Tricyclic 3,4-dihydropyrimidine-2-thione derivatives as potent TRPA1 antagonists
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Acknowledgment
We thank Maarten te Molder for the synthesis of several of the analogs.
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2019, Bioorganic ChemistryCitation Excerpt :Our initial pharmacological work to identify dihydropyrimidine (DHPM) scaffold as potent inhibitors of cholinesterases led us to design a new tricyclic building block [16]. Thus, synthesis of DHPM-based fused ring system (25) was planned through reaction of 1,3-indanedione (22) as a 1,3-dicarbonyl precursor in the Biginelli reaction [30]. The synthesized 25 was then reacted with intermediate 21 to synthesize target heterodimer 4c (see Scheme 4).
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Present address: Hasselt University, Agoralaanbuilding, 3590 Diepenbeek, Belgium.
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