Jia, Hong; Dai, Guangxiu; Su, Weiguo; Xiao, Kun; Weng, Jianyang; Zhang, Zhulin; Wang, Qing; Yuan, Tianhai; Shi, Fuying; Zhang, Zheng; Chen, Wei; Sai, Yang; Wang, Jian; Li, Xiong; Cai, Yu; Yu, Jun; Ren, Ping; Venable, Jennifer; Rao, Tadimeti; Edwards, James P.; Bembenek, Scott D. published the article 《Discovery, Optimization, and Evaluation of Potent and Highly Selective PI3Kγ-PI3Kδ Dual Inhibitors》. Keywords: pyrrolotriazinone synthesis SAR pharmacokinetics PI3K rheumatoid arthritis autoimmune disorders.They researched the compound: 1-Aminopyrrole-2-carboxamide( cas:159326-69-9 ).Product Details of 159326-69-9. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:159326-69-9) here.
An electronic d. model was developed and used to identify a novel pyrrolotriazinone replacement for a quinazolinone, a commonly used moiety to impart selectivity in inhibitors for PI3Kγ and PI3Kδ. Guided by mol. docking, this new specificity piece was then linked to the hinge-binding region of the inhibitor using a novel cyclic moiety. Further structure-activity relationship optimization around the hinge region led to the discovery of candidate 26, a highly potent and selective PI3Kγ-PI3Kδ dual inhibitor with favorable drug metabolism and pharmacokinetic properties in preclin. species.
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Reference:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica