Delving into the Latest Updates on Piperazine with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Diethylenediamine, Piperazidine, Piperazime Phosphate

+ [8]

Target-

Action-

Mechanism-

Therapeutic Areas

Infectious DiseasesRespiratory Diseases

Active Indication

AscariasisCoughEnterobiasis

Inactive Indication-

Originator Organization

Sichuan Emeishan Pharmaceutical Co Ltd.

Active Organization

Sichuan Emeishan Pharmaceutical Co Ltd.

Chengdu Pharmaceutical Co. Ltd.

Inactive Organization-

License Organization-

Drug Highest PhaseApproved

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC4H10N2

InChIKeyGLUUGHFHXGJENI-UHFFFAOYSA-N

CAS Registry110-85-0

Marine biofouling is the natural accumulation of organisms on substrates that reside in rivers, lakes, and seas. To combat this issue, polymer-based coatings historically utilized tin or copper compounds, which, though effective, are also highly toxic. In this study, a series of functionalized toxicant-free PDMS-type polymers were designed with pH buffer and zwitterionic moieties for fouling inhibition. The water contact angles ranged from 41 to 98°, demonstrating significant differences in the wettability of the coated surfaces. XPS and SEM-EDS testing confirmed the surface presence of buffer and zwitterionic functional groups. Assays were carried out using both laboratory and field testing against an array of marine species to gain an understanding of how these buffered polymer coatings hold up in the environment and to measure their antifouling and fouling-release capabilities. The organisms used for testing were a diatom, Navicula incerta, and two types of tubeworms, spirorbid and nonspirorbid serpulids. Piperazine and piperazine zwitterionic-based coatings performed the best overall as antifouling and fouling-release materials. Preliminary biological assays suggest that hydrophobic zwitterion-functionalized siloxane-based polymers may have both preventative antibacterial and antifouling interactions with target species compared to previously studied hydrophobic materials.

15 Apr 2025·ACS Omega

Piperazine-Based Co(III), Ni(II), Cu(II), and Zn(II) Carbodithioate Complexes as Potential Anticancer Agent

Article

Author: Shukla, Alok ; Gupta, Seema ; Zewde, Berhanu ; Bharty, M. K. ; Pandey, Shivendra Kumar ; Acharya, Arbind ; Butcher, Raymond John ; Jha, Shalini

The development of facile and cost-effective anticancer metallodrugs possessing minimal side effects is urgently needed. Piperazine-containing anticancer drugs are already available on the market. A piperazine-based potassium 4-(ethoxycarbonyl)piperazine-1-carbodithioate [pecpcdt] (L) ligand and its metal complexes [Co(ecpcdt)₃] (1), [Ni(ecpcdt)₂] (2), [Cu(ecpcdt)₂] (3), and [Zn(ecpcdt)₂] (4) were synthesized. These compounds were characterized by different spectroscopic methods and single-crystal X-ray crystallography data. Ni(II) and Cu(II) complexes have distorted square planar geometry, whereas the Co(III) complex has distorted octahedral geometry around the metal ions. Complexes are weakly fluorescent in the solution compared to the free ligand. The complexes were further examined for their in vitro anticancer activities against the primary Dalton's lymphoma (DL) cells along with standard drug cisplatin. The anticancer studies of metal complexes have been performed through various biochemical assays, and the findings thus obtained suggest that they demonstrate an effective anticancer activity. [Co(ecpcdt)₃] (1) shows superior cytotoxicity against DL cells than complexes [Cu(ecpcdt)₂] (3), [Zn(ecpcdt)₂] (4), and cisplatin. The superiority preferences of these complexes follows [Co(ecpcdt)₃] (1) > [pecpcdt] > [Cu(ecpcdt)₂] (3) > [Ni(ecpcdt)₂] (2) > [Zn(ecpcdt)₂] (4). Further assays were performed on a cobalt(III) complex having the highest efficacy to gain insights into the mechanism of cell death and showed that reduced mitochondrial membrane potential and increased mitochondrial ROS production, highlighting mitochondrial-dependent apoptosis as the major mechanism for tumor cell death. On the other hand, the viability of normal splenocytes was minimally affected by the [Co(ecpcdt)₃] (1) treatment.

13 Mar 2025·ACS Medicinal Chemistry Letters

Novel Piperazine Derivatives as Selective Antagonists of GluN2B-Containing NMDARs under Acidic pH Conditions

Author: Li, Yinlong ; Liang, Steven H.

This highlight describes novel piperazine derivatives as negative allosteric modulators targeting GluN2B-containing N-methyl-d-aspartic acid receptors (NMDARs). These compounds exhibit enhanced binding affinities to GluN2B under acidic conditions. Additionally, their binding selectivity and pharmaceutical formulations are discussed.

100 Deals associated with Piperazine

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External Link

KEGG	Wiki	ATC	Drug Bank
D00807	Piperazine	P02CB01	DB00592

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Ascariasis	China	Sichuan Emeishan Pharmaceutical Co Ltd.	-
Cough	China	Chengdu Pharmaceutical Co. Ltd.	-
Enterobiasis	China	Sichuan Emeishan Pharmaceutical Co Ltd.	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


AAIC2016	Not Applicable	Cognitive Dysfunction	-	Novel Piperazine Derivatives	gpfomnieoc(qexbmulleo) = vuuqjjfuyd weyoaonbhm (ugsothndqj )	-	01 Jul 2016
NCT02083406 (CTgov)	Phase 1	Malaria	22	OZ439+960mg PQP (Treatment A: OZ439 Prototype 1)	csfbojbers(yzdvewrpru) = ysvwvtnftm msfofzpkel (koexyvrxfx, cffxrtgmui - ubvjncstqe) View more	-	23 Mar 2015
NCT02083406 (CTgov)	Phase 1	Malaria	22	OZ439+960mg PQP (Treatment B: OZ439 Prototype 2)	csfbojbers(yzdvewrpru) = qgbznkjgid msfofzpkel (koexyvrxfx, fmmsgeifoe - ktrhfsmino) View more	-	23 Mar 2015