Article ; Online: Design, Synthesis, and Pharmacological Evaluation of Spiro[carbazole-3,3'-pyrrolidine] Derivatives as cGAS Inhibitors for Treatment of Acute Lung Injury.
Journal of medicinal chemistry
2024 Volume 67, Issue 8, Page(s) 6268–6291
Abstract: Overactivation of cyclic GMP-AMP synthase (cGAS) is implicated in the occurrence of many inflammatory and autoimmune diseases, and inhibition of cGAS with a specific inhibitor has been proposed as a potential therapeutic strategy. However, only a few low- ...
Abstract | Overactivation of cyclic GMP-AMP synthase (cGAS) is implicated in the occurrence of many inflammatory and autoimmune diseases, and inhibition of cGAS with a specific inhibitor has been proposed as a potential therapeutic strategy. However, only a few low-potency cGAS inhibitors have been reported, and few are suitable for clinical investigation. As a continuation of our structural optimization on the reported cGAS inhibitor |
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MeSH term(s) | Acute Lung Injury/drug therapy ; Animals ; Mice ; Drug Design ; Male ; Humans ; Rats ; Carbazoles/chemical synthesis ; Carbazoles/pharmacology ; Carbazoles/chemistry ; Carbazoles/therapeutic use ; Carbazoles/pharmacokinetics ; Pyrrolidines/pharmacology ; Pyrrolidines/chemical synthesis ; Pyrrolidines/chemistry ; Pyrrolidines/therapeutic use ; Pyrrolidines/pharmacokinetics ; Nucleotidyltransferases/antagonists & inhibitors ; Nucleotidyltransferases/metabolism ; Lipopolysaccharides ; Rats, Sprague-Dawley ; Spiro Compounds/chemical synthesis ; Spiro Compounds/pharmacology ; Spiro Compounds/chemistry ; Spiro Compounds/therapeutic use ; Spiro Compounds/pharmacokinetics ; Enzyme Inhibitors/chemical synthesis ; Enzyme Inhibitors/pharmacology ; Enzyme Inhibitors/therapeutic use ; Enzyme Inhibitors/pharmacokinetics ; Enzyme Inhibitors/chemistry ; Structure-Activity Relationship ; Molecular Docking Simulation |
Chemical Substances | Carbazoles ; Pyrrolidines ; Nucleotidyltransferases (EC 2.7.7.-) ; Lipopolysaccharides ; Spiro Compounds ; Enzyme Inhibitors ; cGAS protein, human (EC 2.7.7.-) |
Language | English |
Publishing date | 2024-04-15 |
Publishing country | United States |
Document type | Journal Article ; Research Support, Non-U.S. Gov't |
ZDB-ID | 218133-2 |
ISSN | 1520-4804 ; 0022-2623 |
ISSN (online) | 1520-4804 |
ISSN | 0022-2623 |
DOI | 10.1021/acs.jmedchem.3c02229 |
Database | MEDical Literature Analysis and Retrieval System OnLINE |
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