F.G.De Las Heras, S. Vega, Federico G. De Las Heras,'s Medicinal Chemistry Advances. Proceedings of the Seventh PDF

By F.G.De Las Heras, S. Vega, Federico G. De Las Heras, Salvador Vega

ISBN-10: 0080252974

ISBN-13: 9780080252971

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.

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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

Example text

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thymine nucleoside, 2'-fluoro-5-methyl-ara-U, [FMAU, 5f, Fig. 3] is more conveni­ ently prepared (Watanabe, Su, Fox, unpublished) by treatment of 4f with aqueous acetic acid at reflux temperature.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) .

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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


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