Synthesis of novel piperazine tethered benzocycloheptenone hybrids and their antimicrobial evaluation

Prameela, Subhashini Naikal James; Jilla, Lavanya; Vanguru, Sowmya

doi:10.1002/jhet.3778

Cited by 4 publications

(1 citation statement)

References 27 publications

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“…Due to its facile ability to form hydrogen and ionic bonds, it is frequently incorporated as a pivotal moiety in drug design for the purpose of modulating the biological activity of the parent scaffold [24]. The investigation of piperazine in the realm of pesticides primarily focuses on its antiviral [25][26][27][28], antibacterial [29][30][31][32][33], and insecticidal [34][35][36][37] properties. In the antiviral field, piperazine has spawned a number of commercial drugs with excellent antiviral activity, such as fleroxacin, flunarizine, and sparfloxacin (Figure 1).…”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis, and Anti-PVY Biological Activity of 1,3,5-Triazine Derivatives Containing Piperazine Structure

Bai

Wei

Zhang

et al. 2023

IJMS

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In this study, a commercial agent with antivirus activity and moroxydine hydrochloride were employed to perform a lead optimization. A series of 1,3,5-triazine derivatives with piperazine structures were devised and synthesized, and an evaluation of their anti-potato virus Y (PVY) activity revealed that several of the target compounds possessed potent anti-PVY activity. The synthesis of compound C35 was directed by a 3D-quantitative structure–activity relationship that used the compound’s structural parameters. The assessment of the anti-PVY activity of compound C35 revealed that its curative, protective, and inactivation activities (53.3 ± 2.5%, 56.9 ± 1.5%, and 85.8 ± 4.4%, respectively) were comparable to the positive control of ningnanmycin (49.1 ± 2.4%, 50.7 ± 4.1%, and 82.3 ± 6.4%) and were superior to moroxydine hydrochloride (36.7 ± 2.7%, 31.4 ± 2.0%, and 57.1 ± 1.8%). In addition, molecular docking demonstrated that C35 can form hydrogen bonds with glutamic acid at position 150 (GLU 150) of PVY CP, providing a partial theoretical basis for the antiviral activity of the target compounds.

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Section: Introductionmentioning

confidence: 99%

Design, Synthesis, and Anti-PVY Biological Activity of 1,3,5-Triazine Derivatives Containing Piperazine Structure

Bai

Wei

Zhang

et al. 2023

IJMS

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Design, Synthesis, Computational Study, and Biological Evaluation of Sulfonyl Tethered Piperazine Derivatives as Antimicrobial Agents

Thopate,

Dhawale,

Kawale

et al. 2024

ChemistrySelect

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Piperazine, a nitrogen‐containing heterocyclic compound, has potential in medical chemistry due to its versatile structure and ease of modification. Therefore, researchers have designed novel piperazine derivatives with various biological activities, including antiviral, antibacterial, and antifungal properties. In this study, a new series of 2‐(4‐((5‐bromo‐2‐methoxyphenyl)sulfonyl) piperazine‐1‐yl) acetamide derivatives (7a‐l) were synthesized and their structures were identified using 1H‐NMR, 13C‐NMR, and HRMS spectroscopic methods. The in vitro antimicrobial activity of these compounds was tested against four bacterial strains and two fungi strains. Some of the sulfonyl piperazine derivatives (7d, 7e, 7f, 7j, 7k, and 7l) exhibited relatively good antimicrobial and antifungal activities compared to standard drugs. Further analysis using computational docking confirmed strong binding interactions, aligning with our results. Our compounds exhibited improved potency compared to existing standard treatments.

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Discovery of novel, potent and orally available benzoazipinone derivatives that elicit MKLP2-inhibitory phenotypes

Huang,

Zhang,

Kalashova

et al. 2024

European Journal of Medicinal Chemistry Reports

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Synthesis of novel piperazine tethered benzocycloheptenone hybrids and their antimicrobial evaluation

Cited by 4 publications

References 27 publications

Design, Synthesis, and Anti-PVY Biological Activity of 1,3,5-Triazine Derivatives Containing Piperazine Structure

Design, Synthesis, and Anti-PVY Biological Activity of 1,3,5-Triazine Derivatives Containing Piperazine Structure

Design, Synthesis, Computational Study, and Biological Evaluation of Sulfonyl Tethered Piperazine Derivatives as Antimicrobial Agents

Discovery of novel, potent and orally available benzoazipinone derivatives that elicit MKLP2-inhibitory phenotypes

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