The world's first wiki where authorship really matters (Nature Genetics, 2008). Due credit and reputation for authors. Imagine a global collaborative knowledge base for original thoughts. Search thousands of articles and collaborate with scientists around the globe.

wikigene or wiki gene protein drug chemical gene disease author authorship tracking collaborative publishing evolutionary knowledge reputation system wiki2.0 global collaboration genes proteins drugs chemicals diseases compound
Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
 
 

Importance of the alanine methyl ester side chain for the biological activity profile of dual-function phenyl phosphate derivatives of bromo-methoxy-zidovudine.

In a systematic search for developing a virucidal spermicide with potent anti-human immunodeficiency virus (HIV) and spermicidal activities, we synthesized and evaluated 14 phosphoramidate derivatives of 5-bromo-6-methoxy-zidovudine (PP-BMZ) with differing amino acid ester side chains and para substitutions on the phenyl moiety. Anti-HIV activity was tested by measuring viral p24 antigen production as a marker of viral replication in HIV-1-infected human peripheral blood mononuclear cells. The effect of various PP-BMZ compounds on human sperm motion kinematics was analysed by computer-assisted sperm analysis. Varying the Ala side chain of the phosphoramidate group to other non-polar amino acids, including the cyclic amino acids proline and tryptophan, led to significant alterations in both anti-HIV and spermicidal activities. Our findings highlight the necessity of the Ala side chain and the presence of an electron-withdrawing para-bromo substituent on the phenyl moiety in addition to the bromo-methoxy functional groups on the thymine ring for the PP-BMZ compounds to be effective virucidal spermicides. These membrane permeable dual-function nucleoside analogues may provide the basis for a new strategy aimed at prevention of the sexual transmission of HIV while providing fertility control for women.[1]

References

 
WikiGenes - Universities