Diarylpyrimidines

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Diarylpyrimidines and diaryltriazines are two closely related classes of molecules resembling the pyrimidine nucleotides found in DNA. They show great potency in inhibiting the activity of HIV reverse transcriptase.[1][2] Several compounds in this class are currently underdevelopment as the next generation of non-nucleoside reverse transcriptase inhibitors,[3][4] notably a compound called TMC278 expected to receive FDA approval in 2009.[5]

References

  1. Van Herrewege Y, Vanham G, Michiels J, Fransen K, Kestens L, Andries K, Janssen P, Lewi P (2004). "A series of diaryltriazines and diarylpyrimidines are highly potent nonnucleoside reverse transcriptase inhibitors with possible applications as microbicides". Antimicrob. Agents Chemother. 48 (10): 3684–9. doi:10.1128/AAC.48.10.3684-3689.2004. PMID 15388420.
  2. Mordant C, Schmitt B, Pasquier E, Demestre C, Queguiner L, Masungi C, Peeters A, Smeulders L, Bettens E, Hertogs K, Heeres J, Lewi P, Guillemont J (2007). "Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains". Eur J Med Chem. 42 (5): 567–79. doi:10.1016/j.ejmech.2006.11.014. PMID 17223230.
  3. Goebel F, Yakovlev A, Pozniak AL, Vinogradova E, Boogaerts G, Hoetelmans R, de Béthune MP, Peeters M, Woodfall B (2006). "Short-term antiviral activity of TMC278--a novel NNRTI--in treatment-naive HIV-1-infected subjects". AIDS. 20 (13): 1721–6. doi:10.1097/01.aids.0000242818.65215.bd. PMID 16931936.
  4. Fang C, Bauman JD, Das K, Remorino A, Arnold E, Hochstrasser RM (2007). "Two-dimensional infrared spectra reveal relaxation of the nonnucleoside inhibitor TMC278 complexed with HIV-1 reverse transcriptase". Proc Natl Acad Sci U S A. doi:10.1073/pnas.0709320104. PMID 18040050.
  5. Steve Mitchell. HIV Market To Top 10 Billion Dollars. United Press International. April 11, 2007.

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