32998-04-2Relevant academic research and scientific papers
BICYCLIC COMPOUND AND USE THEREOF FOR INHIBITING SUV39H2
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Page/Page column 330; 333, (2017/08/01)
The present invention directs to a compound represented by formula (I).
Discrete assembly of synthetic peptide-DNA triplex structures from polyvalent melamine-thymine bifacial recognition
Zeng, Yingying,Pratumyot, Yaowalak,Piao, Xijun,Bong, Dennis
supporting information; experimental part, p. 832 - 835 (2012/03/07)
We have designed a 21-residue α-peptide that simultaneously recognizes two decadeoxyoligothymidine (dT10) tracts to form triplexes with a peptide-DNA strand ratio of 1:2. The synthetic peptide side chain displays 10 melamine rings, which provide a bifacial thymine-recognition interface along the length of the 21-residue peptide. Recognition is selective for thymine over other nucleobases and drives the formation of ternary peptide· [dT10]2 complexes as well as heterodimeric peptide· [dT10C10T10] hairpin structures with triplex stems.
Design and synthesis of a series of melamine-based nitroheterocycles with activity against trypanosomatid parasites
Baliani, Alessandro,Bueno, Gorka Jimenez,Stewart, Mhairi L.,Yardley, Vanessa,Brun, Reto,Barrett, Michael P.,Gilbert, Ian H.
, p. 5570 - 5579 (2007/10/03)
The parasites that give rise to human African trypanosomiasis (HAT) are auxotrophs for various nutrients from the human host, including purines. They have specialist nucleoside transporters to import these metabolites. In addition to uptake of purine nucleobases and purine nucleosides, one of these transporters, the P2 transporter, can carry melamine derivatives; these derivatives are not substrates for the corresponding mammalian transporters. In this paper, we report the coupling of the melamine moiety to selected nitro heterocycles with the aim of selectively delivering these compounds to the parasites. Some compounds prepared have similar in vitro trypanocidal activities as melarsoprol, the principal drug used against late-stage HAT, with 50% growth inhibitory concentrations in the submicromolar range. Selected compounds were also evaluated in vivo in rodent models infected with Trypanosoma brucei brucei and T. brucei rhodesiense and showed pronounced activity and in two cases were curative without overt signs of toxicity. Compounds were also tested against other trypanosomatid pathogens, Leishmania donovani and Trypanosoma cruzi, and significant activity in vitro was noted for T. cruzi against which various nitro heterocycles are already registered for use.
Novel pyrimidine and 1,3,5-triazine hypolipidemic agents
d'Atri,Gomarasca,Resnati,Tronconi,Scolastico,Sirtori
, p. 1621 - 1629 (2007/10/02)
New compounds were synthesized by changing the substituents of a trisubstituted pyrimidine, i.e., [[4-chloro-6-[(2,3-dimethylphenyl)amino]-2-pyrimidinyl]thio]acetic acid, a potent hypolipidemic agent, impaired, however, by a marked hepatomegaly-inducing effect. The structural variations led to the subsidence (14b, i.e., 4-chloro-2-(dimethylamino)-6-[(2,3-dimethylphenyl)amino]pyrimidine) or to the reduction (18b, [[4-chloro-6-[(2,3-dimethylphenyl)amino]-2-pyrimidinyl]amino]acetic acid) of said untoward effect but still maintained the hypolipidemic effect that, although markedly decreased, still proves significant for serum cholesterol and triglycerides (18b) or for serum triglycerides only (14b).
The Synthesis of Alkyl- and Aryl-Substituted 1,3,5-Triazines
Harris, Roger L. N.
, p. 623 - 634 (2007/10/02)
The reaction of chloromethyleneiminium salts with N-cyanoamidines provides a new and versatile route to alkyl- and aryl-substituted 1,3,5-triazines.Variation of substituents in the starting materials allows the synthesis of monoaryl-, diaryl-, alkyl-aryl- and certain mono- and di-alkyl-1,3,5-triazines bearing a variety of other substituents including hydrogen, chlorine and O-, S- and N-radicals.The generally good yields, ready availability of starting materials, and the scope and facility of the reaction make it the method of choice for the synthesis of 1,3,5-triazines with these substitution patterns.
