2005Benzopyran derivatives R 0350 IK Ca -Channel Blockers. Part 2. Discovery of Cyclohexadienes. -The development of a novel class of cyclohexadiene derivatives [cf. (III), (V)] as potent low molecular weight IKCa-channel blockers starting from the dihydropyridine Nifedipine as a weak lead is reported. The most promising derivative (Va) shows above 10-fold enrichment in rat brain, reduces the intracranial pressure, the water content in brain tissue and the infarct volume. -(URBAHNS*, K.; GOLDMANN, S.; KRUEGER, J.; HORVATH, E.; SCHUHMACHER, J.; GROSSER, R.; HINZ, V.; MAULER, F.; Bioorg. Med. Chem. Lett. 15 (2005) 2, 401-404; Inst. Med. Chem.,

The compound (VI) can be prepared as a chiral tartrate salt on a two‐kilogram‐scale.

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ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.