Synthesis, structure-activity relationship studies and evaluation of a TLR 3/8/9 agonist and its analogues | Zendy

A. Sarkar | Zendy; Anushka C. Galasiti Kankanamalage | Zendy; Qian Zhang | Zendy; Heng Cheng | Zendy; Prasanna Sivaprakasam | Zendy; Joseph G. Naglich | Zendy; Chunshan Xie | Zendy; Sanjeev Gangwar | Zendy; Dale L. Boger | Zendy

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Synthesis, structure-activity relationship studies and evaluation of a TLR 3/8/9 agonist and its analogues

Author(s) -

A. Sarkar,

Anushka C. Galasiti Kankanamalage,

Qian Zhang,

Heng Cheng,

Prasanna Sivaprakasam,

Joseph G. Naglich,

Chunshan Xie,

Sanjeev Gangwar,

Dale L. Boger

Publication year - 2021

Publication title -

medicinal chemistry research

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.352

H-Index - 45

eISSN - 1554-8120

pISSN - 1054-2523

DOI - 10.1007/s00044-021-02736-3

Subject(s) - agonist , chemistry , intrinsic activity , potency , pharmacology , partial agonist , ec50 , structure–activity relationship , stereochemistry , receptor , in vitro , biochemistry , medicine

A comprehensive SAR study of a putative TLR 3/8/9 agonist was conducted. Despite the excitement surrounding the potential of the first small molecule TLR3 agonist with a compound that additionally displayed agonist activity for TLR8 and TLR9, compound 1 displayed disappointing activity in our hands, failing to match the potency (EC 50 ) reported and displaying only a low efficacy for the extent of stimulated NF-κB activation and release. The evaluation of >75 analogs of 1 , many of which constitute minor modifications in the structure, failed to identify any that displayed significant activity and none that exceeded the modest activity found for 1 .

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