Substituent effects on electron spin distribution and conformation of radical ions obtained from 9-diphenylmethylenefluorenes

Franco, M. Luisa T. M. B.; Herold, Bernardo J.; Evans, Jeffrey; Rowlands, Christopher C.

doi:10.1039/p29880000443

Cited by 9 publications

(2 citation statements)

References 4 publications

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“…21 The 2,2′ and 3,3′ difluorinated benzophenones (14a and 14b) were not commercially available and were prepared as shown in Scheme 2. Addition of ethylformate to the appropriate aryllithium, generated in situ via lithium-halogen exchange, 22 afforded the intermediate alcohol 13a. Oxidation of 13a using PCC gave the desired benzophenone 14a in good overall yield.…”

Section: Chemistrymentioning

confidence: 99%

Novel Inhibitors of the Gardos Channel for the Treatment of Sickle Cell Disease

et al. 2008

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Sickle cell disease (SCD) is a hereditary condition characterized by deformation of red blood cells (RBCs). This phenomenon is due to the presence of abnormal hemoglobin that polymerizes upon deoxygenation. This effect is exacerbated when dehydrated RBCs experience a loss of both water and potassium salts. One critical pathway for the regulation of potassium efflux from RBCs is the Gardos channel, a calcium-activated potassium channel. This paper describes the synthesis and biological evaluation of a series of potent inhibitors of the Gardos channel. The goal was to identify compounds that were potent and selective inhibitors of the channel but had improved pharmacokinetic properties compared to 1, Clotrimazole. Several triarylamides such as 10 and 21 were potent inhibitors of the Gardos channel (IC50 of <10 nM) and active in a mouse model of SCD. Compound 21 (ICA-17043) was advanced into phase 3 clinical trials for SCD.

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Section: Chemistrymentioning

confidence: 99%

Novel Inhibitors of the Gardos Channel for the Treatment of Sickle Cell Disease

et al. 2008

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“…Therefore, it is a long-term goal to develop efficient methods for the synthesis of 9-fluorenylidenes in organic synthesis. Traditionally, 9-fluorenylidenes are usually synthesized using fluorene derivatives . Notably, a variety of novel methods for the construction of 9-fluorenylidene frameworks have been developed, primarily by transition-metal-catalyzed cyclization reactions .…”

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confidence: 99%