《New antiparasitic flexible triaryl diamidines, their prodrugs and aza analogues: Synthesis, in vitro and in vivo biological evaluation, and molecular modelling studies》 was written by Arafa, Reem K.; Ismail, Mohamed A.; Wenzler, Tanja; Brun, Reto; Paul, Ananya; Wilson, W. David; Alakhdar, Amira A.; Boykin, David W.. Recommanded Product: 2,6-DibromopyridineThis research focused ontriaryl diamidine prodrug preparation SAR antimalarial antitrypanosomal; Antimalarial; Antitrypanosomal; Flexible diamidines; Minor groove binders; Molecular dynamics; Triaryl dications. The article conveys some information:
Dicationic diamidines have been well established as potent antiparasitic agents with proven activity against tropical diseases like trypanosomiasis and malaria. This work presents the synthesis of new mono and diflexible triaryl amidines their aza analogs and resp. methoxyamidine prodrugs. All diamidines were assessed in vitro against Trypanosoma brucei rhodesiense (T. b. r.) and Plasmodium falciparum (P. f.) where they displayed potent to moderate activities at the nanomolar level with IC50s = 11 – 378 nM for T. b. r. and 4 – 323 nM against P. f.. In vivo efficacy testing against T. b. r. STIB900 has shown the monoflexible diamidine 2-(4′-Amidinophenyl)-5-(4”-amidinobenzyl)pyridine acetate salt as the most potent derivative in this study eliciting 4/4 cures of infected mice for a treatment period of >60 days upon a 4 x 5 mg/kg dose i. p. treatment. Moreover, thermal melting anal. measurement ΔTm for this series of diamidines/poly (dA-dT) complexes fell between 0.5 and 19° with the above compound showing the highest binding to the DNA minor groove. Finally, a 50 ns mol. dynamics study of an AT-rich DNA dodecamer with the above compound revealed a strong binding complex supported by vdW and electrostatic interactions. The results came from multiple reactions, including the reaction of 2,6-Dibromopyridine(cas: 626-05-1Recommanded Product: 2,6-Dibromopyridine)
2,6-Dibromopyridine(cas: 626-05-1) belongs to pyridine. Pyridine-based materials are valued for their optical and physical properties as well as their medical potential. Additionally, pyridine-based natural products continue to be discovered and studied for their properties and to understand their biosynthesis.Recommanded Product: 2,6-Dibromopyridine