- Microwave assisted synthesis, docking and antimalarial evaluation of hybrid PABA-substituted 1,3,5-triazine derivatives
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A series of novel PABA-substituted 1,3,5-triazine derivatives were developed via microwave assisted synthesis and subsequently tested for antimalarial activity against chloroquine sensitive 3D7 strain of Plasmodium falciparum using chloroquine as standard. Antimalarial screening result showed that synthesized compounds exhibited IC50 in the range of 4.46 to 79.72 μg mL?1. Among the tested compounds, 4c and 4f showed significant antimalarial activity with low binding energies (BE) -172.32 and 160.41 kcal mol?1 via interacting with Arg122 through the involvement of COOH of the phenyl linked to 1,3,5-triazine. In conclusion, these core scaffolds can be used for future antimalarial drug development.
- Adhikari, Nayana,Kashyap, Ankita,Shakya, Anshul,Ghosh, Surajit Kumar,Bhattacharyya, Dibya Ranjan,Bhat, Hans Raj,Singh, Udaya Pratap
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p. 2389 - 2399
(2020/03/24)
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- Novel functionalized melamine-based nitroheterocycles: Synthesis and activity against trypanosomatid parasites
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Human African trypanosomiasis (HAT), caused by the protozoan parasite Trypanosoma brucei spp., is a major health problem in sub-Saharan Africa. New drugs are urgently required for the disease. Selective uptake of toxic compounds into trypanosomes has been achieved by exploiting plasma membrane transporters. For example, the P2 aminopurine transporter, along with other transporters, selectively concentrates melamine and benzamidine moieties into trypanosomes. We have previously reported the use of the melamine motif to selectively target nitrofuran to the trypanosome. In this paper we report the further investigation of the structure activity relationships and the effect of the introduction of different functionalized substituents onto the melamine unit. Most of the compounds tested in vitro for their trypanocidal activity showed activities in the submicromolar range against T. b. rhodesiense. The Royal Society of Chemistry 2009.
- Baliani, Alessandro,Peal, Valerie,Gros, Ludovic,Brun, Reto,Kaiser, Marcel,Barrett, Michael P.,Gilbert, Ian H.
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supporting information; experimental part
p. 1154 - 1166
(2009/05/30)
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- Thermodynamic stabilities of linear and crinkled tapes and cyclic rosettes in melamine-cyanurate assemblies: A model description
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In this paper we describe model calculations for the self-assembly of N,N-disubstituted melamines 1 and N-substituted cyanuric acid or 5,5-disubstituted barbituric acid derivatives 2 into linear or crinkled tapes and cyclic rosettes via cooperative hydrog
- Bielejewska,Marjo,Prins,Timmerman,De Jong,Reinhoudt
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p. 7518 - 7533
(2007/10/03)
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- Method for modifying 1,3,5-triazine derivatives
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PCT No. PCT/JP96/03762 Sec. 371 Date Jun. 22, 1998 Sec. 102(e) Date Jun. 22, 1998 PCT Filed Dec. 24, 1996 PCT Pub. No. WO97/24338 PCT Pub. Date Jul. 10, 1997A method for modifying 1,3,5-triazine derivatives characterized by heating and reacting a 1,3,5-triazine derivatives having at least one amino or mono-substituted amino group on a carbon atom or atoms on its ring with an alcohol in the presence of a metal catalyst and a hydrogen atom to introduce an alkyl group or an alkenyl group into each amino or mono-substituted amino group; another method for modifying 1,3,5-triazine derivatives characterized by heating and reacting a 1,3,5-triazine derivatives having at least one amino or mono-substituted amino group on a carbon atom or atoms on its ring with a dihydric alcohol in the presence of a metal catalyst and a hydrogen atom to introduce an alkyl group having a hydroxyl group into each amino or mono-substituted amino group; and 1,3,5-triazine derivatives obtained by the methods. The various modified sustituted 1,3,5-triazine derivatives thus produced are generally obtained as a mixture. These derivatives can be isolated as compounds having high-purity by a normal separation method for organic compounds, and the compounds are usable in the various applications mentioned in the specification.
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