245660-15-5Relevant articles and documents
Novel route to the synthesis of hydroxylated piperidine and pyrrolidine derivatives via the intramolecular reaction of γ-aminoallylstannane with aldehyde
Kadota, Isao,Kawada, Miho,Saya, Shioko,Yamamoto, Yoshinori
, p. 2109 - 2112 (1996)
The Lewis acid mediated intramolecular reaction of gamma-aminoallyl-stannane 6 gave trans-beta-hydroxypiperidine derivative 7a as a major product. On the other hand, the thermal cyclization of 6 and 8 afforded cis-beta-hydroxypiperidine 7b and pyrrolidine derivative 9b, respectively, with very high stereoselectivity.
NOVEL DUAL MODE OF ACTION SOLUBLE GUANYLATE CYCLASE ACTIVATORS AND PHOSPHODIESTERASE INHIBITORS AND USES THEREOF
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Page/Page column 113, (2021/12/28)
The present invention relates to compounds of formula (I), or pharmaceutically acceptable salt, solvate or hydrate thereof, wherein said compound of formula (I) comprises at least one covalently bound -ONO2 or -ONO moiety and at most four covalently bound -ONO2 or -ONO moieties, and wherein AR, R1, X, R3 and R4 are as defined in claim 1; and pharmaceutical compositions thereof, and their use in methods of treating or preventing a disease alleviated by inhibition of PDE5 in a human or in a non-human mammal.
Improved potency and reduced toxicity of the antifungal peptoid AEC5 through submonomer modification
Middleton, Madyson P.,Armstrong, Scott A.,Bicker, Kevin L.
supporting information, p. 3514 - 3519 (2018/10/15)
As proteolytically stable peptidomimetics, peptoids could serve as antifungal agents to supplement a therapeutic field wrought with toxicity issues. We report the improvement of an antifungal peptoid, AEC5, through an iterative structure-activity relationship study. A sarcosine scan was used to first identify the most pharmacophorically important peptoid building blocks of AEC5, followed by sequential optimization of each building block. The optimized antifungal peptoid from this study, β-5, has improved potency towards Cryptococcus neoformans and decreased toxicity towards mammalian cells. For example, the selectivity ratio for C. neoformans over mammalian fibroblasts was improved from 8 for AEC5 to 37 for β-5.