- 6,5-HETEROCYCLIC PROPARGYLIC ALCOHOL COMPOUNDS AND USES THEREFOR
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The invention relates to novel compounds of Formula I: wherein A, Y, R1, R2 and the subscript b each has the meaning as described herein and compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, isotopes, pharmaceutically acceptable salts, or prodrugs thereof. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.
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Page/Page column 80
(2015/05/06)
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- Mapping the landscape of potentially primordial informational oligomers: (3′→2′)-D-phosphoglyceric acid linked acyclic oligonucleotides tagged with 2,4-disubstituted 5-aminopyrimidines as recognition elements
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The (3′→2′)-phosphodiester glyceric acid backbone containing an acyclic oligomer tagged with 2,4-disubstituted pyrimidines as alternative recognition elements have been synthesized. Strong cross-pairing of a 2,4-dioxo-5-aminopyrimidine hexamer, rivaling locked nucleic acid (LNA) and peptide nucleic acid (PNA), with complementary adenine-containing DNA and RNA sequences was observed. The corresponding 2,4-diamino- and 2-amino-4-oxo-5- aminopyrimidine-tagged oligomers were synthesized, but difficulties in deprotection, purification, and isolation thwarted further investigations. The acyclic phosphate backbone structure of the protected oligomer seems to be prone to an eliminative degradation owing to the acidic hydrogen at the 2′-position-an arrangement that renders the oligomer vulnerable to the conditions used for the removal of the protecting groups on the heterocyclic recognition element. However, the free oligomers seem to be stable under the conditions investigated. Prehistoric pairs: The (3′→2′)- phosphodiester glyceric acid backbone containing an acyclic oligomer tagged with 2,4-dioxo-5-aminopyrimidine pairs (see scheme) strongly with complementary adenine-containing DNA and RNA sequences. An eliminative degradation of the acyclic phosphate backbone owing to the acidic hydrogen at the 2′-position hampered studies of the corresponding 2,4-diamino- and 2-amino-4-oxo-5- aminopyrimidine series.
- Hernandez-Rodriguez, Marcos,Xie, Jian,Osornio, Yazmin M.,Krishnamurthy, Ramanarayanan
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scheme or table
p. 1252 - 1262
(2011/12/14)
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- Mapping the landscape of potentially primordial informational oligomers: Oligodipeptides tagged with 2,4-disubstituted 5-aminopyrimidines as recognition elements
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(Chemical Equation Presented) Bit different: 2,4-Dioxo- and 2,4-diamino-5-aminopyrimidine nuclei attached to an oligodipeptide backbone display a disparity in their base-pairing strength which is opposite to that shown by corresponding triazines. This behavior points to a remarkable correlation between pairing strength and ΔpKa values of pairs of complementary bases.
- Mittapalli, Gopi Kumar,Osornio, Yazmin M.,Guerrero, Miguel A.,Reddy, Kondreddi Ravinder,Krishnamurthy, Ramanarayanan,Eschenmoser, Albert
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p. 2478 - 2484
(2008/03/11)
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