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  1. Article ; Online: In vitro

    Bakale, Rajubai D / Phatak, Pramod S / Rathod, Sanket S / Choudhari, Prafulla B / Rekha, Estharla Madhu / Sriram, Dharmarajan / Kulkarni, Ravibhushan S / Haval, Kishan P

    Journal of biomolecular structure & dynamics

    2023  , Page(s) 1–20

    Abstract: In the present study, we have reported the synthesis of novel isoniazid-triazole derivatives ( ...

    Abstract In the present study, we have reported the synthesis of novel isoniazid-triazole derivatives (
    Language English
    Publishing date 2023-12-11
    Publishing country England
    Document type Journal Article
    ZDB-ID 49157-3
    ISSN 1538-0254 ; 0739-1102
    ISSN (online) 1538-0254
    ISSN 0739-1102
    DOI 10.1080/07391102.2023.2291826
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Design and synthesis of new indanol-1,2,3-triazole derivatives as potent antitubercular and antimicrobial agents.

    Phatak, Pramod S / Bakale, Rajubai D / Kulkarni, Ravibhushan S / Dhumal, Sambhaji T / Dixit, Prashant P / Krishna, Vagolu Siva / Sriram, Dharmarajan / Khedkar, Vijay M / Haval, Kishan P

    Bioorganic & medicinal chemistry letters

    2020  Volume 30, Issue 22, Page(s) 127579

    Abstract: In a search of new antitubercular agents, herein we have reported a series of new thirty-two indanol-1,2,3-triazole derivatives. The synthesized compounds were screened for their in vitro antitubercular and antimicrobial activities. Among the screened ... ...

    Abstract In a search of new antitubercular agents, herein we have reported a series of new thirty-two indanol-1,2,3-triazole derivatives. The synthesized compounds were screened for their in vitro antitubercular and antimicrobial activities. Among the screened compounds, most of the compounds have displayed good antitubercular activity against Mycobacterium tuberculosis H37Rv. The compound 5g has been identified as potent antitubercular agent with MIC value 1.56 µM. The most active compounds of the series were further studied for their cytotoxicity against HEK 293 cells using MTT assay and found to be nontoxic. In addition, ten compounds were shown good antimicrobial activities against both antibacterial and antifungal pathogens. A molecular docking study against Mycobacterial enoyl-ACP-reductase (InhA) was performed to gain an insight into the molecular mechanism of antitubercular action. The pharmacokinetic parameters of these compounds were studied and displayed acceptable drug-likeness score.
    MeSH term(s) Antitubercular Agents/chemical synthesis ; Antitubercular Agents/chemistry ; Antitubercular Agents/pharmacology ; Dose-Response Relationship, Drug ; Drug Design ; HEK293 Cells ; Humans ; Microbial Sensitivity Tests ; Molecular Structure ; Mycobacterium tuberculosis/drug effects ; Structure-Activity Relationship ; Triazoles/chemical synthesis ; Triazoles/chemistry ; Triazoles/pharmacology
    Chemical Substances Antitubercular Agents ; Triazoles
    Language English
    Publishing date 2020-09-25
    Publishing country England
    Document type Journal Article
    ZDB-ID 1063195-1
    ISSN 1464-3405 ; 0960-894X
    ISSN (online) 1464-3405
    ISSN 0960-894X
    DOI 10.1016/j.bmcl.2020.127579
    Database MEDical Literature Analysis and Retrieval System OnLINE

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