An appraisal of anti-mycobacterial activity with structure-activity relationship of piperazine and its analogues: A review

Girase, Pankaj S.; Dhawan, Sanjeev; Kumar, Vishal; Shinde, Suraj; Palkar, Mahesh B.; Karpoormath, Rajshekhar

doi:10.1016/j.ejmech.2020.112967

Cited by 43 publications

(19 citation statements)

References 88 publications

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“…Lipid-based carriers are efficient in siRNA delivery [ 85 ]. Piperazine is frequently utilized in bioactive compounds and medicine [ 86 , 87 ]. A recent study reported that piperazine-containing ionizable lipid (Pi-Lipids) favorably deliver genes to immune cells in vivo without targeting the ligand [ 86 ].…”

Section: Breast Cancer Therapy With Biopolymer-based Sirna Nanoplatformmentioning

confidence: 99%

Biopolymer-Based Nanosystems for siRNA Drug Delivery to Solid Tumors including Breast Cancer

Subhan

Torchilin

2023

Pharmaceutics

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Nanobiopolymers such as chitosan, gelatin, hyaluronic acid, polyglutamic acid, lipids, peptides, exosomes, etc., delivery systems have prospects to help overwhelmed physiological difficulties allied with the delivery of siRNA drugs to solid tumors, including breast cancer cells. Nanobiopolymers have favorable stimuli-responsive properties and therefore can be utilized to improve siRNA delivery platforms to undruggable MDR metastatic cancer cells. These biopolymeric siRNA drugs can shield drugs from pH degradation, extracellular trafficking, and nontargeted binding sites and are consequently suitable for drug internalization in a controlled-release fashion. In this review, the utilization of numerous biopolymeric compounds such as siRNA drug delivery systems for MDR solid tumors, including breast cancers, will be discussed.

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Section: Breast Cancer Therapy With Biopolymer-based Sirna Nanoplatformmentioning

confidence: 99%

Biopolymer-Based Nanosystems for siRNA Drug Delivery to Solid Tumors including Breast Cancer

Subhan

Torchilin

2023

Pharmaceutics

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“…The Resazurin method was used to assess the MIC of the synthesized 5(a-l) analogs. MRSA resistance was tested using the parent structure piperazine and phthalimide 28 . The 5e has a remarkable MIC value of 45±0.15 µg/mL, which was validated by streptomycin and bacitracin 10 g/mL, which are both broad-spectrum antibiotics (Table 3).…”

Section: Antibacterial Activity Of Piperazine Derivatives Against Mrsamentioning

confidence: 99%

Design, synthesis, and anti-bacterial activities of piperazine based phthalimide derivatives against superbug-Methicillin-Resistant Staphylococcus aureus

Prasad¹,

Ananda²,

Mukarambi³

et al. 2023

10.5267/j.ccl

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A series of piperazine-based phthalimide derivatives 5 (a-l) were synthesized and extensively characterized using a variety of spectrum methods, including LC-MS, 1H-NMR, 13C-NMR, and FT-IR. All the derivatives were examined for their physicochemical, pharmacokinetic, bio-activity score, and PASS analysis. The 5e piperazine-based phthalimide derivative demonstrated promising antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA) in the in vitro antibacterial studies. In comparison to streptomycin and bacitracin (10 µg/mL), the minimum inhibitory concentration of 5e against MRSA was discovered to be 45±0.15 micro g/ml. The anti-MRSA activity was validated with membrane damage studies by using SEM, and in silico docking studies were against 3VMT and 6FTB proteins of MRSA. In the toxicity study, 5e derivatives were evaluated against L6 cell lines. The results of the studies show the synthesized 2-(2-(4-((4-chlorophenyl) sulfonyl) piperazin-1-yl) ethyl) isoindoline-1,3-dione (5e) can be used for the development of anti-MRSA drugs.

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“…12, 23 , antimycobacterial (Ciprofloxacin, Norfloxacin) 24 , promising Scaffold with Analgesic and Antiinflammatory Potential 25 .…”

Section: Hmentioning

confidence: 99%

Untitled

2022

IJPSR

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Substituted quinoxaline has received considerable attention during the last few years as they are endowed with various biological activities and have a wide range of therapeutic properties. Piperazine has proven its worth in numerous clinically active drugs broader areas of therapeutic index. Hence, biologically important quinoxaline derivatives containing a piperazine moiety and Schiff base scaffolds were prepared. The structures of the synthesized compounds were characterised by elemental analysis, IR, NMR, and Mass spectra. All the prepared derivatives were screened for antibacterial and antifungal activity by disc diffusion method using nutrient agar media against Bacillus subtilis, Bacillus pumilus, Escherichia coli and Pseudomonas aeruginosa, & potato dextrose agar medium for activity against Aspergillus niger and Candida albicans using ciprofloxacin as a standard for antibacterial and clotrimazole as a standard for antifungal activity respectively. Fluoro and trimethoxy-containing derivatives have shown promising activity against gram-ve bacteria P. aeruginosa. Some compounds have shown moderate antifungal and antibacterial activity. INTRODUCTION:Quinoxaline derivatives are an important class of heterocyclic compounds, formed by replacing carbon atoms in naphthalene ring with an N atom. Quinoxaline consists of two rings, one aromatic benzene ring, and another heterocyclic aromatic pyrazine ring because of which this is also called benzopyrazine. It is recognized as a bioisoster of quinoline, naphthalene and benzothiophene. Quinoxaline has occupied an enormous focus against biologically important broad-spectrum bacteria, fungi, viruses, leishmania, tuberculosis, malaria, cancer, depression, and neurological activities.

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An appraisal of anti-mycobacterial activity with structure-activity relationship of piperazine and its analogues: A review

Cited by 43 publications

References 88 publications

Biopolymer-Based Nanosystems for siRNA Drug Delivery to Solid Tumors including Breast Cancer

Biopolymer-Based Nanosystems for siRNA Drug Delivery to Solid Tumors including Breast Cancer

Design, synthesis, and anti-bacterial activities of piperazine based phthalimide derivatives against superbug-Methicillin-Resistant Staphylococcus aureus

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