New antifilarial agents. 1. Epoxy sulfonamides and ethynesulfonamides was written by Brienne, Marie Josephe;Varech, Daniel;Leclercq, Martine;Jacques, Jean;Radembino, Nathalie;Dessalles, Christine;Mahuzier, Georges;Gueyouche, Chantal;Bories, Christian. And the article was included in Journal of Medicinal Chemistry in 1987.SDS of cas: 21867-64-1 This article mentions the following:
Two series of 2-substituted 1,2-epoxyethanesulfonamides I (R = Me, R1 = Ph, substituted Ph, Me; NR2 = morpholino, 4-methylpiperazinyl, etc.) and ethynesulfonamides, e.g., R2NSO2CCR1 (II, R2N = morpholino, 4-methylpiperazinyl, R1 = Ph) were synthesized and evaluated for their antifilarial activity. Trans-I were stereospecifically prepared by a Darzens reaction between aldehydes and halomethanesulfonamides. Cis-I were obtained from ethynesulfonamides II by semihydrogenation followed by KOCl epoxidation 2-Substituted ethynesulfonamides II were synthesized from appropriate trans-ethensulfonamides by bromination-dehydrobromination. These products, as well as several synthetic intermediates, were evaluated for antifilarial activity against Molinema dessetae either in vivo in its natural host, the rodent Proechimys oris, or in vitro by a new test using cultures of the infective larvae. Most of the trans–I and II bearing a 2-aryl substituent were active in vitro. trans–I (NR2 = morpholino, NMe2, 4-methylpiperazinyl; R1 = Ph, 3,4-Cl2C6H3) and PhCCSO2NR2 (NR2 = morpholino) showed marked macrofilaricidal activity in vivo without any microfilaricidal activity. The differences between the in vivo and in vitro results may be due, in part, to the low chem. stability of trans-I. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1SDS of cas: 21867-64-1).
1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. SDS of cas: 21867-64-1
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics