4837-90-5Relevant articles and documents
CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs
Lebar, Matthew D.,Hahn, Kristopher N.,Mutka, Tina,Maignan, Patrick,McClintock, James B.,Amsler, Charles D.,Van Olphen, Alberto,Kyle, Dennis E.,Baker, Bill J.
, p. 5756 - 5762 (2011)
The marine invertebrate-derived meridianin A, the originally proposed structure for psammopemmin A, and several related 3-pyrimidylindole analogs were synthesized and subsequently investigated for central nervous system, antimalarial, and cytotoxic activity. A Suzuki coupling of an indoleborate ester to the pyrimidine electrophile was utilized to form the natural product and derivatives thereof. The 3-pyrimidineindoles were found to prevent radioligand binding to several CNS receptors and transporters, most notably, serotonin receptors (i for 5HT2B). Two compounds also inhibited the human malaria parasite Plasmodium falciparum (IC50 50 = 15 μM).
Potassium tert-Butoxide-Promoted Acceptorless Dehydrogenation of N-Heterocycles
Liu, Tingting,Wu, Kaikai,Wang, Liandi,Yu, Zhengkun
supporting information, p. 3958 - 3964 (2019/08/01)
Potassium tert-butoxide-promoted acceptorless dehydrogenation of N-heterocycles was efficiently realized for the generation of N-heteroarenes and hydrogen gas under transition-metal-free conditions. In the presence of KOtBu base, a variety of six- and five-membered N-heterocyclic compounds efficiently underwent acceptorless dehydrogenation to afford the corresponding N-heteroarenes and H2 gas in o-xylene at 140 °C. The present protocol provides a convenient route to aromatic nitrogen-containing compounds and H2 gas. (Figure presented.).
A indole compound and its preparation method and application (by machine translation)
-
Paragraph 0131; 0132; 0133, (2018/10/02)
The invention discloses a indole compound and its preparation method and application. The indole compounds of the structural formula such as formula (I) is shown. The indoles, rice galenical demonstrate the excellent inhibitory activity, the effect of most of the compound is obviously better than the positive control drug validamycin; especially compound I - 43, I - 44, I - 54, I - 73, II - 7 and II - 17, its galenical very good living body protection and treating effect, effect is better than the positive control; more specifically, compound I - 43 of the rice sheath blight bacteriostatic activity than validamycin activity is improved by nearly 300 times. The indole compounds in the prevention and/or treatment of rice sheath blight has great application prospects. In addition the compound of the invention is simple in construction, the preparation method is simple, and is suitable for large-scale industrial production. (I). (by machine translation)