88623-81-8Relevant articles and documents
Total Synthesis and Structural Elucidation of (-)-Cephalezomine G
Jeon, Hongjun,Cho, Hyunkyung,Kim, Sanghee
, p. 1121 - 1124 (2019)
The first asymmetric synthesis and configurational elucidation of (-)-cephalezomine G was achieved. The highly functionalized Cα-substituted proline derivative was prepared from d-proline as the only chiral source via a C → N → C chirality transfer method
Novel 3C-like protease inhibitor as well as preparation method and application thereof
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Paragraph 0047-0048; 0057-0059, (2021/09/26)
The invention provides a novel 3C-like protease inhibitor which is 3 ", 4" - O - diacetyl -epicatechin trans-caffeic acid ester with a specific structure. The invention further provides a preparation method and application of the 3C-like protease inhibitor. The invention has the advantages that the compound 3 ", 4" - O - diacetyl - epicatechin trans-caffeic acid ester is designed and synthesized based on the structure of epicatechin; even when the concentration is low, the activity of 3C-like protease in the novel coronavirus can be obviously inhibited. The compounds can be used as 3C-like protease inhibitors and are used for preparing anti-novel coronavirus SARS-CoV - 2 infection drugs.
TRPV3 inhibitor and preparation method thereof
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Paragraph 0037; 0043; 0050; 0051; 0058; 0059; 0066; 0067, (2021/04/10)
The invention discloses a TRPV3 inhibitor. The TRPV3 inhibitor is formed by sequentially connecting an R1 group, an R group and an R2 group, and the molecular structural general formula of the TRPV3 inhibitor is shown as a formula 1, wherein the structural formula of the R1 group is represented by a formula 2, R3 is selected from any one of -H, -OAc, -OH, a halogen group, -F3CO or a group containing a benzenesulfonyloxy group, and R4 is selected from any one of -H, -OAc or -OH; R1 and R2 are selected from alkyl or formula 3, R5 is selected from C or N, R6 is selected from any one of hydrogen, alkyl, halogen group or trifluoromethyl, R7 is selected from any one of hydrogen, halogen group, cyano group, nitro group or trifluoromethoxy group, and R8 is selected from hydrogen or halogen group. The invention also discloses a preparation method and application of the TRPV3 inhibitor. The TRPV3 inhibitor disclosed by the invention can specifically inhibit a TRPV3 ion channel and has huge scientific research and clinical values.
ORAL PHARMACEUTICAL FORMULATIONS OF BITTER COMPOUNDS FOR PULMONARY HYPERTENSION
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Page/Page column 11-12, (2020/02/06)
There is disclosed an oral pharmaceutical formulation of bitter compounds that are agonists of TAS2R receptors for the treatment of pulmonary hypertension (PAH). More specifically, there is disclosed a PAH oral formulation comprising a bitter agent selected from the group consisting of 3-caffeoylquinic-1,5-lactone (3-CQL), chlorogenic acid (CGA), denatonium benzoate (DB), denatonium chloride (DC), denatonium saccharide (DS), denatonium acetate (DA), and combinations thereof and a PDE-5 inhibitor.