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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.
  • Agarwal S; Zydus Research Centre, Cadila Healthcare Ltd., Sarkhej-Bavla N.H. No. 8 A, Moraiya, Ahmedabad 382 210, India. Electronic address: sameeragarwal@zyduscadila.com.
  • Pethani JP; Zydus Research Centre, Cadila Healthcare Ltd., Sarkhej-Bavla N.H. No. 8 A, Moraiya, Ahmedabad 382 210, India.
  • Shah HA; Zydus Research Centre, Cadila Healthcare Ltd., Sarkhej-Bavla N.H. No. 8 A, Moraiya, Ahmedabad 382 210, India.
  • Vyas V; Zydus Research Centre, Cadila Healthcare Ltd., Sarkhej-Bavla N.H. No. 8 A, Moraiya, Ahmedabad 382 210, India.
  • Sasane S; Zydus Research Centre, Cadila Healthcare Ltd., Sarkhej-Bavla N.H. No. 8 A, Moraiya, Ahmedabad 382 210, India.
  • Bhavsar H; Zydus Research Centre, Cadila Healthcare Ltd., Sarkhej-Bavla N.H. No. 8 A, Moraiya, Ahmedabad 382 210, India.
  • Bandyopadhyay D; Zydus Research Centre, Cadila Healthcare Ltd., Sarkhej-Bavla N.H. No. 8 A, Moraiya, Ahmedabad 382 210, India.
  • Giri P; Zydus Research Centre, Cadila Healthcare Ltd., Sarkhej-Bavla N.H. No. 8 A, Moraiya, Ahmedabad 382 210, India.
  • Viswanathan K; Zydus Research Centre, Cadila Healthcare Ltd., Sarkhej-Bavla N.H. No. 8 A, Moraiya, Ahmedabad 382 210, India.
  • Jain MR; Zydus Research Centre, Cadila Healthcare Ltd., Sarkhej-Bavla N.H. No. 8 A, Moraiya, Ahmedabad 382 210, India.
  • Sharma R; Zydus Research Centre, Cadila Healthcare Ltd., Sarkhej-Bavla N.H. No. 8 A, Moraiya, Ahmedabad 382 210, India. Electronic address: Rajiv.Sharma@zyduscadila.com.
Bioorg Med Chem Lett ; 30(21): 127571, 2020 11 01.
Article in English | MEDLINE | ID: covidwho-791276
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.
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Full text: Available Collection: International databases Database: MEDLINE Main subject: Sulfonylurea Compounds / Inflammasomes / NLR Family, Pyrin Domain-Containing 3 Protein Limits: Animals / Humans Language: English Journal: Bioorg Med Chem Lett Journal subject: Biochemistry / Chemistry Year: 2020 Document Type: Article

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Full text: Available Collection: International databases Database: MEDLINE Main subject: Sulfonylurea Compounds / Inflammasomes / NLR Family, Pyrin Domain-Containing 3 Protein Limits: Animals / Humans Language: English Journal: Bioorg Med Chem Lett Journal subject: Biochemistry / Chemistry Year: 2020 Document Type: Article