DR AVIJIT MAZUMDER

@nietpharmacy.co.in

DIRECTOR
NOIDA INSTITUTE OF ENGINEERING AND TECHNOLOGY (PHARMACY INSTITUTE)

EDUCATION

COMPLETED BPHARM, MPHARM, MPHD from Jadavpur University Kolkata

RESEARCH INTERESTS

PHARMACY, PHARMACOLOGY AND MICROBIOLOGY

255

Scopus Publications

Scopus Publications


  • Fused and Substituted Piperazines as Anticancer Agents: A Review
    Saumya Singh, Rajnish Kumar, Shrishti Tripathi, Salahuddin, Avijit Mazumder, and Nardev Singh

    Wiley
    ABSTRACTCancer is an abnormal and uncontrolled proliferation of normal cells. The availability of safer anticancer drugs with exceptional selectivity for healthy cells and great efficacy against various cancer forms continues to be a significant obstacle. The piperazine moiety is used as the building block of several molecules and is reported to have the ability to inhibit the cell cycle (G1/S phase), inhibit angiogenesis, and interact with DNA. Piperazine also has a flexible binding feature that allows it to interact with a variety of biological targets, which makes it effective against cancers. As there is a continuous need to obtain an anticancer drug with improved efficacy and fewer side effects, the piperazine derivatives attract the attention of researchers. This review highlights the recently reported methods of synthesis of fused/substituted piperazines, structure–activity relationship, and interactions with targets/receptors as anticancer agents. Thus, the presented review will help medicinal chemists in designing anticancer molecules with piperazines.

  • Insight into the Synthesis Approaches of Oxadiazole and its Derivatives, Focuses on their Pharmacological Activities
    Sadhana Sharma, Chandana Majee, Rupa Mazumder, Avijit Mazumder, Pankaj Kumar Taygi, and Sachin Kumar Singh

    Manuscript Technomedia LLP


  • Acyl Urea Compounds Therapeutics and its Inhibition for Cancers in Women: A Review
    Preeti Kumari, Rakhi Mishra, Rupa Mazumder, and Avijit Mazumder

    Bentham Science Publishers Ltd.
    Acyl urea compounds have garnered significant attention in cancer therapeutics, particularly for their potential effectiveness against cancers that predominantly affect women, such as breast and ovarian cancers. The paper presents a report on the investigation of acyl urea compounds that are reported to involve a multi-faceted approach, including synthetic chemistry, biological assays, and computational modeling. A wealth of information on acyl urea and its purported effects on cancer affecting women has been gathered from different sources and condensed to provide readers with a broad understanding of the role of acyl urea in combating cancer. Acylureas demonstrate promising results by selectively inhibiting key molecular targets associated with cancer progressions, such as EGFR, ALK, HER2, and the Wnt/β-catenin signaling pathway. Specifically, targeting acyl ureas impedes tumor proliferation and metastasis while minimizing harm to healthy tissues, offering a targeted therapeutic approach with reduced side effects compared to conventional chemotherapy. Continued research and clinical trials are imperative to optimize the efficacy and safety profiles of acylurea-based therapies and broaden their applicability across various cancer types. Acyl urea compounds represent a promising class of therapeutics for the treatment of cancers in women, particularly due to their ability to selectively inhibit key molecular targets involved in tumor growth and progression. The combination of synthetic optimization, biological evaluation, and computational modeling has facilitated the identification of several lead compounds with significant anticancer potential. This abstract explores the therapeutic mechanisms and targeted pathways of acyl ureas in combating these malignancies, which will be useful for future studies.


  • Recent Advances in Synthetic Strategies of Piperazine & its Analogs Via Rearrangement Reactions: A Review
    Upasana Sharma, Rajnish Kumar, Avijit Mazumder, Salahuddin, Neelima Kukreti, Pankaj Kumar Tyagi, and Navneet Khurana

    Bentham Science Publishers Ltd.
    In the six-membered heterocyclic compound piperazine, two nitrogen atoms are positioned within the ring at 1 and 4 positions. Numerous studies have shown that piperazine has the potential to be a useful pharmacophore in many harmful pharmacological conditions such as microbiocidal, antiinflammatory, anticancer, antioxidant, etc. In this present review, we highlighted the synthetic protocols for piperazine and its analogs, as well as the synthetic protocol for piperazine <i>via</i> rearrangement reaction, which have been adopted in recent years. The study also involved a listing of several patents (granted), which comprised important work on piperazine and its derivatives. Among all the methods, the most commonly adopted synthetic methods included the synthesis of piperazine analogs by dizacope, hydrolytic, mumm, multi-component, ugi-smiles, [2+3]-stevens, aza-Wittig, Curtius, Schmidt rearrangement reactions, etc. These synthetic protocols have also been compared based on different reaction conditions, feasibility, and economy to help the researchers in designing their work.

  • Recently Adopted Synthetic Protocols for Piperazines: A Review
    Mohit Gangwar, Rajnish Kumar, Ranjeet Kumar Yadav, Avijit Mazumder, Salahuddin, Neelima Kukreti, Pankaj Kumar Tyagi, and Bhupinder Kapoor

    Bentham Science Publishers Ltd.
    Piperazines, a class of heterocyclic compounds, have garnered significant attention in the field of organic synthesis due to their diverse pharmacological activities and widespread applications in medicinal chemistry. This review provides a comprehensive overview of the recent advancements in the synthesis of piperazines, highlighting innovative methodologies, novel reagents, and green synthesis approaches adopted by researchers. The synthesis of piperazines has witnessed remarkable progress, with a focus on developing efficient and sustainable synthetic routes. Various strategies, such as transition-metal-catalyzed reactions, microwave-assisted synthesis, photo-redox reactions, and bio-inspired methods, have emerged as powerful tools for constructing piperazine scaffolds. The review also encompasses discussions on the stereochemistry and regioselectivity issues associated with piperazine synthesis, shedding light on the intricacies of achieving specific substitution patterns. The impact of newly synthesized piperazines in drug discovery and development is also explored, emphasizing the therapeutic potential of these compounds in various disease areas. In conclusion, this review provides a comprehensive and up-to-date account of the recent advancements in piperazine synthesis, offering insights into the current state of the field and guiding future research directions. The integration of innovative methodologies and the exploration of sustainable practices underscore the ongoing efforts to streamline the synthesis of piperazines, contributing to the expansion of their applications in medicinal chemistry and related disciplines.

  • Hydrazides: An Important Tool for the Synthesis of 1,3,4-oxadiazole
    Shrishti Tripathi, Rajnish Kumar, Avijit Mazumder, Salahuddin, Neelima Kukreti, Arvind Kumar, and Gurvinder Singh

    Bentham Science Publishers Ltd.
    Abstract: Hydrazides, derivatives of hydrazine, are widely used in pharmaceuticals, polymers, dyes, herbicides, and as chemical preservatives. A notable application is in synthesizing 1,3,4-oxadiazole, an important aromatic compound with a five-membered heterocyclic ring containing two nitrogen atoms and one oxygen atom. Among the four oxadiazole isomers, 1,3,4-oxadiazole is the most significant, used in drug discovery, pharmaceuticals, and dyes. It is synthesized from various substituted hydrazides or hydrazones using reagents like copper, cobalt, cerium, phosphorus oxychloride, mercury oxide, potassium iodide, triflic anhydride, and carbon disulfide. This study reviews the synthesis methods of 1,3,4-oxadiazole, highlighting the advantages and disadvantages of different catalysts and conditions, providing useful insights for researchers.

  • An Insight into the Synthetic Strategies and Pharmacological Effects of Cinnoline Derivatives
    Shagun Saxena, Rakhi Mishra, Avijit Mazumder, Rupa Mazumder, and Mohd Shuaib

    Manuscript Technomedia LLP
    The cinnoline ring is a new aromatic heterocyclic connected with two nitrogen atoms in a 6 membered ring and compounds containing this ring have been shown to have a wide variety of pharmacological effects. This review study extensively explains the synthetic strategy by which researchers have produced cinnoline derivatives reported to have numerous pharmacological effects, including antitubercular, antibacterial, anticancer, antimolluscidal, etc., The cinnoline moiety is a highly powerful lead that may give a range of pharmacological effects and this study provides brief information on the various synthesis techniques and pharmacological activity of reported cinnoline analogs that support this claim. This succinct review summarizes the several known cinnoline analogs, outlining their respective synthesis strategies and pharmacological activity and conclusively showing that the cinnoline moiety is a potent lead capable of producing a wide range of therapeutic actions. This article's literature review will serve as a springboard for further research into the synthesis of cinnoline derivatives, which in turn will aid in the creation of cinnoline-based compounds with improved pharmacokinetic and pharmacodynamic characteristics

  • Quest for discovering novel CDK12 inhibitor
    Abhijit Debnath, Rajesh Kumar Singh, Rupa Mazumder, Avijit Mazumder, Shikha Srivastava, Hema Chaudhary, Saloni Mangal, Jahanvi Sanchitra, Pankaj Kumar Tyagi, Sachin Kumar Singh,et al.

    Informa UK Limited
    CDK12 is essential for cellular processes like RNA processing, transcription, and cell cycle regulation, inhibiting cancer cell growth and facilitating macrophage invasion. CDK12 is a significant oncogenic factor in various cancers, including HER2-positive breast cancer, Anaplastic thyroid carcinoma, Hepatocellular carcinoma, prostate cancer, and Ewing sarcoma. It is also regarded as a potential biomarker, emphasizing its broader significance in oncology. Targeting CDK12 offers a promising strategy to develop therapy. Various monoclonal antibodies have drawn wide attention, but they are expensive compared to small-molecule inhibitors, limiting their accessibility and affordability for patients. Consequently, this research aims to identify effective CDK12 inhibitors using comprehensive high-throughput virtual screening. RASPD protocol has been employed to screen three different databases against the target followed by drug-likeness, molecular docking, ADME, toxicity, Consensus molecular docking, MD Simulation, and in-vitro studies MTT assay. The research conducted yielded one compound ZINC11784547 has demonstrated robust binding affinity, favorable ADME features, less toxicity, remarkable stability, and cytotoxic effect. The identified compound holds promise for promoting cancer cell death through CDK12 inhibition.

  • Immunological Implications in Diabetes: A Review on Various Diseases and Conditions 119
    Sanskriti Upadhyay, Avijit Mazumder, Bhavani Pentela, Priyanka Bansal, Neeraj Agarwal, and Dileep Singh Baghel

    Bentham Science Publishers Ltd.
    : Diabetes Mellitus (DM) is a long-term metabolic condition that has significant social, health, and economic consequences. There are various forms of diabetes mellitus, but the two most common varieties are type I and type II. Insulin-dependent diabetes (IDDM) is one of the most wellknown autoimmune illnesses that cause insulin insufficiency and hyperglycemia by either damaging or destroying Langerhans' beta cells. Available scientific data evidenced the greatest genetic contribution of Human Leukocyte Antigen class II in the IDDM. Hyperglycemia and individual components of the insulin resistance (metabolic) syndrome put people with type II diabetes at increased risk for microvascular consequences (retinopathy, nephropathy, and neuropathy) as well as macrovascular issues (cardiovascular comorbidities). A number of pathophysiological abnormalities, including obesity, poor diet, and physical inactivity, as well as genetic variables, are involved in the disturbed glucose homeostasis associated with type II diabetes. Diseases like lipid abnormalities contribute to the progression of diabetes, whereas obesity and its related medical disorders (such as hypertension, diabetes, insulin resistance, and sleep apnea syndrome) are eventually linked to an elevated cardiovascular risk. Diabetes raises the incidence, intensity, and duration of peri-densities in people with diabetes compared to healthy persons, making it a risk factor for periodontal disease. Diabetes conditions in patients concurrently also increase the progression or risk of other diseases, i.e., cardiovascular- related diseases (hypertension, oxidative stress, hyperlipidemia), nervous system-related diseases, and COVID-19, by increasing the overall infection rate. There is widespread evidence that correlates the direct connection between diabetes and other diseases, including immunity disorders, CVS disorders, etc. This review provides a correlation between diabetes and another disease with an overall impact on the progression of cardiovascular diseases, neurological diseases, COVID-19, and periodontal diseases. This current review focuses on the collation of some plants that show antidiabetic activity, including plant part, family, chemical constituent, mechanism of action, and chemical used for extraction. Studies on the role, causes, clinical management, prevention, and treatment of diabetes heavily rely on epidemiological evidence. This review also explains different factors responsible for diabetes, like genetic factors, environmental factors, and viral infections.

  • Pharmacological Evaluation of Bioisosterically Replaced and Triazole-Tethered Derivatives for Anticancer Therapy
    Dipesh Kumar, Salahuddin, Avijit Mazumder, Rajnish Kumar, Mohamed Jawed Ahsan, Mohammad Shahar Yar, Abbussalam, Pankaj Kumar Tyagi, and M.V.N.L. Chaitanya

    Bentham Science Publishers Ltd.
    Cancer has been the cause of the highest number of deaths in the human population despite the development and advancement in treatment therapies. The toxicity, drug resistance, and side effects of the current medicaments and therapies have left the void for more research and development. One of the possibilities to fill this void is by incorporating Triazole moieties within existing anticancer pharmacophores to develop new hybrid drugs with less toxicity and more potency. The placement of nitrogen in the triazole ring has endowed its characterization of being integrated with anticancer pharmacophores via bioisosteric replacement, click chemistry and organocatalyzed approaches. This review paper emphasizes the discussions from articles published from the early 2000s to the current 2020s about the triazole-based derivatives used in anticancer therapy, elaborating more on their chemical structures, target receptors or enzymes, mechanism of action, structure-activity relationships, different triazole-derived hybrid drugs under clinical and nonclinical trials, and recent advancements toward developing more potent and less toxic anticancer agents.

  • The role of neurotransmitter receptors in antipsychotic medication efficacy for Alzheimer’s-related psychosis
    Bhawana Sharma, Saumya Das, Avijit Mazumder, Deepraj Singh Rautela, Pankaj Kumar Tyagi, and Navneet Khurana

    Springer Science and Business Media LLC
    Abstract Background Alzheimer's disease (AD) is marked by cognitive decline along with the presence of mental symptoms, most notably psychosis. Although antipsychotic drugs are commonly recommended to treat these symptoms, there is ongoing discussion on the safety and effectiveness of these drugs in AD patients. The therapeutic management of Alzheimer’s disease-related psychosis (ARP) is hampered by its limited therapy options, determining the precise brain regions in Alzheimer’s patients with understanding of the neurological substrates implicated in ARP. While new therapies including brexpiprazole and atypical antipsychotics present promising therapeutic choices, practical implementation and potential upcoming therapies approaches is discussed along with mechanism-based understanding of different neurotransmitters with pharmaceutical therapies. Our objective is to contribute to more efficient and individualized treatment approaches by offering a thorough resource for medical professionals and researchers working in the field of managing and researching psychosis associated with AD. Results The examination containing new data supporting newer therapeutic approaches that target receptors and providing better safety and effectiveness characteristics. This study point out gaps in our existing understanding and make recommendations for future research, emphasizing the necessity of clinical trials created especially for psychotic Alzheimer’s patients. Secondly, the neurochemical and neuropathological bases of ARP, with a focus on changes in the dopamine, serotonin, and glutamate systems of neurotransmitters are also described in detail. Different pharmacodynamics antipsychotic medications are covered in later sections of this paper, with an emphasis on how these medications' interactions with certain neurotransmitter receptors may affect their therapeutic efficacy and side-effects profile. Conclusion The review article summarizes the most recent findings regarding the contribution of neurotransmitter receptors to the effectiveness of antipsychotic drugs in the management of ADP. We provide a thorough overview of second-generation (atypical) antipsychotics, emphasizing how their unique affinity for neurotransmitter receptors influences their clinical application in psychosis associated with AD. The difficulties of treating Alzheimer’s with antipsychotics are also covered in this study, including the potential for cognitive impairment to worsen, the emergence of extrapyramidal symptoms, and other unfavorable effects. New approaches to studying and treating ARP including neuroinflammation-targeting medicines, transcranial magnetic stimulation (TMS), cerebrospinal fluid (CSF) biomarkers, and muscarinic acetylcholine receptor (mAChR) agonists like xanomeline. Reducing psychosis through treatment options could be improved by knowledge of N-methyl-D-aspartate glutamate receptors (NMDAR) hypofunction processes in gamma-aminobutyric acid (GABAergic) neurons.

  • Synthesis, In Vivo, ADME Determination, and Molecular Docking Studies of 1,3,4-Oxadiazoles Containing Pyridine and Piperazine Moieties as New Diuretic Agents
    Md Faizan, Rajnish Kumar, Avijit Mazumder, Salahuddin, Pankaj Kumar Tyagi, Farid S. Ataya, Virat Khanna, Rajeev Sobti, A. Sai Pavani, Ganesh Bushi,et al.

    Wiley
    AbstractA series of 1‐(piperazin‐1‐yl)‐2‐((5‐(pyridin‐4‐yl)‐1,3,4‐oxadiazol‐2‐yl)thio)ethan‐1‐one derivatives (9a–l) were prepared using a multistep reaction between 2‐chloro‐1‐(piperazin‐1yl)ethan‐1‐one derivatives (4a–l) and 5‐(pyridine‐4‐yl)‐1,3,4‐oxadiazole‐2‐thiol (8) and studied their diuretic potential by following established in vivo and in silico protocols. The data obtained from the experimental rat animal model in vivo diuretic studies indicated that synthesized derivatives 9d, 9e, 9g, 9i, and 9j possess excellent diuretic potential. The results obtained from in vivo study were also reinforced by the data of in silico studies performed using AutoDock (1.5.7) software. The molecular docking involved interactions of synthesized molecules with two target proteins, that is, human carbonic anhydrase II protein (hCA‐II, PDB ID: 3HS4) and human NKCCl K289NA492E protein (NKCCl, PDB ID: 7S1Y). The ADME properties of the synthesized molecules have also been determined using pkCSM software that established that the synthesized molecules are good candidates for oral absorption. All the data of in vivo and in silico studies synergized the results that state that the diuretic activity of all synthesized compounds is greater than that of the standard drug (furosemide), whereas compounds 9d, 9e, 9g, 9i, and 9j show excellent activity with values of 1.32, 1.33, 1.35, 1.39, and 1.35, respectively.




  • Synthesis, In vivo, and In silico Evaluation of New Pyrazoline-Benzothiazole Conjugates as Antiepileptic Agents
    Himanshu Singh, Rajnish Kumar, Avijit Mazumder, Salahuddin, Ranjeet Kumar Yadav, Neelima Kukreti, Mohd. Mustaqeem Abdullah, Pankaj Kumar Tyagi, and MVNL Chaitanya

    Wiley
    AbstractNew 2‐(4‐benzothiazol‐2‐yl‐phenoxy)‐1‐(3,5‐diphenyl‐4,5‐dihydro‐pyrazol‐1‐yl)‐ethanones (9a–o) have been designed and synthesized. All the synthesized compounds were characterized by thin layer chromatography and spectral analysis. The antiepileptic potential of the synthesized compounds has been tested by following standard animal screening models, including maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) models. The neurotoxic and antidepression effects of the synthesized compounds were checked by utilizing rotarod apparatus, and motor impairment test (by actophotometer) respectively. The study concluded that compounds 9c, 9d, 9f, 9i, 9n, and 9o possessed good antiepileptic potential compared to standard drugs like carbamazepine and phenytoin. The results of the rotarod performance test also established them without any neurotoxicity. The motor impairment test revealed that the synthesized compounds are also good antidepressants. In‐silico studies have been performed for calculation of pharmacophore pattern, prediction of pharmacokinetic properties which determine the eligibility of synthesized compounds as orally administered molecules and interactions with the target proteins. The result of in‐silico studies reinforced results obtained by in vivo study of the synthesized compounds and their possible mechanism of antiepileptic action i. e. via inhibiting voltage‐gated sodium channels (VGSCs) and gamma‐aminobutyric acid‐A receptor.



  • The medicinal chemistry of piperazines: A review
    Md Faizan, Rajnish Kumar, Avijit Mazumder, Salahuddin, Neelima Kukreti, Arvind Kumar, and M. V. N. L. Chaitanya

    Wiley
    AbstractThe versatile basic structure of piperazine allows for the development and production of newer bioactive molecules that can be used to treat a wide range of diseases. Piperazine derivatives are unique and can easily be modified for the desired pharmacological activity. The two opposing nitrogen atoms in a six‐membered piperazine ring offer a large polar surface area, relative structural rigidity, and more acceptors and donors of hydrogen bonds. These properties frequently result in greater water solubility, oral bioavailability, and ADME characteristics, as well as improved target affinity and specificity. Various synthetic protocols have been reported for piperazine and its derivatives. In this review, we focused on recently published synthetic protocols for the synthesis of the piperazine and its derivatives. The structure–activity relationship concerning different biological activities of various piperazine‐containing drugs has also been highlighted to provide a good understanding to researchers for future research on piperazines.

  • Substrate-based synthetic strategies and biological activities of 1,3,4-oxadiazole: A review
    Upasana Sharma, Rajnish Kumar, Avijit Mazumder, Salahuddin, Neelima Kukreti, Rashmi Mishra, and M. V. N. L. Chaitanya

    Wiley
    AbstractThe five‐membered 1,3,4‐oxadiazole heterocyclic ring has received considerable attention because of its unique bio‐isosteric properties and an unusually wide spectrum of biological activities. After a century since 1,3,4‐oxadiazole was discovered, its uncommon potential attracted medicinal chemist's attention, leading to the discovery of a few presently accessible drugs containing 1,3,4‐oxadiazole units, and a large number of patents have been granted on research related to 1,3,4‐oxadiazole. It is worth noting that interest in 1,3,4‐oxadiazoles' biological applications has doubled in the last few years. Herein, this review presents a comprehensive overview of the recent achievements in the synthesis of 1,3,4‐oxadiazole‐based compounds and highlights the major advances in their biological applications in the last 10 years, as well as brief remarks on prospects for further development. We hope that researchers across the scientific streams will benefit from the presented review articles for designing their work related to 1,3,4‐oxadiazoles.

  • A critical overview of challenging roles of medicinal plants in improvement of wound healing technology
    Deepika Pathak and Avijit Mazumder

    Springer Science and Business Media LLC

  • Exploring the Potential of Traditional Herbal Plants in the Management of Diabetes Mellitus: A Comprehensive Investigation
    Sanskriti, Avijit Mazumder, Priyanka Bansal, Bhavani Pentela, Pankaj Kumar Tyagi, and Navneet Khurana

    Informatics Publishing Limited
    Diabetes Mellitus (DM) is one of the most prevalent chronic conditions bearing considerable social, health, and economic ramifications. Uncontrolled DM manifests secondary complications such as foot ulceration, retinopathy, neuropathy, nephropathy, and cardiomyopathy. The heterogeneity inherent in DM necessitates a comprehensive therapeutic strategy that is equally safe and effective against multifaceted diseases like DM. Conventionally, DM management relies on lifestyle modifications and dietary adjustments, complemented by pharmacological interventions. However, the limitations associated with oral hypoglycaemic agents prompt an exploration of alternative modalities. These days, substantial resources within healthcare are dedicated to investigating traditional systems of medicine, notably Ayurveda and traditional Chinese medicine, seeking novel interventions for DM management. This systematic review aims to evaluate the available literature of 2017-2023, focusing on identifying herbs with potential efficacy in DM management with their potent mechanism of action. By synthesizing current scientific knowledge, the review elucidates the intricate molecular-level mechanisms of action of medicinal plants in DM. This contribution enriches the scientific discourse by providing a comprehensive resource for the nuanced exploration of innovative approaches to address the complex facets of DM. As healthcare endeavours to diversify its strategies, the insights from this review may pave the way for developing novel and effective interventions for managing DM using medicinal plants.

Industry, Institute, or Organisation Collaboration

NOIDA INSTITUTE OF ENGINEERING AND TECHNOLOGY (PHARMACY INSTITUTE)