78449-75-9Relevant academic research and scientific papers
The novel preparation methods of 5-substituted methyl-1 -azabicyclo[3.3.0]octane
Oka, Mitsuru,Baba, Kunihisa,Suzuki, Tomoo,Matsumoto, Yukiharu
, p. 2317 - 2320 (1997)
5-Substituted methyl-1-azabicyclo[3.3.0]octane, which is a useful intermediate for drugs, was readily synthesized from 1,7-dichloro-4-heptanone without isolating unstable intermediates.
Pyrrolizidines for direct air capture and CO2 conversion
Hanusch, Jan M.,Kerschgens, Isabel P.,Huber, Florian,Neuburger, Markus,Gademann, Karl
, p. 949 - 952 (2019/01/23)
Greenhouse gases such as CO2 strongly contribute to the rising temperatures of our planet, but as long as our society is dependent on fossil fuels, this trend will even increase in the near future. Therefore, CO2 capture and subseque
Antimalarial activity of novel pyrrolizidinyl derivatives of 4-aminoquinoline
Sparatore, Anna,Basilico, Nicoletta,Casagrande, Manolo,Parapini, Silvia,Taramelli, Donatella,Brun, Reto,Wittlin, Sergio,Sparatore, Fabio
scheme or table, p. 3737 - 3740 (2009/04/06)
Two pyrrolizidinylalkyl derivatives of 4-amino-7-chloroquinoline (MG2 and MG3) were prepared and tested in vitro against CQ-sensitive and CQ-resistant strains of Plasmodium falciparum and in vivo in a Plasmodium berghei mouse model of infection. Both compounds exhibited excellent activity in all tests and low toxicity against mammalian cells. Preliminary studies of the acute toxicity and of the metabolism of the most active compound MG3 indicate a promising profile as a new antimalarial drug candidate.
Synthesis and muscarinic activity of a series of quinolines and naphthalenes with a 1-azabicyclo[3.3.0]octane moiety
Suzuki, Tomoo,Usui, Toshinao,Oka, Mitsuru,Suzuki, Tsunemasa,Kataoka, Tadashi
, p. 1265 - 1273 (2007/10/03)
In order to discover a medicine effective against Alzheimer's disease, we synthesized a series of quinoline derivatives having a characteristic 1- azabicyclo[3.3.0]octane amine ring, and performed pharmacological evaluation of them. Acetylcholine esterase inhibitory activities of these derivatives were unexpectedly weak. Tests for central nervous muscarinic cholinergic receptor binding affinity indicated that these compounds had higher affinities to muscarinic M1 receptors than to M2 receptors. A series of naphthalene derivatives substituted with the 1-azabicyclo[3.3.0]octane ring were also synthesized and muscarinic M1 and M2 receptor binding affinity determined. These compounds had much higher affinity for M1 receptors than the quinoline derivatives, and 1-[N-(1-azabicyclo[3.3.0]octan-5-yl)methyl-N- methylamino]-4-nitronaphthalene showed the highest affinity and selectivity. The ability of this compound to improve cognitive function was assessed using the passive avoidance test in scopolamine-induced mice.
5-HT3 receptor agonist, novel thiazole derivative and intermediate thereof
-
, (2008/06/13)
A 5-HT3 receptor against containing a thiazole derivative as the effective ingredient is provided and is represented by the Formula (I): STR1 wherein the A ring is substituted or unsubstituted and represents a benzene or a heterocyclic ring with one or two heteroatoms; one of L1 or L2 represents a single bond and the other is non-existent or represents an alkylene or alkenylene group; R represents: STR2
N-[2-(1-azabicyclo[3.3.0]octan-5-YL)ethyl]-2-nitroaniline, a potent muscarinic agonist
Suzuki,Oka,Maeda,Furusawa,Mitani,Kataoka
, p. 1218 - 1220 (2007/10/03)
The muscarine receptor agonist SK-946, an aniline derivative with a characteristic bicyclo amine, was found. We describe a new synthetic method for 1-azabicyclo[3.3.0]octane and describe the biological activity of SK- 946.
Antivirally active N-cycloalkyl alkanol compounds
-
, (2008/06/13)
The compounds are of the general formula or where R1 is -OH, amino or -SH, R2 is H, α- or β-naphthyl or optionally substituted phenyl, R3 is mono-, di- or tricycloalkyl of C6-16, optionally substituted, R4
A NEW ROUTE TO 8-SUBSTITUTED PYRRAZOLIZIDINES
Miyano, Seiji,Yamashita, Osamu,Fujii, Shinichiro,Somehara, Takao,Sumoto, Kunihiro
, p. 755 - 758 (2007/10/02)
A new route to 8-substituted pyrrazolizidines starting with Δ4(8)-dehydropyrrolizidinium perchlorate is described.
