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  1. Article ; Online: Carbazole-based semicarbazones and hydrazones as multifunctional anti-Alzheimer agents.

    Patel, Kishan B / Patel, Dushyant V / Patel, Nirav R / Kanhed, Ashish M / Teli, Divya M / Gandhi, Bhumi / Shah, Bhavik S / Chaudhary, Bharat N / Prajapati, Navnit K / Patel, Kirti V / Yadav, Mange Ram

    Journal of biomolecular structure & dynamics

    2021  Volume 40, Issue 20, Page(s) 10278–10299

    Abstract: With the aim to combat a multi-faceted neurodegenerative Alzheimer's disease (AD), a series of carbazole-based semicarbazide and hydrazide derivatives were designed, synthesized and assessed for their cholinesterase (ChE) inhibitory, antioxidant and ... ...

    Abstract With the aim to combat a multi-faceted neurodegenerative Alzheimer's disease (AD), a series of carbazole-based semicarbazide and hydrazide derivatives were designed, synthesized and assessed for their cholinesterase (ChE) inhibitory, antioxidant and biometal chelating activity. Among them, (
    MeSH term(s) Humans ; Cholinesterase Inhibitors/pharmacology ; Cholinesterase Inhibitors/chemistry ; Acetylcholinesterase/chemistry ; Semicarbazones/pharmacology ; Hydrazones ; Molecular Docking Simulation ; Carbazoles/pharmacology ; Carbazoles/chemistry ; Chelating Agents/pharmacology ; Chelating Agents/chemistry ; Antioxidants/pharmacology ; Antioxidants/chemistry ; Alzheimer Disease/drug therapy ; Structure-Activity Relationship
    Chemical Substances Cholinesterase Inhibitors ; Acetylcholinesterase (EC 3.1.1.7) ; hydrazinecarbothioamide ; Semicarbazones ; Hydrazones ; Carbazoles ; Chelating Agents ; Antioxidants
    Language English
    Publishing date 2021-07-02
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 49157-3
    ISSN 1538-0254 ; 0739-1102
    ISSN (online) 1538-0254
    ISSN 0739-1102
    DOI 10.1080/07391102.2021.1942212
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Further Studies on Triazinoindoles as Potential Novel Multitarget-Directed Anti-Alzheimer's Agents.

    Patel, Dushyant V / Patel, Nirav R / Kanhed, Ashish M / Teli, Divya M / Patel, Kishan B / Gandhi, Pallav M / Patel, Sagar P / Chaudhary, Bharat N / Shah, Dharti B / Prajapati, Navnit K / Patel, Kirti V / Yadav, Mange Ram

    ACS chemical neuroscience

    2020  Volume 11, Issue 21, Page(s) 3557–3574

    Abstract: The inadequate clinical efficacy of the present anti-Alzheimer's disease (AD) drugs and their low impact on the progression of Alzheimer's disease in patients have revised the research focus from single targets to multitarget-directed ligands. A novel ... ...

    Abstract The inadequate clinical efficacy of the present anti-Alzheimer's disease (AD) drugs and their low impact on the progression of Alzheimer's disease in patients have revised the research focus from single targets to multitarget-directed ligands. A novel series of substituted triazinoindole derivatives were obtained by introducing various substituents on the indole ring for the development of multitarget-directed ligands as anti-AD agents. The experimental data indicated that some of these compounds exhibited significant anti-AD properties. Among them, 8-(piperidin-1-yl)-
    MeSH term(s) Acetylcholinesterase/metabolism ; Alzheimer Disease/drug therapy ; Amyloid beta-Peptides/metabolism ; Animals ; Blood-Brain Barrier/metabolism ; Cholinesterase Inhibitors/pharmacology ; Drug Design ; Humans ; Ligands ; Mice ; Pharmaceutical Preparations ; Rats ; Structure-Activity Relationship
    Chemical Substances Amyloid beta-Peptides ; Cholinesterase Inhibitors ; Ligands ; Pharmaceutical Preparations ; Acetylcholinesterase (EC 3.1.1.7)
    Language English
    Publishing date 2020-10-19
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ISSN 1948-7193
    ISSN (online) 1948-7193
    DOI 10.1021/acschemneuro.0c00448
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: Indoloquinoxaline derivatives as promising multi-functional anti-Alzheimer agents.

    Kanhed, Ashish M / Patel, Dushyant V / Patel, Nirav R / Sinha, Anshuman / Thakor, Priyanka S / Patel, Kishan B / Prajapati, Navnit K / Patel, Kirti V / Yadav, Mange Ram

    Journal of biomolecular structure & dynamics

    2020  Volume 40, Issue 6, Page(s) 2498–2515

    Abstract: To confront a disease like Alzheimer's disease having complex pathogenesis, development of multitarget-directed ligands has emerged as a promising drug discovery approach. In our endeavor towards the development of multitarget-directed ligands for ... ...

    Abstract To confront a disease like Alzheimer's disease having complex pathogenesis, development of multitarget-directed ligands has emerged as a promising drug discovery approach. In our endeavor towards the development of multitarget-directed ligands for Alzheimer's disease, a series of indoloquinoxaline derivatives were designed and synthesized. In vitro cholinesterase inhibition studies revealed that all the synthesized compounds exhibited moderate to good cholinesterase inhibitory activity. 6-(6-(Piperidin-1-yl)hexyl)-6
    MeSH term(s) Acetylcholinesterase/metabolism ; Alzheimer Disease/drug therapy ; Alzheimer Disease/metabolism ; Amyloid beta-Peptides ; Cholinesterase Inhibitors/chemistry ; Cholinesterases/metabolism ; Drug Design ; Humans ; Ligands ; Molecular Docking Simulation ; Structure-Activity Relationship
    Chemical Substances Amyloid beta-Peptides ; Cholinesterase Inhibitors ; Ligands ; Acetylcholinesterase (EC 3.1.1.7) ; Cholinesterases (EC 3.1.1.8)
    Language English
    Publishing date 2020-10-28
    Publishing country England
    Document type Journal Article
    ZDB-ID 49157-3
    ISSN 1538-0254 ; 0739-1102
    ISSN (online) 1538-0254
    ISSN 0739-1102
    DOI 10.1080/07391102.2020.1840441
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article ; Online: Novel carbazole-stilbene hybrids as multifunctional anti-Alzheimer agents.

    Patel, Dushyant V / Patel, Nirav R / Kanhed, Ashish M / Teli, Divya M / Patel, Kishan B / Joshi, Prashant D / Patel, Sagar P / Gandhi, Pallav M / Chaudhary, Bharat N / Prajapati, Navnit K / Patel, Kirti V / Yadav, Mange Ram

    Bioorganic chemistry

    2020  Volume 101, Page(s) 103977

    Abstract: Molecules capable of engaging with multiple targets associated with pathological condition of Alzheimer's disease have proved to be potential anti-Alzheimer's agents. In our goal to develop multitarget-directed ligands for the treatment of Alzheimer's ... ...

    Abstract Molecules capable of engaging with multiple targets associated with pathological condition of Alzheimer's disease have proved to be potential anti-Alzheimer's agents. In our goal to develop multitarget-directed ligands for the treatment of Alzheimer's disease, a novel series of carbazole-based stilbene derivatives were designed by the fusion of carbazole ring with stilbene scaffold. The designed compounds were synthesized and evaluated for their anti-AD activities including cholinesterase inhibition, Aβ aggregation inhibition, antioxidant and metal chelation properties. Amongst them, (E)-1-(4-(2-(9-ethyl-9H-carbazol-3-yl)vinyl)phenyl)-3-(2-(pyrrolidin-1-yl)ethyl)thiourea (50) appeared to be the best candidate with good inhibitory activities against AChE (IC
    MeSH term(s) Alzheimer Disease/drug therapy ; Humans ; Molecular Docking Simulation ; Molecular Structure ; Stilbenes/therapeutic use ; Structure-Activity Relationship
    Chemical Substances Stilbenes
    Language English
    Publishing date 2020-05-26
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 120080-x
    ISSN 1090-2120 ; 0045-2068
    ISSN (online) 1090-2120
    ISSN 0045-2068
    DOI 10.1016/j.bioorg.2020.103977
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article ; Online: Novel Multitarget Directed Triazinoindole Derivatives as Anti-Alzheimer Agents.

    Patel, Dushyant V / Patel, Nirav R / Kanhed, Ashish M / Patel, Sagar P / Sinha, Anshuman / Kansara, Deep D / Mecwan, Annie R / Patel, Sarvangee B / Upadhyay, Pragnesh N / Patel, Kishan B / Shah, Dharti B / Prajapati, Navnit K / Murumkar, Prashant R / Patel, Kirti V / Yadav, Mange Ram

    ACS chemical neuroscience

    2019  Volume 10, Issue 8, Page(s) 3635–3661

    Abstract: The multifaceted nature of Alzheimer's disease (AD) demands treatment with multitarget-directed ligands (MTDLs) to confront the key pathological aberrations. A novel series of triazinoindole derivatives were designed and synthesized. In vitro studies ... ...

    Abstract The multifaceted nature of Alzheimer's disease (AD) demands treatment with multitarget-directed ligands (MTDLs) to confront the key pathological aberrations. A novel series of triazinoindole derivatives were designed and synthesized. In vitro studies revealed that all the compounds showed moderate to good anticholinesterase activity; the most active compound
    MeSH term(s) Alzheimer Disease/drug therapy ; Alzheimer Disease/metabolism ; Animals ; Cell Line, Tumor ; Cholinesterase Inhibitors/pharmacology ; Cholinesterase Inhibitors/therapeutic use ; Humans ; Hydrogen Peroxide/pharmacology ; Male ; Maze Learning/drug effects ; Mice ; Molecular Docking Simulation ; Neurons/drug effects ; Neurons/metabolism ; Neuroprotective Agents/pharmacology ; Neuroprotective Agents/therapeutic use ; Oxidative Stress/drug effects ; Oxidative Stress/physiology ; Structure-Activity Relationship
    Chemical Substances Cholinesterase Inhibitors ; Neuroprotective Agents ; Hydrogen Peroxide (BBX060AN9V)
    Language English
    Publishing date 2019-07-29
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ISSN 1948-7193
    ISSN (online) 1948-7193
    DOI 10.1021/acschemneuro.9b00226
    Database MEDical Literature Analysis and Retrieval System OnLINE

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