Journal
ARCHIV DER PHARMAZIE
Volume 351, Issue 5, Pages -Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ardp.201800018
Keywords
annulated thienopyrimidines; cycloalkene-fused thienopyrimidines; phosphodiesterase inhibitor; planarity
Funding
- National Cancer Institute (USA) [NCI 5 R01 CA155638]
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Novel cycloalkene-fused thienopyrimidine analogues with enhanced phosphodiesterase 5 (PDE5) inhibitory properties are presented. The structure of the reported scaffold was modulated through variation of the terminal cycloalkene ring size, as well as by varying the substituents at position 4 through the attachment of different groups including aniline, benzylamine, cyclohexylethylamine, methyl/acetyl/aryl piperazines, and aryl hydrazones. Compound 15Y with a benzylamine substituent and cycloheptene as terminal ring showed the highest PDE5 inhibitory activity with an IC50 value as low as 190 nM and with good selectivity versus PDE7 and PDE9.
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