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  1. Article ; Online: Synthesis of novel furan-based chalcone derivatives as anti-tuberculosis agents:

    Dhivya, Loganathan Sumathi / Kumaradoss, Kathiravan Muthu

    Future medicinal chemistry

    2023  Volume 15, Issue 18, Page(s) 1687–1701

    Abstract: Background: ...

    Abstract Background:
    MeSH term(s) Humans ; Antitubercular Agents/chemistry ; Chalcones/pharmacology ; Mycobacterium tuberculosis ; HeLa Cells ; Chalcone/pharmacology ; Microbial Sensitivity Tests ; Structure-Activity Relationship ; Molecular Docking Simulation
    Chemical Substances Antitubercular Agents ; Chalcones ; Chalcone (5S5A2Q39HX)
    Language English
    Publishing date 2023-09-21
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ISSN 1756-8927
    ISSN (online) 1756-8927
    DOI 10.4155/fmc-2023-0110
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Strategies in the Design and Development of Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs).

    Vanangamudi, Murugesan / Palaniappan, Senthilkumar / Kathiravan, Muthu Kumaradoss / Namasivayam, Vigneshwaran

    Viruses

    2023  Volume 15, Issue 10

    Abstract: AIDS (acquired immunodeficiency syndrome) is a potentially life-threatening infectious disease caused by human immunodeficiency virus (HIV). To date, thousands of people have lost their lives annually due to HIV infection, and it continues to be a big ... ...

    Abstract AIDS (acquired immunodeficiency syndrome) is a potentially life-threatening infectious disease caused by human immunodeficiency virus (HIV). To date, thousands of people have lost their lives annually due to HIV infection, and it continues to be a big public health issue globally. Since the discovery of the first drug, Zidovudine (AZT), a nucleoside reverse transcriptase inhibitor (NRTI), to date, 30 drugs have been approved by the FDA, primarily targeting reverse transcriptase, integrase, and/or protease enzymes. The majority of these drugs target the catalytic and allosteric sites of the HIV enzyme reverse transcriptase. Compared to the NRTI family of drugs, the diverse chemical class of non-nucleoside reverse transcriptase inhibitors (NNRTIs) has special anti-HIV activity with high specificity and low toxicity. However, current clinical usage of NRTI and NNRTI drugs has limited therapeutic value due to their adverse drug reactions and the emergence of multidrug-resistant (MDR) strains. To overcome drug resistance and efficacy issues, combination therapy is widely prescribed for HIV patients. Combination antiretroviral therapy (cART) includes more than one antiretroviral agent targeting two or more enzymes in the life cycle of the virus. Medicinal chemistry researchers apply different optimization strategies including structure- and fragment-based drug design, prodrug approach, scaffold hopping, molecular/fragment hybridization, bioisosterism, high-throughput screening, covalent-binding, targeting highly hydrophobic channel, targeting dual site, and multi-target-directed ligand to identify and develop novel NNRTIs with high antiviral activity against wild-type (WT) and mutant strains. The formulation experts design various delivery systems with single or combination therapies and long-acting regimens of NNRTIs to improve pharmacokinetic profiles and provide sustained therapeutic effects.
    MeSH term(s) Humans ; Reverse Transcriptase Inhibitors/pharmacology ; Reverse Transcriptase Inhibitors/therapeutic use ; HIV Infections/drug therapy ; HIV-1 ; Acquired Immunodeficiency Syndrome/drug therapy ; Zidovudine/therapeutic use ; HIV Reverse Transcriptase/genetics ; HIV Reverse Transcriptase/chemistry ; Anti-HIV Agents/adverse effects
    Chemical Substances Reverse Transcriptase Inhibitors ; Zidovudine (4B9XT59T7S) ; HIV Reverse Transcriptase (EC 2.7.7.49) ; Anti-HIV Agents
    Language English
    Publishing date 2023-09-25
    Publishing country Switzerland
    Document type Journal Article ; Review
    ZDB-ID 2516098-9
    ISSN 1999-4915 ; 1999-4915
    ISSN (online) 1999-4915
    ISSN 1999-4915
    DOI 10.3390/v15101992
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article: Dual Anti-Inflammatory and Anticancer Activity of Novel 1,5-Diaryl Pyrazole Derivatives: Molecular Modeling, Synthesis, In Vitro Activity, and Dynamics Study.

    Deivasigamani, Priya / Rubavathy, S M Esther / Jayasankar, Narayanan / Saravanan, Venkatesan / Thilagavathi, Ramasamy / Prakash, Muthuramalingam / Selvam, Chelliah / Rajagopal, Rajakrishnan / Alfarhan, Ahmed / Kathiravan, Muthu Kumaradoss / Arokiyaraj, Selvaraj / Arockiaraj, Jesu

    Biomedicines

    2024  Volume 12, Issue 4

    Abstract: A series of novel 1,5-diaryl pyrazole derivatives targeting the COX enzyme were designed by combined ligand and structure-based approach. The designed molecules were then further subjected to ADMET and molecular docking studies. Out of 34 designed ... ...

    Abstract A series of novel 1,5-diaryl pyrazole derivatives targeting the COX enzyme were designed by combined ligand and structure-based approach. The designed molecules were then further subjected to ADMET and molecular docking studies. Out of 34 designed compounds, the top-10 molecules from the computation studies were synthesized, characterized, and evaluated for COX-2 inhibition and anti-cancer activity. Initially, the target compounds were screened for the protein denaturation assay. The results of the top-five molecules T2, T3, T5, T6, and T9 were further subjected to in vitro COX-2 enzymatic assay and anti-cancer activity. As far as COX-2 inhibitory activity is considered, two compounds, T3 and T5, exhibited the half maximum inhibitory concentration (IC
    Language English
    Publishing date 2024-04-03
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2720867-9
    ISSN 2227-9059
    ISSN 2227-9059
    DOI 10.3390/biomedicines12040788
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  4. Article ; Online: Furan-based Chalcone Annihilates the Multi-Drug-Resistant Pseudomonas aeruginosa and Protects Zebra Fish Against its Infection.

    Nayak, Santosh Pushpa Ramya Ranjan / Basty, Catharine / Boopathi, Seenivasan / Dhivya, Loganathan Sumathi / Alarjani, Khaloud Mohammed / Gawwad, Mohamed Ragab Abdel / Hager, Raghda / Kathiravan, Muthu Kumaradoss / Arockiaraj, Jesu

    Journal of microbiology (Seoul, Korea)

    2024  Volume 62, Issue 2, Page(s) 75–89

    Abstract: The emergence of carbapenem-resistant Pseudomonas aeruginosa, a multi-drug-resistant bacteria, is becoming a serious public health concern. This bacterium infects immunocompromised patients and has a high fatality rate. Both naturally and synthetically ... ...

    Abstract The emergence of carbapenem-resistant Pseudomonas aeruginosa, a multi-drug-resistant bacteria, is becoming a serious public health concern. This bacterium infects immunocompromised patients and has a high fatality rate. Both naturally and synthetically produced chalcones are known to have a wide array of biological activities. The antibacterial properties of synthetically produced chalcone were studied against P. aeruginosa. In vitro, study of the compound (chalcone derivative named DKO1), also known as (2E)-1-(5-methylfuran-2-yl)-3-(4-nitrophenyl) prop-2-en-1-one, had substantial antibacterial and biofilm disruptive action. DKO1 effectively shielded against P. aeruginosa-induced inflammation, oxidative stress, lipid peroxidation, and apoptosis in zebrafish larvae. In adult zebrafish, the treatment enhanced the chances of survivability and reduced the sickness-like behaviors. Gene expression, biochemical analysis, and histopathology studies found that proinflammatory cytokines (TNF-α, IL-1β, IL-6, iNOS) were down regulated; antioxidant enzymes such as superoxide dismutase (SOD) and catalase (CAT) levels increased, and histoarchitecture was restored in zebrafish. The data indicate that DKO1 is an effective antibacterial agent against P. aeruginosa demonstrated both in vitro and in vivo.
    MeSH term(s) Adult ; Animals ; Humans ; Zebrafish ; Pseudomonas aeruginosa/metabolism ; Chalcone/metabolism ; Chalcone/pharmacology ; Chalcones/metabolism ; Chalcones/pharmacology ; Anti-Bacterial Agents/pharmacology ; Anti-Bacterial Agents/metabolism ; Bacteria ; Microbial Sensitivity Tests
    Chemical Substances Chalcone (5S5A2Q39HX) ; Chalcones ; Anti-Bacterial Agents
    Language English
    Publishing date 2024-02-21
    Publishing country Korea (South)
    Document type Journal Article
    ZDB-ID 2012399-1
    ISSN 1976-3794 ; 1225-8873
    ISSN (online) 1976-3794
    ISSN 1225-8873
    DOI 10.1007/s12275-024-00103-6
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 5211: Show issues Location:
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    Jg. 1995 - 2021: Lesesall (2.OG)
    ab Jg. 2022: Lesesaal (EG)

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  5. Article ; Online: An Overview of Spike Surface Glycoprotein in Severe Acute Respiratory Syndrome–Coronavirus

    Muthu Kumaradoss Kathiravan / Srimathi Radhakrishnan / Vigneshwaran Namasivayam / Senthilkumar Palaniappan

    Frontiers in Molecular Biosciences, Vol

    2021  Volume 8

    Abstract: The novel coronavirus originated in December 2019 in Hubei, China. This contagious disease named as COVID-19 resulted in a massive expansion within 6 months by spreading to more than 213 countries. Despite the availability of antiviral drugs for the ... ...

    Abstract The novel coronavirus originated in December 2019 in Hubei, China. This contagious disease named as COVID-19 resulted in a massive expansion within 6 months by spreading to more than 213 countries. Despite the availability of antiviral drugs for the treatment of various viral infections, it was concluded by the WHO that there is no medicine to treat novel CoV, SARS-CoV-2. It has been confirmed that SARS-COV-2 is the most highly virulent human coronavirus and occupies the third position following SARS and MERS with the highest mortality rate. The genetic assembly of SARS-CoV-2 is segmented into structural and non-structural proteins, of which two-thirds of the viral genome encodes non-structural proteins and the remaining genome encodes structural proteins. The most predominant structural proteins that make up SARS-CoV-2 include spike surface glycoproteins (S), membrane proteins (M), envelope proteins (E), and nucleocapsid proteins (N). This review will focus on one of the four major structural proteins in the CoV assembly, the spike, which is involved in host cell recognition and the fusion process. The monomer disintegrates into S1 and S2 subunits with the S1 domain necessitating binding of the virus to its host cell receptor and the S2 domain mediating the viral fusion. On viral infection by the host, the S protein is further cleaved by the protease enzyme to two major subdomains S1/S2. Spike is proven to be an interesting target for developing vaccines and in particular, the RBD-single chain dimer has shown initial success. The availability of small molecules and peptidic inhibitors for host cell receptors is briefly discussed. The development of new molecules and therapeutic druggable targets for SARS-CoV-2 is of global importance. Attacking the virus employing multiple targets and strategies is the best way to inhibit the virus. This article will appeal to researchers in understanding the structural and biological aspects of the S protein in the field of drug design and discovery.
    Keywords SARS-CoV-2 ; coronavirus ; spike (S) glycoprotein ; entry inhibitors ; corona ; Biology (General) ; QH301-705.5
    Subject code 572
    Language English
    Publishing date 2021-03-01T00:00:00Z
    Publisher Frontiers Media S.A.
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  6. Article ; Online: Discovery and development of COVID-19 vaccine from laboratory to clinic.

    Saravanan, Venkatesan / Chagaleti, Bharath Kumar / Narayanan, Pavithra Lakshmi / Anandan, Vijay Babu / Manoharan, Haritha / Anjana, G V / Peraman, Ramalingam / Namasivayam, S Karthik Raja / Kavisri, M / Arockiaraj, Jesu / Muthu Kumaradoss, Kathiravan / Moovendhan, Meivelu

    Chemical biology & drug design

    2023  Volume 103, Issue 1, Page(s) e14383

    Abstract: The world has recently experienced one of the biggest and most severe public health disasters with severe acute respiratory syndrome coronavirus (SARS-CoV-2). SARS-CoV-2 is responsible for the coronavirus disease of 2019 (COVID-19) which is one of the ... ...

    Abstract The world has recently experienced one of the biggest and most severe public health disasters with severe acute respiratory syndrome coronavirus (SARS-CoV-2). SARS-CoV-2 is responsible for the coronavirus disease of 2019 (COVID-19) which is one of the most widespread and powerful infections affecting human lungs. Current figures show that the epidemic had reached 216 nations, where it had killed about 6,438,926 individuals and infected 590,405,710. WHO proclaimed the outbreak of the Ebola virus disease (EVD), in 2014 that killed hundreds of people in West Africa. The development of vaccines for SARS-CoV-2 becomes more difficult due to the viral mutation in its non-structural proteins (NSPs) especially NSP2 and NSP3, S protein, and RNA-dependent RNA polymerase (RdRp). Continuous monitoring of SARS-CoV-2, dynamics of the genomic sequence, and spike protein mutations are very important for the successful development of vaccines with good efficacy. Hence, the vaccine development for SARS-CoV-2 faces specific challenges starting from viral mutation. The requirement of long-term immunity development, safety, efficacy, stability, vaccine allocation, distribution, and finally, its cost is discussed in detail. Currently, 169 vaccines are in the clinical development stage, while 198 vaccines are in the preclinical development stage. The majority of these vaccines belong to the Ps-Protein subunit type which has 54, and the minor BacAg-SPV (Bacterial antigen-spore expression vector) type, at least 1 vaccination. The use of computational methods and models for vaccine development has revolutionized the traditional methods of vaccine development. Further, this updated review highlights the upcoming vaccine development strategies in response to the current pandemic and post-pandemic era, in the field of vaccine development.
    MeSH term(s) Humans ; COVID-19 Vaccines ; COVID-19/prevention & control ; SARS-CoV-2 ; Viral Vaccines ; Pandemics/prevention & control
    Chemical Substances COVID-19 Vaccines ; Viral Vaccines
    Language English
    Publishing date 2023-11-13
    Publishing country England
    Document type Journal Article ; Review
    ZDB-ID 2216600-2
    ISSN 1747-0285 ; 1747-0277
    ISSN (online) 1747-0285
    ISSN 1747-0277
    DOI 10.1111/cbdd.14383
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  7. Article: An Overview of Spike Surface Glycoprotein in Severe Acute Respiratory Syndrome-Coronavirus.

    Kathiravan, Muthu Kumaradoss / Radhakrishnan, Srimathi / Namasivayam, Vigneshwaran / Palaniappan, Senthilkumar

    Frontiers in molecular biosciences

    2021  Volume 8, Page(s) 637550

    Abstract: The novel coronavirus originated in December 2019 in Hubei, China. This contagious disease named as COVID-19 resulted in a massive expansion within 6 months by spreading to more than 213 countries. Despite the availability of antiviral drugs for the ... ...

    Abstract The novel coronavirus originated in December 2019 in Hubei, China. This contagious disease named as COVID-19 resulted in a massive expansion within 6 months by spreading to more than 213 countries. Despite the availability of antiviral drugs for the treatment of various viral infections, it was concluded by the WHO that there is no medicine to treat novel CoV, SARS-CoV-2. It has been confirmed that SARS-COV-2 is the most highly virulent human coronavirus and occupies the third position following SARS and MERS with the highest mortality rate. The genetic assembly of SARS-CoV-2 is segmented into structural and non-structural proteins, of which two-thirds of the viral genome encodes non-structural proteins and the remaining genome encodes structural proteins. The most predominant structural proteins that make up SARS-CoV-2 include spike surface glycoproteins (S), membrane proteins (M), envelope proteins (E), and nucleocapsid proteins (N). This review will focus on one of the four major structural proteins in the CoV assembly, the spike, which is involved in host cell recognition and the fusion process. The monomer disintegrates into S1 and S2 subunits with the S1 domain necessitating binding of the virus to its host cell receptor and the S2 domain mediating the viral fusion. On viral infection by the host, the S protein is further cleaved by the protease enzyme to two major subdomains S1/S2. Spike is proven to be an interesting target for developing vaccines and in particular, the RBD-single chain dimer has shown initial success. The availability of small molecules and peptidic inhibitors for host cell receptors is briefly discussed. The development of new molecules and therapeutic druggable targets for SARS-CoV-2 is of global importance. Attacking the virus employing multiple targets and strategies is the best way to inhibit the virus. This article will appeal to researchers in understanding the structural and biological aspects of the S protein in the field of drug design and discovery.
    Language English
    Publishing date 2021-03-16
    Publishing country Switzerland
    Document type Journal Article ; Review
    ZDB-ID 2814330-9
    ISSN 2296-889X
    ISSN 2296-889X
    DOI 10.3389/fmolb.2021.637550
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  8. Article ; Online: Exploring Pyrimidine Pharmacophore as Thymidine Monophosphate Kinase Inhibitors for Antitubercular Activity: A Review.

    Chitre, Trupti Sameer / Asgaonkar, Kalyani Dhirendra / Patil, Shital Manoj / Kathiravan, Muthu Kumaradoss / Padhye, Subhash Balkrishna

    Current topics in medicinal chemistry

    2016  Volume 16, Issue 28, Page(s) 3211–3223

    Abstract: Tuberculosis (TB) has been declared as a health emergency due to emergence of resistant strains of M. tuberculosis, multidrug resistant (MDR), extensively drug resistant (XDR) TB strains and totally drug resistant tuberculosis (TDR-TB) reported recently ... ...

    Abstract Tuberculosis (TB) has been declared as a health emergency due to emergence of resistant strains of M. tuberculosis, multidrug resistant (MDR), extensively drug resistant (XDR) TB strains and totally drug resistant tuberculosis (TDR-TB) reported recently in some parts of the world. Therefore, the current situation necessitates developing new antitubercular agents acting on novel targets for effectively controlling TB. Thymidine Monophosphate Kinase (TMPKmt) enzyme is one such target, which is being explored. This review focuses on Structure Activity Relationship studies (SARs) and computational studies of various nucleotide and nucleoside derivatives of pyrimidine analogs reported as TMPKmt inhibitors.
    MeSH term(s) Enzyme Inhibitors/pharmacology ; Humans ; Nucleoside-Phosphate Kinase/antagonists & inhibitors ; Pyrimidines/chemistry
    Chemical Substances Enzyme Inhibitors ; Pyrimidines ; Nucleoside-Phosphate Kinase (EC 2.7.4.4) ; dTMP kinase (EC 2.7.4.9)
    Language English
    Publishing date 2016-04-19
    Publishing country United Arab Emirates
    Document type Journal Article ; Review
    ZDB-ID 2064823-6
    ISSN 1873-4294 ; 1568-0266
    ISSN (online) 1873-4294
    ISSN 1568-0266
    DOI 10.2174/1568026616666160506130914
    Database MEDical Literature Analysis and Retrieval System OnLINE

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