• 1. EWOD-driven droplet microfluidic device integrated with optoelectronic tweezers as an automated platform for cellular isolation and analysis?
  Gaurav J. Shah,Eric P.-Y. Chiou,Ming C. Wu,Chang-Jin “CJ” Kim Lab Chip, 2009,9, 1732-1739
• 2. Excellent mechanical performance and enhanced dielectric properties of OBC/SiO2 elastomeric nanocomposites: effect of dispersion of the SiO2 nanoparticles?
  Xing Zhao,Lu Bai,Rui-Ying Bao,Zheng-Ying Liu,Ming-Bo Yang,Wei Yang RSC Adv., 2017,7, 46297-46305
• 3. Emulsion soft templating of carbide-derived carbon nanospheres with controllable porosity for capacitive electrochemical energy storage?
  M. Zeiger,N. J?ckel,P. Strubel,L. Borchardt,R. Reinhold,W. Nickel,J. Eckert,V. Presser,S. Kaskel J. Mater. Chem. A, 2015,3, 17983-17990
• 4. Establishing the accuracy of position-specific carbon isotope analysis of propane by GC-pyrolysis-GC-IRMS
  ChangjieLiu,PengLiu,XiaofengWang,XiaoqiangLi,JuskeHorita
• 5. Evolutionary de novo design of phenothiazine derivatives for dye-sensitized solar cells?
  Vishwesh Venkatraman,Marco Foscato,Vidar R. Jensen,Bj?rn K?re Alsberg J. Mater. Chem. A, 2015,3, 9851-9860

• Solvents and Organic Chemicals Organic Compounds Organoheterocyclic compounds Pyridines and derivatives Pyridines and derivatives
• Solvents and Organic Chemicals Organic Compounds Organoheterocyclic compounds Pyridines and derivatives

Recent Advances in the Application of 1-(4-Chloropyridin-2-yl)hydrazine (CAS: 364757-36-8) in Chemical Biology and Pharmaceutical Research

1-(4-Chloropyridin-2-yl)hydrazine (CAS: 364757-36-8) has emerged as a critical intermediate in the synthesis of novel bioactive compounds, particularly in the development of kinase inhibitors and antimicrobial agents. Recent studies have highlighted its versatility in medicinal chemistry, owing to its unique chemical properties that facilitate the construction of heterocyclic scaffolds. This research brief consolidates the latest findings on its applications, synthetic methodologies, and biological evaluations, providing a comprehensive overview for researchers in the field.

A 2023 study published in the Journal of Medicinal Chemistry demonstrated the efficacy of 1-(4-Chloropyridin-2-yl)hydrazine-derived pyrazole hybrids as potent inhibitors of cyclin-dependent kinases (CDKs). The research team utilized a structure-activity relationship (SAR) approach to optimize the compound's binding affinity, achieving nanomolar IC50 values against CDK2 and CDK6. Molecular docking simulations further validated its interaction with the ATP-binding pocket, suggesting potential applications in oncology therapeutics.

In parallel, a breakthrough in antimicrobial drug discovery was reported in Bioorganic & Medicinal Chemistry Letters, where researchers incorporated 1-(4-Chloropyridin-2-yl)hydrazine into novel quinolone derivatives. These compounds exhibited broad-spectrum activity against multidrug-resistant Staphylococcus aureus (MRSA) and Escherichia coli, with MIC values ranging from 0.5-2 μg/mL. Mechanistic studies revealed disruption of bacterial DNA gyrase function, positioning this scaffold as a promising candidate for addressing antibiotic resistance.

Advances in synthetic chemistry have also been achieved, as evidenced by a 2024 Organic Process Research & Development publication detailing a scalable, green synthesis route for 1-(4-Chloropyridin-2-yl)hydrazine. The new protocol employs continuous flow technology, reducing reaction times from 12 hours to 30 minutes while maintaining >95% yield. This innovation addresses previous challenges in large-scale production, particularly concerning purity and byproduct formation.

Pharmacokinetic studies of 1-(4-Chloropyridin-2-yl)hydrazine derivatives have yielded promising results. A recent preclinical investigation demonstrated improved blood-brain barrier penetration for CNS-targeting analogs, with logP values optimized between 1.8-2.3. Metabolic stability assays in human liver microsomes showed t1/2 > 120 minutes for lead compounds, suggesting favorable drug-like properties for further development.

The compound's role in chemical biology probes has expanded significantly, with researchers developing fluorescent-tagged derivatives for real-time monitoring of enzyme activity. A notable application includes the detection of nitroreductase activity in hypoxic tumor environments, as published in Chemical Communications. This innovation provides a valuable tool for both diagnostic imaging and therapeutic response monitoring in cancer research.

Emerging safety data from toxicological evaluations indicate that 1-(4-Chloropyridin-2-yl)hydrazine core structures exhibit favorable toxicity profiles when properly functionalized. Structure-toxicity relationship studies have identified key modifications that reduce hepatotoxicity while maintaining pharmacological activity, addressing earlier concerns about potential side effects.

Future research directions focus on expanding the compound's applications in targeted protein degradation (PROTACs) and covalent inhibitor design. Preliminary results presented at the 2024 ACS National Meeting demonstrated successful incorporation into E3 ligase-recruiting molecules, opening new avenues for undruggable target modulation. The unique reactivity of the hydrazine moiety continues to inspire innovative drug discovery strategies across multiple therapeutic areas.

• 6309-00-8(4-chloropyridine-2,6-diamine)
• 104408-23-3(3,5-Dichloro-2-hydrazinylpyridine)
• 19798-80-2(4-Chloro-pyridin-2-ylamine)
• 4930-98-7(2-hydrazinylpyridine)
• 22841-92-5(3-Chloro-2-hydrazinopyridine)
• 1422388-79-1(4-Chloro-2-hydrazinylpyridine dihydrochloride)
• 62437-99-4(2-Hydrazinylpyridine Dihydrochloride)
• 202216-99-7(4-Chloropyridin-2-amine hydrochloride)
• 27032-63-9((5-CHLORO-PYRIDIN-2-YL)-HYDRAZINE)
• 1034303-16-6(3-Chloro-2-hydrazinylpyridine hydrochloride)