86571-57-5Relevant articles and documents
Synthesis of Seco-Analogues of the DHCR24 Inhibitor SH-42
Bracher, Franz,Heerdegen, Desirée,Kornmayer, Moritz M.,Kriegler, Katharina N.,Müller, Christoph,Mayer, Peter,Reuter, Doreen
, p. 6270 - 6288 (2020)
In a project aimed at the further development of the potent steroidal anti-inflammatory Δ24-dehydrocholesterol reductase (DHCR24) inhibitor SH-42 we worked out routes to ring B seco-steroidal analogues. The required building blocks, bearing rings C and D of the parent steroidal structure, were synthesised starting from ergocalciferol. The novel seco-analogues carry aromatic residues as ring A equivalents at C-4 position with variation of the linker length resulting in 4-aryl-, 4-benzyl- and 4-(arylethyl)perhydroindanes. As saturated analogues of the latter 4-(cyclohexylethyl)perhydroindanes were prepared. Moreover, aromatic and aliphatic residues were attached to C-5 position of the perhydroindane scaffold. Unfortunately, none of these structurally diverse seco-analogues of SH-42 showed noteworthy inhibition of target enzyme DHCR24, indicating the relevance of the intact steroidal structure for the development of potent inhibitors of this enzyme.
Heterocylic antiviral compounds
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Page/Page column 24, (2008/12/08)
This invention relates to piperidine derivatives of formula I wherein R1, R2, R3 and R4 are as defined herein useful in the treatment of a variety of disorders, including those in which the modulation of CCR5 re
NITROGENOUS FUSED BICYCLIC COMPOUND
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Page/Page column 73, (2010/11/26)
A novel nitrogenous fused bicyclic compound represented by the following general formula [1] or a pharmacologically acceptable salt of the compound. They have excellent SK channel blocking activity and are useful as a medicine. [I] (In the formula, R 0 represents hydrogen, halogeno, etc.; R 1 represents a group represented by the formula (a) or (b); A represents a group represented by the formula (X) or (Y); D 1 , D 2 and D 3 each represents N or CH; R 2 represents halogeno or optionally halogenated lower alkyl, etc.; R 3 represents hydrogen or lower alkyl; and Q represents lower alkylene.)
