137968-28-6Relevant articles and documents
Design, synthesis and biological evaluation of spiropyrazolopyridone derivatives as potent dengue virus inhibitors
Chen, Haiying,Shi, Pei-Yong,Xie, Xuping,Xu, Jimin,Xue, Yu,Ye, Na,Zhou, Jia,Zou, Jing
, (2020/04/10)
The effective treatment for dengue virus infection continues to be a challenge. We herein reported our continued SAR exploration on the spiropyrazolopyridone scaffold. Introducing different substituents at the 3?- or 5?-site of the pyrazolopyridone core or moving the benzyl chain to the adjacent nitrogen led to a significant loss of potency on DENV-2. While a narrow range of substitutions were tolerated at the para-position of the phenyl ring, di-substitution on the phenyl ring is beneficial for DENV-2 potency and has variable influences on DENV-3 potency depending on the exact compound. Among these molecules, compounds 22 (JMX0376) with 4-chloro-3-fluorobenzyl and 24 (JMX0395) with 2,4-bis(trifluoromethyl)benzyl showed the most potent and broadest inhibitory activities against DENV-1 to ?3 with nanomolar to low micromolar EC50 values.
TETRAZOLE COMPOUNDS AS OREXIN RECEPTOR ANTAGONISTS
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Page/Page column 36, (2010/01/07)
The invention relates to tetrazole compounds of formula (I) wherein X, Y, Z, R1, R2 and R3 are as described in the description; to pharmaceutically acceptable salts thereof, and to the use of such compounds use as medicaments, especially as orexin receptor antagonists.