3.8 Article

Synthesis, Free Radical Scavenging Activity, Antimicrobial And Molecular Docking Studies Of Novel Pyrazine 2-Carboxylic Acid Derivatives Of Piperazines

出版社

RJPBCS RESEARCH JOURNAL PHARMACEUTICAL, BIOLOGICAL & CHEMICAL SCIENCES

关键词

Antioxidant; Antimicrobial; Coupling reagent; Pyrazine-2-carboxylic acid; Piperazines; T3P

资金

  1. Department of Science and Technology (DST) [SERB/F/3690/2013-14]

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A novel series of pyrazine-2-carboxylic acid derivatives were synthesized using substituted pyrazine 2carboxylic acids with various piperazines in the presence of T3P (propyl phosphonic anhydride) as a coupling reagent. The synthetic approach, a possible reaction mechanism and the analytical data of the synthesized compounds are presented and these compounds were analyzed using M.P, LC-MS, (HNMR)-N-1, and FT-IR. Further, the synthesized compounds were evaluated for their antioxidant (ABTS and DPPH method) and antimicrobial activities(agar well diffusion method) Among the synthesized pyrazine-2-carboxylic acid derivatives (3-aminopyrazin-2-yl)(4-(6-aminopyrimidin-4-yl)piperazin-1-yl) methanone (P10) exhibited good antioxidant activity as well as moderate antimicrobial activity where in, (4-(6-aminopyrimidin-4-yl)piperazin-1-yl)(5-methylpyrazin-2-yl) methanone (P4) depicted highest antimicrobial activity alone. In molecular docking studies, although all the molecules showed good inhibition with GlcN-6-P synthase, the P4 showed higher docking score. So, it can be predicted as inhibition of GlcN-6-P synthase may be responsible for antibacterial activity of the synthesized piperazine derivatives. The results obtained prompt us in further studies for characterizing these derivatives for their diverse biological activities.

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