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  • 1
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    In silico study, synthesis, and evaluation of the antimalarial activity of hybrid dimethoxy pyrazole 1,3,5‐triazine derivatives
    Wiley ; 2021
    In:  Journal of Biochemical and Molecular Toxicology Vol. 35, No. 3 ( 2021-03)
    Details
    In: Journal of Biochemical and Molecular Toxicology, Wiley, Vol. 35, No. 3 ( 2021-03)
    Abstract: Malaria continues to become a major global health problem, particularly in Sub‐Saharan Africa, Asia, and Latin America. The widespread emergence of resistance to first‐line drugs has further bolstered an urgent need for a new and cost‐effective antimalarial(s). Thus, the present study enumerates the synthesis of novel hybrid dimethoxy pyrazole 1,3,5‐triazine derivatives  7 ( a – j ) and their in silico results short‐listed three compounds with good binding energies and dock scores. Docking analysis shows that hydrogen‐bonding predominates and typically involves key residues, such as Asp54, Tyr170, Ile164, and Arg122. The in vitro antimalarial evaluation of three top‐ranked compounds ( 7e , 7g , and 7h ) showed half‐maximal inhibitory concentration values range from 53.85 to 100 μg/ml against chloroquine‐sensitive strain 3D7 of Plasmodium falciparum . Compound 7e may be utilized as a lead for further optimization work in drug discovery due to good antimalarial activity.
    Type of Medium: Online Resource
    ISSN: 1095-6670 , 1099-0461
    URL: Issue
    URL: Article
    DOI: 10.1002/jbt.v35.3
    DOI: 10.1002/jbt.22682
    Language: English
    Publisher: Wiley
    Publication Date: 2021
    detail.hit.zdb_id: 1481995-8
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  • 2
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    Microwave‐assisted synthesis of hybrid PABA‐1,3,5‐triazine derivatives as an antimalarial agent
    Wiley ; 2021
    In:  Journal of Biochemical and Molecular Toxicology Vol. 35, No. 9 ( 2021-09)
    Details
    In: Journal of Biochemical and Molecular Toxicology, Wiley, Vol. 35, No. 9 ( 2021-09)
    Abstract: The present manuscript deals with the development of novel p ‐aminobenzoic acid (PABA) associated 1,3,5‐triazine derivatives as antimalarial agents. The molecules were developed via microwave‐assisted synthesis and structures of compounds were ascertained via numerous analytical and spectroscopic techniques. The synthesized compounds were also subjected to ADMET analysis. In a docking analysis, the title compounds showed high and diverse binding affinities towards wild (−162.45 to −369.38 kcal/mol) and quadruple mutant (−165.36 to −209.47 kcal/mol) Pf‐ DHFR‐TS via interacting with Phe58, Arg59, Ser111, Ile112, Phe116. The in vitro antimalarial activity suggested that compounds 4e , 4b , and 4h showed IC 50 ranging from 4.18 to 8.66 μg/ml against the chloroquine‐sensitive (3D7) strain of Plasmodium falciparum . Moreover, compounds 4g , 4b , 4e , and 4c showed IC 50 ranging from 8.12 to 12.09 μg/ml against chloroquine‐resistant (Dd2) strain. In conclusion, our study demonstrated the development of hybrid PABA substituted 1,3,5‐triazines as a novel class of Pf ‐DHFR inhibitor for antimalarial drug discovery.
    Type of Medium: Online Resource
    ISSN: 1095-6670 , 1099-0461
    URL: Issue
    URL: Article
    DOI: 10.1002/jbt.v35.9
    DOI: 10.1002/jbt.22860
    Language: English
    Publisher: Wiley
    Publication Date: 2021
    detail.hit.zdb_id: 1481995-8
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  • 3
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    Online Resource
    Design, Facile Synthesis, and Antibacterial Activity of Hybrid 1,3,4‐thiadiazole‐1,3,5‐triazine Derivatives Tethered via –S– Bridge
    Wiley ; 2012
    In:  Chemical Biology & Drug Design Vol. 80, No. 4 ( 2012-10), p. 598-604
    Details
    In: Chemical Biology & Drug Design, Wiley, Vol. 80, No. 4 ( 2012-10), p. 598-604
    Abstract: Some hybrid 1,3,4‐thiadiazole‐1,3,5‐triazine derivatives tethered via –S– bridge were synthesized and characterized with the aid of spectroscopic and elemental analysis. These hybrid conjugates were then investigated for their antibacterial activity against selected Gram‐positive and Gram‐negative bacteria. Excellent to moderate antibacterial activity was presented by the target compounds.
    Type of Medium: Online Resource
    ISSN: 1747-0277 , 1747-0285
    URL: Issue
    URL: Article
    DOI: 10.1111/jpp.2012.80.issue-4
    DOI: 10.1111/j.1747-0285.2012.01433.x
    Language: English
    Publisher: Wiley
    Publication Date: 2012
    detail.hit.zdb_id: 2216600-2
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  • 4
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    Investigation of Oral Subacute Toxicity and In-Vitro Antioxidant Activity of Standardized Methanolic Extract of Quercus serrata Leaves
    Bentham Science Publishers Ltd. ; 2021
    In:  Current Bioactive Compounds Vol. 17, No. 9 ( 2021-11)
    Details
    In: Current Bioactive Compounds, Bentham Science Publishers Ltd., Vol. 17, No. 9 ( 2021-11)
    Abstract: Quercus serrata Murray leaves are traditionally used for the treatment of diabetes, dysmenorrhoea, inflammation and urinary tract infection. So, far no study has reported on the toxicological profile and antioxidant properties of the plant. Objective: The present study aimed to investigate the in-vivo toxicological profile and in-vitro antioxidant activities of the methanolic extract of standardized Quercus serrata leaves. Methods: Per-oral sub-acute toxicity study was performed in rats using three dose levels (200, 400 and 800 mg/kg b.w.) of the extract for 28 days. The control group received gum acacia suspended in water. Bodyweight was measured weekly. Biochemical parameters were analysed using the serum; the blood-cell count was performed using the whole blood. Pathological changes were also checked in highly perfused tissues. Further, in-vitro reducing power assay, nitric oxide scavenging assay, and DPPH free-radical scavenging assay were performed to evaluate the antioxidant activity of the extract. Results: There were no significant alterations found in the blood-cell count and biochemical parameters analysed in the treatment group when compared with the normal control. Histopathology study of liver, kidney, pancreas, heart and brain revealed normal cellular architecture in the treatment groups alike the control group animals. Quercus serrata also showed a significant reduction of DPPH with an IC 50 value of 4.48±0.254 μg/mL, in-vitro reducing power activity with an IC 50 value of 121.65±0.320 μg/mL and nitric oxide scavenging activity with an IC50 value of 106.43±0.338 μg/mL. Conclusion: The study showed that standardized methanolic extract of Quercus serrata leaves was safe after sub-acute oral administration in rats and possesses good antioxidant potential.
    Type of Medium: Online Resource
    ISSN: 1573-4072
    URL: Article
    DOI: 10.2174/1573407216999201224150602
    Language: English
    Publisher: Bentham Science Publishers Ltd.
    Publication Date: 2021
    SSG: 15,3
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  • 5
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    Online Resource
    Discovery of novel 1,3,5‐triazine as adenosine A 2A receptor antagonist for benefit in Parkinson's disease
    Wiley ; 2021
    In:  Journal of Biochemical and Molecular Toxicology Vol. 35, No. 3 ( 2021-03)
    Details
    In: Journal of Biochemical and Molecular Toxicology, Wiley, Vol. 35, No. 3 ( 2021-03)
    Abstract: Parkinson's disease (PD) is a chronic neuro‐degenerative ailment characterized by impairment in various motor and nonmotor functions of the body. In the past few years, adenosine A 2 A receptor (A 2 AR) antagonists have attracted much attention due to significant relief in PD. Therefore, in the current study, we intend to disclose the development of novel 1,3,5‐triazines as A 2 AR antagonist. The radioligand binding and selectivity of analogs were tested in HEK293 (human embryonic kidney) and the cells were transfected with pcDNA 3.1(+) containing full‐length human A 2 AR cDNA and pcDNA 3.1(+) containing full‐length human A 1 R cDNA, where they exhibit selective affinity for A 2 AR. Molecular docking analysis was also conducted to rationalize the probable mode of action, binding affinity, and orientation of the most potent molecule ( 7c ) at the active site of A 2 AR. It has been shown that compound 7c form numerous nonbonded interactions in the active site of A 2 AR by interacting with Ala59, Ala63, Ile80, Val84 Glu169, Phe168, Met270, and Ile274. The study revealed 1,3,5‐triazines as a novel class of A 2 AR antagonists.
    Type of Medium: Online Resource
    ISSN: 1095-6670 , 1099-0461
    URL: Issue
    URL: Article
    DOI: 10.1002/jbt.v35.3
    DOI: 10.1002/jbt.22659
    Language: English
    Publisher: Wiley
    Publication Date: 2021
    detail.hit.zdb_id: 1481995-8
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  • 6
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    Design and development of novel N ‐(4‐aminobenzoyl)‐ l ‐glutamic acid conjugated 1,3,5‐triazine derivatives as Pf ‐DHFR inhibitor: An in‐silico and in‐vitro study
    Wiley ; 2023
    In:  Journal of Biochemical and Molecular Toxicology Vol. 37, No. 4 ( 2023-04)
    Details
    In: Journal of Biochemical and Molecular Toxicology, Wiley, Vol. 37, No. 4 ( 2023-04)
    Abstract: In the present work, a library of 120 compounds was prepared using various aliphatic and aromatic amines. Finally, 10 compounds were selected through in silico screening carrying 4‐aminobenzoyl‐ l ‐glutamic acid and 1,3,5‐triazine moiety. The docking results of compounds 4d16 and 4d38 revealed higher binding interaction with amino acids Asp54 (−537.96 kcal/mol) and Asp54, Phe116 (−618.22 kcal/mol) against wild (1J3I) and quadruple mutant (1J3K) type of Pf ‐DHFR inhibitors and were comparable to standard WR99210. These compounds were developed by facile and microwave‐assisted synthesis via nucleophilic substitution reaction and characterized by different spectroscopic methods. In vitro antimalarial assay results also suggested that these two compounds were having higher antimalarial activity against chloroquine‐sensitive (3D7) and chloroquine‐resistant (Dd2) strain out of the ten synthesized compounds with IC 50 13.25 μM and 14.72 μM, respectively. These hybrid scaffolds might be useful in the lead discovery of a new class of Pf ‐DHFR inhibitors.
    Type of Medium: Online Resource
    ISSN: 1095-6670 , 1099-0461
    URL: Issue
    URL: Article
    DOI: 10.1002/jbt.v37.4
    DOI: 10.1002/jbt.23290
    Language: English
    Publisher: Wiley
    Publication Date: 2023
    detail.hit.zdb_id: 1481995-8
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  • 7
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    Discovery of novel pyrazole derivatives as a potent anti‐inflammatory agent in RAW264.7 cells via inhibition of NF‐ĸB for possible benefit against SARS‐CoV‐2
    Wiley ; 2021
    In:  Journal of Biochemical and Molecular Toxicology Vol. 35, No. 3 ( 2021-03)
    Details
    In: Journal of Biochemical and Molecular Toxicology, Wiley, Vol. 35, No. 3 ( 2021-03)
    Abstract: Due to unavailability of a specific drug/vaccine to attenuate severe acute respiratory syndrome coronavirus 2, the current strategy to combat the infection has been largely dependent upon the use of anti‐inflammatory drugs to control cytokines storm responsible for respiratory depression. Thus, in this study, we discovered novel pyrazole analogs as a potent nuclear factor kappa B (NF‐ĸB) inhibitor. The compounds were assessed for NF‐ĸB transcriptional inhibitory activity in RAW264.7 cells after stimulation with lipopolysaccharides (LPS), revealing Compound 6c as the most potent analog among the tested series. The effect of Compound 6c was further investigated on the levels of interleukin‐1β, tumor necrosis factor‐α, and interleukin‐6 in LPS‐stimulated RAW267.4 cells by enzyme immunoassay, where it causes a significant reduction in the level of these cytokines. In Western blot analysis, Compound 6c also causes the inhibition of inhibitor kappa B‐α and NF‐κB. It was found to be snugly fitted into the inner grove of the active site of NF‐ĸB by forming H‐bonds and a nonbonded interaction with Asn28 in a docking analysis.
    Type of Medium: Online Resource
    ISSN: 1095-6670 , 1099-0461
    URL: Issue
    URL: Article
    DOI: 10.1002/jbt.v35.3
    DOI: 10.1002/jbt.22656
    Language: English
    Publisher: Wiley
    Publication Date: 2021
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  • 8
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    Implication of in silico studies in the search for novel inhibitors against SARS‐CoV‐2
    Wiley ; 2022
    In:  Archiv der Pharmazie Vol. 355, No. 5 ( 2022-05)
    Details
    In: Archiv der Pharmazie, Wiley, Vol. 355, No. 5 ( 2022-05)
    Abstract: Corona Virus Disease‐19 (COVID‐19) is a pandemic disease mainly caused by severe acute respiratory syndrome coronavirus 2 (SARS‐CoV‐2). It had spread from Wuhan, China, in late 2019 and spread over 222 countries and territories all over the world. Earlier, at the very beginning of COVID‐19 infection, there were no approved medicines or vaccines for combating this disease, which adversely affected a lot of individuals worldwide. Although frequent mutation leads to the generation of more deadly variants of SARS‐CoV‐2, researchers have developed several highly effective vaccines that were approved for emergency use by the World Health Organization (WHO), such as mRNA‐1273 by Moderna, BNT162b2 by Pfizer/BioNTech, Ad26.COV2.S by Janssen, AZD1222 by Oxford/AstraZeneca, Covishield by the Serum Institute of India, BBIBP‐CorV by Sinopharm, coronaVac by Sinovac, and Covaxin by Bharat Biotech, and the first US Food and Drug Administration‐approved antiviral drug Veklury (remdesivir) for the treatment of COVID‐19. Several waves of COVID‐19 have already occurred worldwide, and good‐quality vaccines and medicines should be available for ongoing as well as upcoming waves of the pandemic. Therefore, in silico studies have become an excellent tool for identifying possible ligands that could lead to the development of safer medicines or vaccines. Various phytoconstituents from plants and herbs with antiviral properties are studied further to obtain inhibitors of SARS‐CoV‐2. In silico screening of various molecular databases like PubChem, ZINC, Asinex Biol‐Design Library, and so on has been performed extensively for finding effective ligands against targets. Herein, in silico studies carried out by various researchers are summarized so that one can easily find the best molecule for further in vitro and in vivo studies.
    Type of Medium: Online Resource
    ISSN: 0365-6233 , 1521-4184
    URL: Issue
    URL: Article
    DOI: 10.1002/ardp.v355.5
    DOI: 10.1002/ardp.202100360
    Language: English
    Publisher: Wiley
    Publication Date: 2022
    detail.hit.zdb_id: 1496815-0
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  • 9
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    An Overview of Phytochemical and Pharmacological Profile of Morus alba Linn
    Bentham Science Publishers Ltd. ; 2021
    In:  Current Bioactive Compounds Vol. 17, No. 8 ( 2021-10)
    Details
    In: Current Bioactive Compounds, Bentham Science Publishers Ltd., Vol. 17, No. 8 ( 2021-10)
    Abstract: Morus alba Linn. commonly known as white mulberry, belongs to the family Moraceae, and is a promising traditional medicine. In Asia, besides its use in the preparation of delicacies, every part of this plant is utilized in traditional medicine. Over the past decade, studies related to the identification and isolation of biologically active compounds, with flavonoids as the major class of phytoconstituents, from this plant have been reported. These phytoconstituents are not only found to be beneficial for the maintenance of general health but also are associated with a range of potential pharmacological activities such as antioxidant, anti-inflammatory, anti- diabetic, anticancer, hepatoprotective, cardioprotective, neuroprotective to name a few. Objective: This review aims to provide upgraded and comprehensive information regarding the phytochemical, ethnomedicinal use and pharmacological profile of the plant Morus alba Linn. Method: The significant information has been collected through various databases viz. PubMed, Scopus, Web of Science, Science Direct based on the recent findings, using different terms of Morus alba. Results: The outcome of the study suggests that Morus alba is a multifunctional plant with numerous phytochemicals, and possesses a range of pharmacological activities. Conclusion: The data assembled on Morus alba will be beneficial to trigger research in various fields of pharmaceutical and allied sciences to explore the medicinal importance of this unique plant.
    Type of Medium: Online Resource
    ISSN: 1573-4072
    URL: Article
    DOI: 10.2174/1573407216666201228114004
    Language: English
    Publisher: Bentham Science Publishers Ltd.
    Publication Date: 2021
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  • 10
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    Online Resource
    Design, Synthesis, Antibacterial Activity, and Molecular Docking Studies of Novel Hybrid 1,3‐Thiazine‐1,3,5‐Triazine Derivatives as Potential Bacterial Translation Inhibitor
    Wiley ; 2012
    In:  Chemical Biology & Drug Design Vol. 80, No. 4 ( 2012-10), p. 572-583
    Details
    In: Chemical Biology & Drug Design, Wiley, Vol. 80, No. 4 ( 2012-10), p. 572-583
    Abstract: Some novel hybrid 1,3‐thiazine‐1,3,5‐triazine derivatives were synthesized and tested for antibacterial activity. Compounds 8c and 8f were found active against Gram positive and Gram negative microorganisms. Molecular docking studies have been performed on eubacterial ribosomal decoding A site ( Escherichia coli 16S rRNA A site) to rationalize the probable mode of action, binding affinity, and orientation of the molecules at the active site of receptor. The structures of all these newly synthesized compounds were confirmed by their elemental analyses and spectral data techniques viz. IR, 1 H NMR, 13 C NMR, and mass.
    Type of Medium: Online Resource
    ISSN: 1747-0277 , 1747-0285
    URL: Issue
    URL: Article
    DOI: 10.1111/jpp.2012.80.issue-4
    DOI: 10.1111/j.1747-0285.2012.01430.x
    Language: English
    Publisher: Wiley
    Publication Date: 2012
    detail.hit.zdb_id: 2216600-2
    SSG: 12
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