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  1. Article ; Online: An Overview of Pharmaceutical Care in Type II Diabetes Mellitus Patients: Current Position and Prospects.

    Theivasigamani, Kumutha / Palaniappan, Senthilkumar

    Current diabetes reviews

    2023  Volume 20, Issue 2, Page(s) e050523216588

    Abstract: Diabetes mellitus is an ongoing disease that is related to a high mortality rate due to severe complications. Diabetes mellitus type 2 (DMT2) is a persistent metabolic deficiency and its prevalence has been increasing consistently worldwide. As a result, ...

    Abstract Diabetes mellitus is an ongoing disease that is related to a high mortality rate due to severe complications. Diabetes mellitus type 2 (DMT2) is a persistent metabolic deficiency and its prevalence has been increasing consistently worldwide. As a result, it is rapidly turning into a plague in some parts of the world, and the number of people affected is expected to double in the following decade due to an increase in the maturing populace, adding to the overall existing importance for medical service providers, particularly in the underdeveloped nations. Extensive diabetes care is an intricate task that takes a whole group of medical care experts, including drug specialists, to provide multidisciplinary care for the patients. The duty of drug experts has changed significantly in recent years, changing from conventional drug dispensing in the drug store to patient- centered clinical support services. Upgrading the medication treatment to accomplish better remedial results without causing drug-related issues has been considered the essential objective of treatment for diabetic patients. This review discusses the healthcare needs of patients with T2DM, the current evidence for the role of pharmacists in diabetes care, and insight into the upcoming role of pharmacists in its management. The advanced role of clinical pharmacists in diabetes control through drug treatment, diabetes care centers, and diabetes health counselor schooling, is also discussed in this review.
    MeSH term(s) Humans ; Diabetes Mellitus, Type 2/drug therapy ; Pharmaceutical Services ; Pharmacists
    Language English
    Publishing date 2023-05-03
    Publishing country United Arab Emirates
    Document type Review ; Journal Article
    ISSN 1875-6417
    ISSN (online) 1875-6417
    DOI 10.2174/1573399819666230505123428
    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: 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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  4. Article: Structural Insights to Human Immunodeficiency Virus (HIV-1) Targets and Their Inhibition.

    Vanangamudi, Murugesan / Nair, Pramod C / Engels, S E Maida / Palaniappan, Senthilkumar / Namasivayam, Vigneshwaran

    Advances in experimental medicine and biology

    2021  Volume 1322, Page(s) 63–95

    Abstract: Human immunodeficiency virus (HIV) is a deadly virus that attacks the body's immune system, subsequently leading to AIDS (acquired immunodeficiency syndrome) and ultimately death. Currently, there is no vaccine or effective cure for this infection; ... ...

    Abstract Human immunodeficiency virus (HIV) is a deadly virus that attacks the body's immune system, subsequently leading to AIDS (acquired immunodeficiency syndrome) and ultimately death. Currently, there is no vaccine or effective cure for this infection; however, antiretrovirals that act at various phases of the virus life cycle have been useful to control the viral load in patients. One of the major problems with antiretroviral therapies involves drug resistance. The three-dimensional structure from crystallography studies are instrumental in understanding the structural basis of drug binding to various targets. This chapter provides key insights into different targets and drugs used in the treatment from a structural perspective. Specifically, an insight into the binding characteristics of drugs at the active and allosteric sites of different targets and the importance of targeting allosteric sites for design of new-generation antiretrovirals to overcome complex and resistant forms of the virus has been reviewed.
    MeSH term(s) Acquired Immunodeficiency Syndrome ; Anti-HIV Agents/therapeutic use ; HIV Infections/drug therapy ; HIV-1 ; Humans
    Chemical Substances Anti-HIV Agents
    Language English
    Publishing date 2021-07-13
    Publishing country United States
    Document type Journal Article
    ISSN 2214-8019 ; 0065-2598
    ISSN (online) 2214-8019
    ISSN 0065-2598
    DOI 10.1007/978-981-16-0267-2_3
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article ; Online: Design, Synthesis, and Characterization of Some Hybridized Pyrazolone Pharmacophore Analogs against Mycobacterium tuberculosis.

    Krishnasamy, Sivakumar Kullampalayam / Namasivayam, Vigneshwaran / Mathew, Sincy / Eakambaram, Ragavendran S / Ibrahim, Ibrahim A / Natarajan, Adhirajan / Palaniappan, Senthilkumar

    Archiv der Pharmazie

    2016  Volume 349, Issue 5, Page(s) 383–397

    Abstract: Twenty-seven hybridized pyrazolone analogs were designed, docked, synthesized in two series and evaluated for their in vitro antimycobacterial properties. In the first series, four Schiff base derivatives, 6b, 7b, 7h, and 7i, show good antitubercular ... ...

    Abstract Twenty-seven hybridized pyrazolone analogs were designed, docked, synthesized in two series and evaluated for their in vitro antimycobacterial properties. In the first series, four Schiff base derivatives, 6b, 7b, 7h, and 7i, show good antitubercular activity with minimum inhibition concentration (MIC) values in the range of 32.56-42.55 µM. In the second series, two compounds, 8b and 8c, possessed significant antitubercular activity with MIC <0.37 and <0.44 μM, respectively; they were even more potent than the standards pyrazinamide (12.99 μM), ciprofloxacin (4.82 μM), and streptomycin (5.36 μM), with a selectivity index of >630. Compounds 8b and 8c showed shikimate kinase inhibition activity at 5.84 and 6.93 µM, respectively. The activity and docking results lead to the conclusion that the compounds without double bond in the imine side chain and hydrophobic clashes at the pyrazolone end are necessary for good accommodation in the binding pocket and for imparting flexibility. All the compounds were also tested for antimicrobial activity (antibacterial and antifungal) and show highly significant activities against all the microorganisms tested.
    MeSH term(s) Antitubercular Agents/chemical synthesis ; Antitubercular Agents/chemistry ; Antitubercular Agents/pharmacology ; Ciprofloxacin/pharmacology ; Drug Design ; Microbial Sensitivity Tests ; Molecular Docking Simulation ; Mycobacterium tuberculosis/drug effects ; Phosphotransferases (Alcohol Group Acceptor)/antagonists & inhibitors ; Pyrazinamide/pharmacology ; Pyrazolones/chemical synthesis ; Pyrazolones/chemistry ; Pyrazolones/pharmacology ; Schiff Bases/chemistry ; Schiff Bases/pharmacology ; Streptomycin/pharmacology ; Structure-Activity Relationship
    Chemical Substances Antitubercular Agents ; Pyrazolones ; Schiff Bases ; Pyrazinamide (2KNI5N06TI) ; Ciprofloxacin (5E8K9I0O4U) ; Phosphotransferases (Alcohol Group Acceptor) (EC 2.7.1.-) ; shikimate kinase (EC 2.7.1.71) ; Streptomycin (Y45QSO73OB)
    Language English
    Publishing date 2016-05
    Publishing country Germany
    Document type Journal Article
    ZDB-ID 6381-2
    ISSN 1521-4184 ; 0365-6233 ; 1437-1014
    ISSN (online) 1521-4184
    ISSN 0365-6233 ; 1437-1014
    DOI 10.1002/ardp.201600019
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Uf I Zs.4: Show issues Location:
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  6. Article: Antimycobacterial and phototoxic evaluation of novel 6-fluoro/nitro-4-oxo-7-(sub)-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid.

    Murugesan, Dinakaran / Palaniappan, Senthilkumar / Perumal, Yogeeswari / Arnab, China / Valakunja, Nagaraja / Sriram, Dharmarajan

    International journal of antimicrobial agents

    2008  Volume 31, Issue 4, Page(s) 337–344

    Abstract: Several newer 6-fluoro/nitro-4-oxo-7-(sub)-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acids (10-11a-q) were synthesised from 3,4-difluoro aniline and 3-fluoro-4-nitro aniline by nine-step synthesis. The compounds were evaluated for in vitro and in ... ...

    Abstract Several newer 6-fluoro/nitro-4-oxo-7-(sub)-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acids (10-11a-q) were synthesised from 3,4-difluoro aniline and 3-fluoro-4-nitro aniline by nine-step synthesis. The compounds were evaluated for in vitro and in vivo antimycobacterial activities against Mycobacterium tuberculosis H37Rv (MTB), multidrug-resistant M. tuberculosis (MDR-TB) and Mycobacterium smegmatis (MC2) as well as being tested for their ability to inhibit the supercoiling activity of DNA gyrase from M. smegmatis. Among the synthesised compounds, 7-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-6-nitro-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid (11l) was found to be the most active compound in vitro, with minimum inhibitory concentrations (MICs) of 0.09 microM and <0.09 microM against MTB and MTR-TB, respectively. Compound 11l was found to be 4 times and >506 times more potent than isoniazid against MTB and MDR-TB, respectively. In the in vivo animal model, 11l decreased the bacterial load in lung and spleen tissues by 30% and 42%, respectively, at a dose of 50 mg/kg body weight.
    MeSH term(s) Animals ; Anti-Bacterial Agents/chemistry ; Anti-Bacterial Agents/pharmacology ; Anti-Bacterial Agents/toxicity ; Azetines/chemistry ; Azetines/pharmacology ; Azetines/toxicity ; Cell Survival/drug effects ; Cercopithecus aethiops ; Chemical Phenomena ; Chemistry, Physical ; Dermatitis, Phototoxic/pathology ; Enzyme Inhibitors/pharmacology ; Female ; Lung/drug effects ; Lung/microbiology ; Mice ; Microbial Sensitivity Tests ; Mycobacterium/drug effects ; Mycobacterium Infections/drug therapy ; Mycobacterium Infections/microbiology ; Mycobacterium smegmatis/drug effects ; Mycobacterium tuberculosis/drug effects ; Quinolines/chemistry ; Quinolines/pharmacology ; Quinolines/toxicity ; Spleen/drug effects ; Spleen/microbiology ; Structure-Activity Relationship ; Topoisomerase II Inhibitors ; Vero Cells
    Chemical Substances Anti-Bacterial Agents ; Azetines ; Enzyme Inhibitors ; Quinolines ; Topoisomerase II Inhibitors
    Language English
    Publishing date 2008-04
    Publishing country Netherlands
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 1093977-5
    ISSN 1872-7913 ; 0924-8579
    ISSN (online) 1872-7913
    ISSN 0924-8579
    DOI 10.1016/j.ijantimicag.2007.12.007
    Database MEDical Literature Analysis and Retrieval System OnLINE

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