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.).
High efficiency two-photon uncaging coupled by the correction of spontaneous hydrolysis
Pálfi, Dénes,Chiovini, Balázs,Szalay, Gergely,Kaszás, Attila,Turi, Gergely F.,Katona, Gergely,ábrányi-Balogh, Péter,Szori, Milán,Potor, Attila,Frigyesi, Orsolya,Lukácsné Haveland, Csilla,Szadai, Zoltán,Madarász, Miklós,Vasanits-Zsigrai, Anikó,Molnár-Perl, Ibolya,Viskolcz, Béla,Csizmadia, Imre G.,Mucsi, Zoltán,Rózsa, Balázs
, p. 1958 - 1970 (2018/03/23)
Two-photon (TP) uncaging of neurotransmitter molecules is the method of choice to mimic and study the subtleties of neuronal communication either in the intact brain or in slice preparations. However, the currently available caged materials are just at the limit of their usability and have several drawbacks. The local and focal nature of their use may for example be jeopardized by a high spontaneous hydrolysis rate of the commercially available compounds with increased photochemical release rate. Here, using quantum chemical modelling we show the mechanisms of hydrolysis and two-photon activation, and synthesized more effective caged compounds. Furthermore, we have developed a new enzymatic elimination method removing neurotransmitters inadvertently escaping from their compound during experiment. This method, usable both in one and two-photon experiments, allows for the use of materials with an increased rate of photochemical release. The efficiency of the new compound and the enzymatic method and of the new compound are demonstrated in neurophysiological experiments.
