By F.G.De Las Heras, S. Vega, Federico G. De Las Heras, Salvador Vega
Medicinal Chemistry Advances covers the lawsuits of the 7th foreign Symposium on Medicinal Chemistry. The e-book studies the papers awarded within the symposium.
The major themes that this e-book covers are nucleosides in chemotherapy; theoretical techniques to medicinal chemistry; platelets and antithrombotic brokers; receptors; antiviral brokers; antilipidemic brokers; respiration method; significant fearful method; enzyme inhibitors; and bioactive peptides.
Chemists, pharmacologists, biochemists, physicians and different pros and researchers excited about the advance of pharmaceutical box will locate this ebook attention-grabbing.
Read or Download Medicinal Chemistry Advances. Proceedings of the Seventh International Symposium on Medicinal Chemistry, Torremolinos, Spain 2–5 September 1980 PDF
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Extra info for Medicinal Chemistry Advances. Proceedings of the Seventh International Symposium on Medicinal Chemistry, Torremolinos, Spain 2–5 September 1980
3) to afford blocked nucleosides (£) which were then de-protected with methanolic am monia to nucleosides (4). In similar fashion, condensation of halogenose (2,) with trimethylsilylatecl uracils followed by removal of blocking groups with methanolic ammonia gave the 2'-fluoro-ara-U nucleosides (J5). The synthesis of the 29 J. J. Fox, C. Lopez and K. A. Watanabe thymine nucleoside, 2'-fluoro-5-methyl-ara-U, [FMAU, 5f, Fig. 3] is more conveni ently prepared (Watanabe, Su, Fox, unpublished) by treatment of 4f with aqueous acetic acid at reflux temperature.
04 1 * ED 90 = effective dose to inhibit HSV-I replication by 9 0 % . t I D 5 0 = dose necessary for 5 0 % inhibition of growth of Vero cells. 25 substituent confers better antiviral activity to these 5-iodocytosine nucleosides than does a 2'-hydroxyl or a 2* -hydrogen substituent. A similar conclusion is warranted from a comparison of the 5-iodouracil nucleosides [ara-5-iodouracil (ara-IU), IdU, and FIAU (5§)j. In the thymine series, 2'-fluoro-5-methyl-ara-U (FMAU) is clearly more effective against HSV-1 than is ara-T.
4. H H Ri» H ) (R «CH 3 ■, R, - O H ) Chloramphenicol OH | N o r p l i c a c e t i n ( R = CH 3 HN ) (R« H ,N/1 CH 3 Plicacetin Bamicetin H C—C—CH,O H z I I OH H ό R,«H ) Oxamicetin ; NH 0 ( R = (CH3)2N) H X 0 CH2OH J-N-iH HO. *kNACH o H OH 0 Actinobolin Sparsomycin Chemical structures of pyrimidine nucleoside antibiotics that inhibit protein synthesis (gougerotin, blasticidin S , anthelmycin, amicetin, bamicetin, oxamicetin, plicamicetin and norplicacetin) and other protein synthesis inhibitors that act on the acceptor site of the peptidyl transferase center (chloramphenicol, actinobolin and sparsomycin) .
Medicinal Chemistry Advances. Proceedings of the Seventh International Symposium on Medicinal Chemistry, Torremolinos, Spain 2–5 September 1980 by F.G.De Las Heras, S. Vega, Federico G. De Las Heras, Salvador Vega