Zobrazeno 1 - 10
of 23
pro vyhledávání: '"David, Din Belle"'
Autor:
Shouming, Wang, Anssi, Haikarainen, Antti, Pohjakallio, Julius, Sipilä, Janne, Kaskinoro, Satu, Juhila, Niina, Jalava, Mikko, Koskinen, Marja, Vesajoki, Esa, Kumpulainen, Jarmo, Pystynen, Tuula, Koskelainen, Patrik, Holm, David, Din Belle
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 77:129005
Here is reported the design and synthesis of a series of highly potent and selective α2C antagonists using benzodioxine methyl piperazine as a central scaffold by pharmacophoric analysis to improve the pharmacokinetics of suboptimal clinical candida
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a79817adb5e1c73186ea6f167f3ba422
https://doi.org/10.1016/j.bmcl.2022.129005
https://doi.org/10.1016/j.bmcl.2022.129005
Autor:
Shouming, Wang, Anssi, Haikarainen, Antti, Pohjakallio, Julius, Sipilä, Janne, Kaskinoro, Satu, Juhila, Niina, Jalava, Mikko, Koskinen, Marja, Vesajoki, Esa, Kumpulainen, Jarmo, Pystynen, Tuula, Koskelainen, Patrik, Holm, David, Din Belle
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 69:128783
In this manuscript, we report a series of benzodioxine methyl piperidine derivatives as highly potent and selective α2C antagonists by ligand design to improve the pharmacokinetics of a previous candidate molecule.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d11c0582b9e57eabdf758db92785f82e
https://doi.org/10.1016/j.bmcl.2022.128783
https://doi.org/10.1016/j.bmcl.2022.128783
Autor:
Arto Tolvanen, Jouko Yliruusi, Saara Tiittanen, Karjalainen Arto Johannes, Mäkelä Mikko, David Din Belle, Veli Pekka Tanninen, Anna Shevchenko, Jorma Haarala, Inna Miroshnyk
Publikováno v:
Organic Process Research & Development. 15:666-672
The need for effective solid-form screening approaches, especially designed for the early discovery phases, is well recognized within the pharmaceutical industry. Here we report on the early polymorphism and solvatomorphism evaluation of a new drug c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::8e7ec0bf8e5c63090aedac750bf1c973
https://doi.org/10.1021/op200026f
https://doi.org/10.1021/op200026f
Publikováno v:
Tetrahedron. 54:14845-14858
19S-Hydroxytacamine (3) and 19R-hydroxytacamine (4) were prepared from cis hydroxyesters 7 and 8 via corresponding O-TMS esters 9 and 22. Comparison of the spectral data of isomers 3 and 4 with those of 19-hydroxytacamine from Tabernaemontana eglandu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::114a68bd36842fcb603063af0f806572
https://doi.org/10.1016/s0040-4020(98)00921-1
https://doi.org/10.1016/s0040-4020(98)00921-1
Publikováno v:
Tetrahedron. 54:4673-4678
Intramolecular aldol condensation of ketoaldehyde 8 affords three new compounds: enone 9 , hydroxyketone 10 , and enone 11 . Enone 9 possesses the ring system of (−)-voaketone ( 1 ), which is a skeletal rearrangement product of the indole alkaloid
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::4d5a9f87f11fc634fe4ba3bf7f986e7b
https://doi.org/10.1016/s0040-4020(98)00184-7
https://doi.org/10.1016/s0040-4020(98)00184-7
Publikováno v:
Tetrahedron. 54:157-164
Base-catalysed epimerization of the easily accessible trans ester 3 at C-1 gives rise in good yield to the seemingly less stable cis ester 2, which can be converted into the indole alkaloid tacamonine (1) in three steps.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::92b5299c66377c5409aa8f1bd16bf079
https://doi.org/10.1016/s0040-4020(97)10266-6
https://doi.org/10.1016/s0040-4020(97)10266-6
Publikováno v:
Tetrahedron. 52:11361-11378
Total syntheses are described for seven tacamine-type indole alkaloids (1–7) found in Tabernaemontana eglandulosa. (±)-Tacamine (1), (±)-16-epitacamine (2), and (±)-apotacamine (3) were prepared from pentacyclic intermediates 18. Apotacamine (3)
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c4273167bdc97ac9320dac1e6a6b8365
https://doi.org/10.1016/0040-4020(96)00663-1
https://doi.org/10.1016/0040-4020(96)00663-1
Publikováno v:
Tetrahedron Letters. 37:1513-1516
Methyl 3α-1,2,3,4,6,7,12,12bβ-cotahydroindolo[2,3- a ]quinolizine-1α-carboxylate ( 6 ), a key intermediate for the synthesis of tacamine-type indole alkaloids, was prepared in six simple steps from methyl 5-(1′-hydroxyethyl)nicotinate ( 7 ). The
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::1c904367f9a61392e07073e58ab90d11
https://doi.org/10.1016/0040-4039(96)00052-4
https://doi.org/10.1016/0040-4039(96)00052-4
Publikováno v:
Tetrahedron Letters. 36:7141-7144
A simple and efficient method is described for the preparation of tacamonine (1) from the easily accessible ester 3. The method is based on the stereoselective synthesis of 20-epitacamonine (7), which is transformed to 1 using the Polonovski-Potier r
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::bd4d20aa403a09773ee7ebf30cf8a853
https://doi.org/10.1016/0040-4039(95)01419-i
https://doi.org/10.1016/0040-4039(95)01419-i
Publikováno v:
Tetrahedron Letters. 35:6151-6154
The mixture of pentacyclic intermediates ( 4 ) was successfully converted into the pharmacologically interesting indole alkaloid (±)-tacamine ( 1 ). In a similar manner, the two unnatural isomers of 1 , (±)-14-epitacamine ( 9 ) and (±)-14-epi-16-e
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::9c5d62cd55158800b61e4c2afb884790
https://doi.org/10.1016/0040-4039(94)88102-2
https://doi.org/10.1016/0040-4039(94)88102-2