162170-49-2Relevant academic research and scientific papers
Pyran-2-ones and 5,6-dihydropyran-2-ones useful for treating hyperplasia and other diseases
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, (2010/02/05)
Certain 2H-pyran-2-ones are useful for treating benign prostatic hypertrophy or hyperplasia, prostatic cancer, alopecia, hirsutism, acne vulgaris and seborrhea.
PYRANONE COMPOUNDS USEFUL TO TREAT RETROVIRAL INFECTIONS
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, (2008/06/13)
The present invention relates to compounds of formulae (I) and (II) which are pyran-2-ones, 5,6-dihydro-pyran-2-ones, 4-hydroxy-benzopyran-2-ones, 4-hydroxy-cycloalkyl[b]pyran-2-ones, and derivatives thereof, useful for inhibiting a retrovirus in a mammalian cell infected with said retrovirus, wherein R 10 and R 20 taken together are formulae (III) and (IV). STR1
Structure-based design of novel HIV protease inhibitors: Sulfonamide-containing 4-hydroxycoumarins and 4-hydroxy-2-pyrones as potent non-peptidic inhibitors
Thaisrivongs, Suvit,Janakiraman, Musiri N.,Chong, Kong-Teck,Tomich, Paul K.,Dolak, Lester A.,Turner, Steve R.,Strohbach, Joseph W.,Lynn, Janet C.,Horng, Miao-Miao,Hinshaw, Roger R.,Watenpaugh, Keith D.
, p. 2400 - 2410 (2007/10/03)
The low oral bioavailability and rapid biliary excretion of peptide-derived HIV protease inhibitors have limited their utility as potential therapeutic agents. Our broad screening program to discover non-peptidic HIV protease inhibitors previously identif
Structure-Based Design of Novel HIV Protease Inhibitors: Carboxamide-Containing 4-Hydroxycoumarins and 4-Hydroxy-2-pyrones as Potent Nonpeptidic Inhibitors
Thaisrivongs, Suvit,Watenpaugh, Keith D.,Howe, W. Jeffrey,Tomich, Paul K.,Dolak, Lester A.,et al.
, p. 3624 - 3637 (2007/10/03)
The low oral bioavailability and rapid biliary excretion of peptide-derived HIV protease inhibitors have limited their utility as potential therapeutic agents.Our broad screening program to discover nonpeptidic HIV protease inhibitors had previously identified compound II (phenprocoumon, Ki = 1 μM) as a lead template.Crystal structures of HIV protease complexes containing the peptide-derived inhibitor I (1-(naphthoxyacetyl)-L-histidyl-5(S)-amino-6-cyclohexyl-3(R),4(R)-dihydroxy-2(R)-isopropylhexanoyl-L-isoleucine N-(2-pyridylmethyl)amide) and nonpeptidic inhibitors, such as phenprocoumon (compound II), provided a rational basis for the structure-based design of more active analogues.This investigation reports on the important finding of a carboxamide functionality appropriately added to the 4-hydroxycoumarin and the 4-hydroxy-2-pyrone templates which resulted in new promising series of nonpeptidic HIV protease inhibitors with improved enzyme-binding affinity.The most active diastereomer of the carboxamide-containing compound XXIV inhibited HIV-1 protease with a Ki value of 0.0014 μM.This research provides a new design direction for the discovery of more potent HIV protease inhibitors as potential therapeutic agents for the treatment of HIV infection.
