The invention encompasses a series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.
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(2010/11/29)
Protonation of Some 3-, 4-, and 5-Substituted Thiophen-2-carboxamides
The protonation behaviour at 25 deg C in aqueous sulphuric acid solution of some 3-, 4-, and 5-substituted thiophen-2-carboxamides has been investigated by u.v. spectrophotometry. pKBH+ Values were calculated by HA and Bunnett-Olsen methods using the multivariate analysis.A positive ?α-s value was obtained indicating that the sulphur atom acts as an electron-withdrawing substituent.Plots of pKBH+of 4- and 5-substituted thiophen-2-carboxamides and 3-substituted derivatives against ? were linear with the slope +1.10 and +1.28, respectively.A ρo/ρm,p ratio higher than unity (1.16) has been observed indicating a larger transmission of electronic effects between the 2- and 3-positions of the thiophen ring than between the 2- and 4- or 5-positions.
