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  1. Article ; Online: Withdrawal Notice: S.A.R.S Covid-19 A Medicinal Chemistry Approach

    Bhardwaj, Gautam / Tonk, Rajiv Kumar / Garg, Harish / Bhalla, Vijay

    Mini reviews in medicinal chemistry

    2021  

    Language English
    Publishing date 2021-01-26
    Publishing country Netherlands
    Document type Journal Article
    ZDB-ID 2104081-3
    ISSN 1875-5607 ; 1389-5575
    ISSN (online) 1875-5607
    ISSN 1389-5575
    DOI 10.2174/1389557521666210126125633
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    In stock of ZB MED Cologne/Königswinter

    Zs.A 5891: Show issues Location:
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  2. Article ; Online: The hidden threat: Environmental toxins and their effects on gut microbiota.

    Bhardwaj, Gautam / Riadi, Yassine / Afzal, Muhammad / Bansal, Pooja / Kaur, Harpreet / Deorari, Mahamedha / Tonk, Rajiv Kumar / Almalki, Waleed Hassan / Kazmi, Imran / Alzarea, Sami I / Kukreti, Neelima / Thangavelu, Lakshmi / Saleem, Shakir

    Pathology, research and practice

    2024  Volume 255, Page(s) 155173

    Abstract: The human gut microbiota (GM), which consists of a complex and diverse ecosystem of bacteria, plays a vital role in overall wellness. However, the delicate balance of this intricate system is being compromised by the widespread presence of environmental ... ...

    Abstract The human gut microbiota (GM), which consists of a complex and diverse ecosystem of bacteria, plays a vital role in overall wellness. However, the delicate balance of this intricate system is being compromised by the widespread presence of environmental toxins. The intricate connection between contaminants in the environment and human well-being has garnered significant attention in recent times. Although many environmental pollutants and their toxicity have been identified and studied in laboratory settings and animal models, there is insufficient data concerning their relevance to human physiology. Consequently, research on the toxicity of environmental toxins in GM has gained prominence in recent years. Various factors, such as air pollution, chemicals, heavy metals, and pesticides, have a detrimental impact on the composition and functioning of the GM. This comprehensive review aims to comprehend the toxic effects of numerous environmental pollutants, including antibiotics, endocrine-disrupting chemicals, heavy metals, and pesticides, on GM by examining recent research findings. The current analysis concludes that different types of environmental toxins can lead to GM dysbiosis and have various potential adverse effects on the well-being of animals. We investigate the alterations to the GM composition induced by contaminants and their impact on overall well-being, providing a fresh perspective on research related to pollutant exposure.
    MeSH term(s) Animals ; Humans ; Gastrointestinal Microbiome/physiology ; Ecosystem ; Environmental Pollutants/toxicity ; Metals, Heavy/toxicity ; Pesticides/toxicity
    Chemical Substances Environmental Pollutants ; Metals, Heavy ; Pesticides
    Language English
    Publishing date 2024-01-28
    Publishing country Germany
    Document type Journal Article ; Review
    ZDB-ID 391889-0
    ISSN 1618-0631 ; 0344-0338
    ISSN (online) 1618-0631
    ISSN 0344-0338
    DOI 10.1016/j.prp.2024.155173
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  3. Article ; Online: Quinoline-derivatives as privileged scaffolds for medicinal and pharmaceutical chemists: A comprehensive review.

    Yadav, Vivek / Reang, Jurnal / Sharma, Vinita / Majeed, Jaseela / Sharma, Prabodh Chander / Sharma, Kalicharan / Giri, Namita / Kumar, Arun / Tonk, Rajiv Kumar

    Chemical biology & drug design

    2022  Volume 100, Issue 3, Page(s) 389–418

    Abstract: The quinoline scaffolds are privileged for their numerous biological activities in the pharmaceutical field. This moiety constitutes a well-known space in several marketed preparations. The quinoline scaffolds gained attention in modern days being an ... ...

    Abstract The quinoline scaffolds are privileged for their numerous biological activities in the pharmaceutical field. This moiety constitutes a well-known space in several marketed preparations. The quinoline scaffolds gained attention in modern days being an important chemical moiety in the identification, designing, and synthesis of novel potent derivatives. The current review is developed to shine the light on critical and significant insights on the quinoline derivatives possessing diverse biological activities such as analgesic, anti-inflammatory, antialzheimer, anti-convulsant, anti-oxidant, antimicrobial, anti-cancer activities and so on. A detailed summary of quinoline ring from its origin to the recent advancements regarding its synthesis, green chemistry approaches, patented methods, and its marketed drugs is presented in the review. We attempted to review the literature compiling the critical information that has potential to encourage fellow researchers and scientists for the design and development of quinoline scaffold based active molecules that have improved therapeutic performance along with profound pharmacological properties.
    MeSH term(s) Analgesics/chemistry ; Anti-Infective Agents/chemistry ; Pharmaceutical Preparations/chemistry ; Quinolines/chemistry ; Antineoplastic Agents/chemistry
    Chemical Substances Analgesics ; Anti-Infective Agents ; Pharmaceutical Preparations ; Quinolines ; Antineoplastic Agents
    Language English
    Publishing date 2022-06-16
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't ; Review
    ZDB-ID 2216600-2
    ISSN 1747-0285 ; 1747-0277
    ISSN (online) 1747-0285
    ISSN 1747-0277
    DOI 10.1111/cbdd.14099
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  4. Article: Design and evaluation of sustained release mucoadhesive film of sumatriptan succinate containing grafted co-polymer as the platform.

    Verma, Surajpal / Tonk, Rajiv Kumar / Albratty, Mohammed / Alhazmi, Hassan Ahmad / Najmi, Asim / Kumar, Ravi / Kumar, Mohit / Taleuzzaman, Mohamad / Swami, Gourav / Alam, Md Shamsher

    Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society

    2022  Volume 30, Issue 11, Page(s) 1527–1537

    Abstract: Purpose: The primary goal of this research is to improve the bioavailability and efficacy of Sumatriptan succinate by incorporating it in the mucoadhesive film for the treatment of migraine. Mucoadhesive film offers an excellent substitute to deliver ... ...

    Abstract Purpose: The primary goal of this research is to improve the bioavailability and efficacy of Sumatriptan succinate by incorporating it in the mucoadhesive film for the treatment of migraine. Mucoadhesive film offers an excellent substitute to deliver the drug in the systemic circulation and eliminate the chance of first-pass metabolism.
    Method: Using central composite design (CCD), various formulations were created by incorporating polymer, plasticizer, and water, and an optimized preparation was created using statistical screening. The optimization has been performed by applying a 3
    Results: The actual experimental values obtained were compared with those predicted by the mathematical models. Formulation
    Conclusion: Formulation holding drug-loaded grafted film showed decent sustained and controlled drug release characteristics compared to a pure drug suspension. S9 formulation showed better results than other formulations in drug content, swelling index, folding endurance, and mucoadhesive strength, which is further used to treat migraine.
    Language English
    Publishing date 2022-07-29
    Publishing country Saudi Arabia
    Document type Journal Article
    ZDB-ID 1378024-4
    ISSN 1319-0164
    ISSN 1319-0164
    DOI 10.1016/j.jsps.2022.07.014
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    In stock of ZB MED Cologne/Königswinter

    Zs.A 4758: Show issues Location:
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  5. Article ; Online: Management of Glioblastoma Multiforme by Phytochemicals: Applications of Nanoparticle-Based Targeted Drug Delivery System.

    Mumtaz, Sayed M / Bhardwaj, Gautam / Goswami, Shikha / Tonk, Rajiv Kumar / Goyal, Ramesh K / Abu-Izneid, Tareq / Pottoo, Faheem Hyder

    Current drug targets

    2020  Volume 22, Issue 4, Page(s) 429–442

    Abstract: The Glioblastoma Multiforme (GBM; grade IV astrocytoma) exhorts tumors of star-shaped glial cells in the brain. It is a fast-growing tumor that spreads to nearby brain regions specifically to cerebral hemispheres in frontal and temporal lobes. The ... ...

    Abstract The Glioblastoma Multiforme (GBM; grade IV astrocytoma) exhorts tumors of star-shaped glial cells in the brain. It is a fast-growing tumor that spreads to nearby brain regions specifically to cerebral hemispheres in frontal and temporal lobes. The etiology of GBM is unknown, but major risk factors are genetic disorders like neurofibromatosis and schwannomatosis, which develop the tumor in the nervous system. The management of GBM with chemo-radiotherapy leads to resistance, and current drug regimen like Temozolomide (TMZ) is less efficacious. The reasons behind the failure of drugs are due to DNA alkylation in the cell cycle by enzyme DNA guanidase and mitochondrial dysfunction. Naturally occurring bioactive compounds from plants referred as phytochemicals, serve as vital sources for anti-cancer drugs. Some prototypical examples include taxol analogs, vinca alkaloids (vincristine, vinblastine), podophyllotoxin analogs, camptothecin, curcumin, aloe-emodin, quercetin, berberine etc. These phytochemicals often regulate diverse molecular pathways, which are implicated in the growth and progression of cancers. However, the challenges posed by the presence of BBB/BBTB to restrict the passage of these phytochemicals, culminates in their low bioavailability and relative toxicity. In this review, we integrated nanotech as a novel drug delivery system to deliver phytochemicals from traditional medicine to the specific site within the brain for the management of GBM.
    MeSH term(s) Brain Neoplasms/drug therapy ; Drug Delivery Systems ; Glioblastoma/drug therapy ; Humans ; Nanoparticles ; Phytochemicals/therapeutic use
    Chemical Substances Phytochemicals
    Language English
    Publishing date 2020-07-21
    Publishing country United Arab Emirates
    Document type Journal Article ; Research Support, Non-U.S. Gov't ; Review
    ZDB-ID 2064859-5
    ISSN 1873-5592 ; 1389-4501
    ISSN (online) 1873-5592
    ISSN 1389-4501
    DOI 10.2174/1389450121666200727115454
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    Zs.A 5578: Show issues Location:
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  6. Article: Microwave assisted green synthesis of thiazolidin-4-one derivatives: A perspective on potent antiviral and antimicrobial activities

    Saini, Neha / Sharma, Archana / Thakur, Vijay Kumar / Makatsoris, Charalampos / Dandia, Anshu / Bhagat, Madhulika / Tonk, Rajiv Kumar / Sharma, Prabodh Chander

    Current research in green and sustainable chemistry. 2020 June, v. 3

    2020  

    Abstract: Thiazolidin-4-one has been known as a powerful moiety present in various approved medications. Thiazolidin-4-ones are amongst the most effective and actively explored fields of current antimicrobial and antiviral chemotherapy that portray broad spectrum ... ...

    Abstract Thiazolidin-4-one has been known as a powerful moiety present in various approved medications. Thiazolidin-4-ones are amongst the most effective and actively explored fields of current antimicrobial and antiviral chemotherapy that portray broad spectrum and potent activity. The wide range of medicinal properties of thiazolidin-4-one related drugs encourages the medicinal chemists to synthesize a significant variety of new medicinal substances. Microwave induced organic reactions earned substantial coverages in recent years due to many advantages such as ease of work, cost-effectiveness, short reaction time and excellent yield. Microwave radiations provide a substitute for traditional heating by incorporating energy to the reactions. The usage of microwave irradiation has contributed to the emergence of innovative ideas in chemistry, as energy absorption and propagation in microwave irradiation is entirely dissimilar to the traditional heating method. In synthetic chemistry, microwave heating is a rapidly growing area of research. This review cover organic synthesis of thiazolidin-4-one analogues via the use of microwave irradiation as an effective technique and the antiviral and antimicrobial action of thiazolidin-4-one based compounds.
    Keywords absorption ; antimicrobial properties ; cost effectiveness ; drug therapy ; energy ; green chemistry ; heat ; microwave radiation ; microwave treatment ; moieties ; research
    Language English
    Dates of publication 2020-06
    Publishing place Elsevier B.V.
    Document type Article
    ISSN 2666-0865
    DOI 10.1016/j.crgsc.2020.100021
    Database NAL-Catalogue (AGRICOLA)

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  7. Article ; Online: Microwave Assisted Green synthesis of Thiazolidin-4-One derivatives: A Perspective on Potent Antiviral and Antimicrobial Activities

    Saini, Neha / Sharma, Archana / Thakur, Vijay Kumar / Makatsoris, Harris / Dandia, Anshu / Bhagat, Madhulika / Tonk, Rajiv Kumar / Chander Sharma, Prabodh

    Abstract: Thiazolidin-4-one has been known as a powerful moiety present in various approved medications. Thiazolidin-4-ones are amongst the most effective and actively explored fields of current antimicrobial and antiviral chemotherapy that portray broad spectrum ... ...

    Abstract Thiazolidin-4-one has been known as a powerful moiety present in various approved medications. Thiazolidin-4-ones are amongst the most effective and actively explored fields of current antimicrobial and antiviral chemotherapy that portray broad spectrum and potent activity. The wide range of medicinal properties of thiazolidin-4-one related drugs encourages the medicinal chemists to synthesize a significant variety of new medicinal substances. Microwave induced organic reactions earned substantial coverages in recent years due to many advantages such as ease of work, cost-effectiveness, short reaction time and excellent yield. Microwave radiations provide asubstitutefortraditional heating by incorporating energy to the reactions. The usage of microwave irradiation has contributedto the emergence of innovative ideas in chemistry, as energy absorption and propagation in microwave irradiation is entirely dissimilar tothe traditional heating method. In synthetic chemistry, microwave heating is a rapidly growing area of research. This reviewcoverorganic synthesis of thiazolidin-4-one analogues via the use of microwave irradiation as an effective technique and the antiviral and antimicrobial action of thiazolidin-4-one based compounds.
    Keywords covid19
    Publisher Elsevier; PMC
    Document type Article ; Online
    DOI 10.1016/j.crgsc.2020.100021
    Database COVID19

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  8. Article ; Online: Synthesis and pharmacological evaluation of pyrazolo[4,3-c]cinnoline derivatives as potential anti-inflammatory and antibacterial agents.

    Tonk, Rajiv Kumar / Bawa, Sandhya / Chawla, Gita / Deora, Girdhar Singh / Kumar, Suresh / Rathore, Vandana / Mulakayala, Naveen / Rajaram, Azad / Kalle, Arunasree M / Afzal, Obaid

    European journal of medicinal chemistry

    2012  Volume 57, Page(s) 176–184

    Abstract: A series of pyrazolo[4,3-c]cinnoline derivatives was synthesized, characterized and evaluated for anti-inflammatory and antibacterial activity. Test compounds that exhibited good anti-inflammatory activity were further screened for their ulcerogenic and ... ...

    Abstract A series of pyrazolo[4,3-c]cinnoline derivatives was synthesized, characterized and evaluated for anti-inflammatory and antibacterial activity. Test compounds that exhibited good anti-inflammatory activity were further screened for their ulcerogenic and lipid peroxidation activity. Compounds 4d and 4l showed promising anti-inflammatory activity with reduced ulcerogenic and lipid peroxidation activity when compared to naproxen. Docking results of these two compounds with COX-2 (PDB ID: 1CX2) also exhibited a strong binding profile. Among the test derivatives, compound 4i displayed significant antibacterial property against gram-negative (Escherichia coli and Pseudomonas aeruginosa) and gram-positive (Staphylococcus aureus) bacteria. However, compound 4b emerged as the best dual anti-inflammatory-antibacterial agent in the present study.
    MeSH term(s) Administration, Oral ; Animals ; Anti-Bacterial Agents/chemical synthesis ; Anti-Bacterial Agents/pharmacology ; Anti-Inflammatory Agents/chemical synthesis ; Anti-Inflammatory Agents/pharmacology ; Carrageenan ; Cyclooxygenase 2/metabolism ; Edema/chemically induced ; Edema/drug therapy ; Edema/metabolism ; Escherichia coli/drug effects ; Escherichia coli/growth & development ; Heterocyclic Compounds, 2-Ring/chemical synthesis ; Heterocyclic Compounds, 2-Ring/pharmacology ; Inflammation/chemically induced ; Inflammation/drug therapy ; Inflammation/metabolism ; Lipid Peroxidation/drug effects ; Microbial Sensitivity Tests ; Molecular Docking Simulation ; Naproxen/pharmacology ; Pseudomonas aeruginosa/drug effects ; Pseudomonas aeruginosa/growth & development ; Pyrazoles/chemical synthesis ; Pyrazoles/pharmacology ; Rats ; Rats, Wistar ; Staphylococcus aureus/drug effects ; Staphylococcus aureus/growth & development ; Structure-Activity Relationship ; Ulcer/chemically induced ; Ulcer/pathology
    Chemical Substances Anti-Bacterial Agents ; Anti-Inflammatory Agents ; Heterocyclic Compounds, 2-Ring ; Pyrazoles ; Naproxen (57Y76R9ATQ) ; Carrageenan (9000-07-1) ; Cyclooxygenase 2 (EC 1.14.99.1) ; PTGS2 protein, human (EC 1.14.99.1) ; cinnoline (N5KD6I506O)
    Language English
    Publishing date 2012-11
    Publishing country France
    Document type Journal Article
    ZDB-ID 188597-2
    ISSN 1768-3254 ; 0009-4374 ; 0223-5234
    ISSN (online) 1768-3254
    ISSN 0009-4374 ; 0223-5234
    DOI 10.1016/j.ejmech.2012.08.045
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