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- W1978006346 abstract "Compounds that bind to sickle hemoglobin (Hb S) producing an allosteric shift to the high-affinity Hb S that does not polymerize are being developed to treat sickle cell anemia (SCA). In this study, three series of pyridyl derivatives of substituted benzaldehydes (Classes I–III) that combine structural features of two previously determined potent antisickling agents, vanillin and pyridoxal, were synthesized. When analyzed with normal human whole blood, the compounds form Schiff-base adducts with Hb and left shift the oxygen equilibrium curve (OEC) to the more soluble high-affinity Hb, more than vanillin or pyridoxal. Generally, Class-I compounds with an aromatic aldehyde located ortho to the pyridyl substituent are the most potent, followed by the Class-II compounds with the aldehyde at the meta-position. Class-III compounds with the aldehyde at the para position show the weakest activity. The structure–activity studies of these pyridyl derivatives of substituted benzaldehydes demonstrate significant allosteric potency that may be useful for treating SCA." @default.
- W1978006346 created "2016-06-24" @default.
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- W1978006346 date "2008-09-24" @default.
- W1978006346 modified "2023-10-03" @default.
- W1978006346 title "Pyridyl Derivatives of Benzaldehyde as Potential Antisickling Agents" @default.
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- W1978006346 doi "https://doi.org/10.1002/cbdv.200890165" @default.
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