177937-60-9Relevant articles and documents
Tetraazamacrocyclic derivatives and their metal complexes as antileishmanial leads
Hubin, Timothy J.,Walker, Ashlie N.,Davilla, Dustin J.,Carder Freeman, TaRynn N.,Epley, Brittany M.,Hasley, Travis R.,Amoyaw, Prince N.A.,Jain, Surendra,Archibald, Stephen J.,Prior, Timothy J.,Krause, Jeanette A.,Oliver, Allen G.,Tekwani, Babu L.,Khan, M. Omar F.
, p. 42 - 53 (2019/03/04)
A total of 44 bis-aryl-monocyclic polyamines, monoaryl-monocyclic polyamines and their transition metal complexes were prepared, chemically characterized, and screened in vitro against the Leishmania donovani promastigotes, axenic amastigotes and intracellular amastigotes in THP1 cells. The IC50 and/or IC90 values showed that 10 compounds were similarly active at about 2-fold less potent than known drug pentamidine against promastigotes. The most potent compound had an IC50 of 2.82 μM (compared to 2.93 μM for pentamidine). Nine compounds were 1.1–13.6-fold more potent than pentamidine against axenic amastigotes, the most potent one being about 2-fold less potent than amphotericin B. Fourteen compounds were about 2–10 fold more potent than pentamidine, the most potent one is about 2-fold less potent than amphotericin B against intracellular amastigotes in THP1 cells. The 2 most promising compounds (FeL7Cl2 and MnL7Cl2), with strong activity against both promastigotes and amastigotes and no observable toxicity against the THP1 cells are the Fe2+- and Mn2+-complexes of a dibenzyl cyclen derivative. Only 2 of the 44 compounds showed observable cytotoxicity against THP1 cells. Tetraazamacrocyclic monocyclic polyamines represent a new class of antileishmanial lead structures that warrant follow up studies.
NOVEL NITROGEN-CONTAINING COMPOUND OR SALT THEREOF, OR METAL COMPLEX THEREOF
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, (2016/08/17)
The present invention provides a compound represented by the formula (1) or a salt thereof, or a complex of the compound or the salt with a metal, in the formula (1), A1 represents a chelate group; R1 represents a hydrogen atom or the like; R2 represents a hydrogen atom or the like; and Z1, Z2, Z3, Z4, and Z5 are the same or different and each represent a nitrogen atom or CR3 or the like wherein R3 represents a hydrogen atom or an optionally substituted C1-6 alkyl group or the like; L1 represents a group represented by the formula (3) wherein R13, R14, R15, and R16 are the same or different and each represent a hydrogen atom or the like; L2 represents an optionally substituted C1-6 alkylene group; and L3 represents an optionally substituted C1-6 alkylene group.
Lanthanide(III) complexes with a reinforced cyclam ligand show unprecedented kinetic inertness
Rodrguez-Rodrguez, Aurora,Esteban-G?mez, David,Tripier, Raphal,Tircs?, Gyula,Garda, Zoltn,T?th, Imre,De Blas, Andrs,Rodrguez-Blas, Teresa,Platas-Iglesias, Carlos
supporting information, p. 17954 - 17957 (2015/03/13)
Lanthanide(III) complexes of a cross-bridged cyclam derivative containing two picolinate pendant arms are kinetically inert in very harsh conditions such as 2 M HCl, with no dissociation being observed for at least 5 months. Importantly, the [Ln(dota)]su
