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  1. Article: Discovery of

    Agarwal, Sameer / Sasane, Santosh / Shah, Hardik A / Pethani, Jignesh P / Deshmukh, Prashant / Vyas, Vismit / Iyer, Pravin / Bhavsar, Harsh / Viswanathan, Kasinath / Bandyopadhyay, Debdutta / Giri, Poonam / Mahapatra, Jogeswar / Chatterjee, Abhijit / Jain, Mukul R / Sharma, Rajiv

    ACS medicinal chemistry letters

    2020  Volume 11, Issue 4, Page(s) 414–418

    Abstract: NLRP3 inflammasome mediated release of interleukin-1β (IL-1β) has been implicated in various diseases. In this study, rationally designed mimics of sulfonylurea moiety were investigated as NLRP3 inhibitors. Our results culminated into discovery of series ...

    Abstract NLRP3 inflammasome mediated release of interleukin-1β (IL-1β) has been implicated in various diseases. In this study, rationally designed mimics of sulfonylurea moiety were investigated as NLRP3 inhibitors. Our results culminated into discovery of series of unprecedented
    Language English
    Publishing date 2020-02-27
    Publishing country United States
    Document type Journal Article
    ISSN 1948-5875
    ISSN 1948-5875
    DOI 10.1021/acsmedchemlett.9b00433
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Identification of a novel orally bioavailable NLRP3 inflammasome inhibitor.

    Agarwal, Sameer / Pethani, Jignesh P / Shah, Hardik A / Vyas, Vismit / Sasane, Santosh / Bhavsar, Harsh / Bandyopadhyay, Debdutta / Giri, Poonam / Viswanathan, Kasinath / Jain, Mukul R / Sharma, Rajiv

    Bioorganic & medicinal chemistry letters

    2020  Volume 30, Issue 21, Page(s) 127571

    Abstract: NLRP3 inflammasome mediated release of interleukin-1β (IL-1β) has been implicated in various diseases, including COVID-19. In this study, rationally designed alkenyl sulfonylurea derivatives were identified as novel, potent and orally bioavailable NLRP3 ... ...

    Abstract NLRP3 inflammasome mediated release of interleukin-1β (IL-1β) has been implicated in various diseases, including COVID-19. In this study, rationally designed alkenyl sulfonylurea derivatives were identified as novel, potent and orally bioavailable NLRP3 inhibitors. Compound 7 was found to be potent (IL-1β IC
    MeSH term(s) Administration, Oral ; Animals ; Betacoronavirus ; COVID-19 ; Cell Line, Tumor ; Coronavirus Infections ; Cytochrome P-450 CYP2C8 Inhibitors/administration & dosage ; Cytochrome P-450 CYP2C8 Inhibitors/chemical synthesis ; Cytochrome P-450 CYP2C8 Inhibitors/pharmacokinetics ; Cytochrome P-450 CYP2C8 Inhibitors/pharmacology ; Cytochrome P-450 CYP2C9 Inhibitors/administration & dosage ; Cytochrome P-450 CYP2C9 Inhibitors/chemical synthesis ; Cytochrome P-450 CYP2C9 Inhibitors/pharmacokinetics ; Cytochrome P-450 CYP2C9 Inhibitors/pharmacology ; Dogs ; Drug Stability ; Humans ; Inflammasomes/antagonists & inhibitors ; Interleukin-1beta/antagonists & inhibitors ; Mice, Inbred C57BL ; Microsomes, Liver/metabolism ; Molecular Structure ; NLR Family, Pyrin Domain-Containing 3 Protein/antagonists & inhibitors ; Pandemics ; Pneumonia, Viral ; Rats ; SARS-CoV-2 ; Structure-Activity Relationship ; Sulfonylurea Compounds/administration & dosage ; Sulfonylurea Compounds/chemical synthesis ; Sulfonylurea Compounds/pharmacokinetics ; Sulfonylurea Compounds/pharmacology
    Chemical Substances Cytochrome P-450 CYP2C8 Inhibitors ; Cytochrome P-450 CYP2C9 Inhibitors ; IL1B protein, human ; Inflammasomes ; Interleukin-1beta ; NLR Family, Pyrin Domain-Containing 3 Protein ; NLRP3 protein, human ; Nlrp3 protein, mouse ; Sulfonylurea Compounds
    Keywords covid19
    Language English
    Publishing date 2020-09-24
    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.2020.127571
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article: Identification of a novel orally bioavailable NLRP3 inflammasome inhibitor

    Agarwal, Sameer / Pethani, Jignesh P / Shah, Hardik A / Vyas, Vismit / Sasane, Santosh / Bhavsar, Harsh / Bandyopadhyay, Debdutta / Giri, Poonam / Viswanathan, Kasinath / Jain, Mukul R / Sharma, Rajiv

    Bioorg Med Chem Lett

    Abstract: NLRP3 inflammasome mediated release of interleukin-1ß (IL-1ß) has been implicated in various diseases, including COVID-19. In this study, rationally designed alkenyl sulfonylurea derivatives were identified as novel, potent and orally bioavailable NLRP3 ... ...

    Abstract NLRP3 inflammasome mediated release of interleukin-1ß (IL-1ß) has been implicated in various diseases, including COVID-19. In this study, rationally designed alkenyl sulfonylurea derivatives were identified as novel, potent and orally bioavailable NLRP3 inhibitors. Compound 7 was found to be potent (IL-1ß IC50 = 35 nM; IL-18 IC50 = 33 nM) and selective NLRP3 inflammasome inhibitor with excellent pharmacokinetic profile having oral bioavailability of 99% in mice.
    Keywords covid19
    Publisher WHO
    Document type Article
    Note WHO #Covidence: #791276
    Database COVID19

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