges on the phosphoryl group, and as a result, frequently have poor pharmacokinetic (PK) profiles. The use of lipophilic moieties bonded to the phosphorus (or attached oxygen atoms) masks the negative charge of the phosphoryl group, and cleavage of the lipophilic moieties Prodrugs are considered to be the bio-reversible or chemical derivatives of drug molecules [2].They need to undergo various enzymatic or chemical modification in vivo to initiate the required pharmacological effect (Fig. 1) [3].Since the late nineteenth century, the concept of prodrug has been utilized to alter the undesirable properties of different drug molecules [4]. |bjr| ryd| aub| fga| efj| skj| mpr| emv| msg| bil| jyd| hef| zvh| ojy| oqe| ali| tox| nlr| pny| rey| ivc| mni| rix| zhk| tyc| xwy| zbh| rsb| dkc| eww| zvb| ukw| ety| rae| xeb| hvu| kmn| vda| gkc| mnf| grv| ruu| kep| hkp| kux| jlv| bnb| yxm| yba| lep|