Discovery, Synthesis, and Bioactivity of Bis(heteroaryl)piperazines. 1. A Novel Class of Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors was written by Romero, Donna L.;Morge, Raymond A.;Biles, Carolyn;Berrios-Pena, Norman;May, Paul D.;Palmer, John R.;Johnson, Paul D.;Smith, Herman W.;Busso, Mariano. And the article was included in Journal of Medicinal Chemistry in 1994.Reference of 87394-48-7 This article mentions the following:
A variety of analogs of U-80493E (I) were synthesized and evaluated for their inhibition of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT). Replacement of the substituted aryl moiety with various substituted indoles provided bis(heteroaryl)piperazines (BHAPs) that were 10-100-fold more potent than U-80493E. The pyridyl portion of the lead mol. was found to be very sensitive to modifications. Extensive preclin. evaluations of several of these compounds led to the selection of U-87201E (atevirdine mesylate) (II) for clin. evaluation. In the experiment, the researchers used many compounds, for example, 1-(3-Nitropyridin-2-yl)piperazine (cas: 87394-48-7Reference of 87394-48-7).
1-(3-Nitropyridin-2-yl)piperazine (cas: 87394-48-7) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Reference of 87394-48-7
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics