851726-57-3Relevant academic research and scientific papers
Fluoro-olefins as peptidomimetic inhibitors of dipeptidyl peptidases
Van Der Veken, Pieter,Senten, Kristel,Kertèsz, István,De Meester, Ingrid,Lambeir, Anne-Marie,Maes, Marie-Berthe,Scharpé, Simon,Haemers, Achiel,Augustyns, Koen
, p. 1768 - 1780 (2007/10/03)
The feasibility of the fluoro-olefin function as a peptidomimetic group in inhibitors for dipeptidyl peptidase IV and II (DPP IV and DPP II) is investigated by evaluation of N-substituted Gly-Ψ[CF=C]pyrrolidines, Gly-Ψ[CF=C]piperidines, and Gly-Ψ[CF=C](2-cyano)pyrrolidines. Of this later class, the (Z)- and (E)-fluoro-olefin analogues were prepared and chemical stability in comparison with the parent amide was checked. Most of these compounds exhibited a strong binding preference toward DPP II with IC 50 values in the low micromolar range, while only low DPP IV inhibitory potential is seen.
HYDROXY PYRIDOPYRROLOPYRAZINE DIONE COMPOUNDS USEFUL AS HIV INTEGRASE INHIBITORS
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Page/Page column 81, (2010/02/11)
Hydroxy-substituted pyridopyrrolopyrazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I): (I) wherein a, b, A, B, R1, R2, R3, R4, R5, R6, R7 and R8 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
HIV INTEGRASE INHIBITORS
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Page/Page column 61-62, (2010/02/14)
Bicyclic uracils and related compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the compounds are of Formula (I) wherein a, b, Y, R1, R2, R3 and R4 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
