454170-16-2Relevant articles and documents
ADENOSINE RECEPTOR AGONISTS
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Paragraph 0136-0137, (2020/10/09)
The present invention relates to compounds of Formula (I) for use in the treatment of nervous system disorders and pain, wherein Formula (I) is: formula(I) or a pharmaceutically acceptable salt or isomer thereof, wherein R is defined herein. The compounds are selective A1 adenosine receptor agonists with preferential action in the nervous system, with spared cardiovascular system and respiratory effects. The invention also relates to pharmaceutical compositions comprising the compounds.
Matrix metalloproteinase inhibitors based on the 3-mercaptopyrrolidine core
Jin, Yonghao,Roycik, Mark D.,Bosco, Dale B.,Cao, Qiang,Constantino, Manuel H.,Schwartz, Martin A.,Sang, Qing-Xiang Amy
, p. 4357 - 4373 (2013/07/19)
New series of pyrrolidine mercaptosulfide, 2-mercaptocyclopentane arylsulfonamide, and 3-mercapto-4-arylsulfonamidopyrrolidine matrix metalloproteinase inhibitors (MMPIs) were designed, synthesized, and evaluated. Exhibiting unique properties over other MMPIs (e.g., hydroxamates), these newly reported compounds are capable of modulating activities of several MMPs in the low nanomolar range, including MMP-2 (～2 to 50 nM), MMP-13 (～2 to 50 nM), and MMP-14 (～4 to 60 nM). Additionally these compounds are selective to intermediate- and deep-pocket MMPs but not shallow-pocketed MMPs (e.g., MMP-1, ～850 to >50 000 nM; MMP-7, ～4000 to >25 000 nM). Our previous work with the mercaptosulfide functionality attached to both cyclopentane and pyrrolidine frameworks demonstrated that the cis-(3S,4R)-stereochemistry was optimal for all of the MMPs tested. However, in our newest compounds an interesting shift of preference to the trans form of the mercaptosulfonamides was observed with increased oxidative stability and biological compatibility. We also report several kinetic and biological characteristics showing that these compounds may be used to probe the mechanistic activities of MMPs in disease.
cis-Cyclopentyl PNA (cpPNA) as constrained chiral PNA analogues: stereochemical dependence of DNA/RNA hybridization.
Govindaraju,Kumar, Vaijayanti A,Ganesh, Krishna N
, p. 860 - 861 (2007/10/03)
DNA/RNA hybridization studies of PNA-T oligomers with cis-(1S,2R/1R,2S)-cyclopentyl units in the backbone show stereochemistry dependent binding with RNA/DNA discrimination.
