Design, synthesis, and pharmacological evaluation of benzimidazolo-thiazoles as potent CXCR3 antagonists with therapeutic potential in autoimmune diseases …

E Caroff, EA Meyer, P Äänismaa… - Journal of Medicinal …, 2022 - ACS Publications
… we explored the benzimidazolo-thiazole core scaffold. The … ring was replaced by smaller
heterocycles. Herein, we describe … We started our optimization program with the replacement of …

Designing small molecule CXCR3 antagonists

JE Pease - Expert Opinion on Drug Discovery, 2017 - Taylor & Francis
Optimization of the quinazolinone series from which AMG 487 emerged identified a lead …
Similarly, substitution at the C4-position of the azaquinazolinone core also yielded derivatives …

Research progress of CXCR3 inhibitors

Z Yuan - Anti-Cancer Drugs, 2024 - journals.lww.com
… of the optimized derivative compounds have produced CXCR3 … of two high affinity CXCR3
antagonists were shown, which … nitrogen atoms in the heterocyclic scaffold of the compound …

Visible Light Assisted Direct C3–H Arylation of Pyrido[1,2-a]pyrimidin-4-ones and Thiazolo[3,2-a]pyrimidin-5-ones

RT Bhawale, UA Kshirsagar - The Journal of Organic Chemistry, 2023 - ACS Publications
… of biologically important heterocyclic compounds, herein we … With the optimization of
reaction conditions, further study of … the above-mentioned optimized reaction conditions in good …

Discovery, optimization, and in vivo evaluation of benzimidazole derivatives AM-8508 and AM-9635 as potent and selective PI3Kδ inhibitors

Y Shin, J Suchomel, M Cardozo… - Journal of Medicinal …, 2016 - ACS Publications
… of inhibitors of the CXCR3 receptor, we showed that five–six fused heterocyclic systems, such
… –six fused heterocycles. (23) It was therefore hypothesized that these heterocyclic moieties …

Chemistry of Quinazolin-4 (3H)-ones and their Antiinflammatory activity: A Review.

P SINGH, P RATHI, S SINGHAL… - International Journal of …, 2022 - search.ebscohost.com
… Nitrogen containing compounds are very important heterocyclic derivatives in the field of …
J et al, Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3, …

Dihydropyrazinoquinazolinones via SN2 Sulfamidate Ring-Opening and a Sequential Quinazolinone–Amidine Rearrangement Strategy (SQuAReS)

JN Fitz-Henley, SD Rozema… - The Journal of organic …, 2022 - ACS Publications
… Using the these starting materials and our optimized conditions (entry 8, Table 1), the scope
of the protocol was assessed. Twenty dihydropyrazinoquinazolinones were prepared with …

Catalytic Photoredox C–H Arylation of 4-Oxo-4H-pyrido[1,2-a]pyrimidine-3-diazonium Tetrafluoroborates and Related Heteroaryl Diazonium Salts

K Antolinc, H Brodnik, U Grošelj… - The Journal of …, 2023 - ACS Publications
… Fused heterocycles with bridgehead nitrogen atoms are important scaffolds commonly used
… for the subsequent optimization study. The results of the optimization study are shown in …

2, 4, 6-Triaminopyrimidine as a novel hinge binder in a series of PI3Kδ selective inhibitors

L Patel, J Chandrasekhar, J Evarts… - Journal of Medicinal …, 2016 - ACS Publications
… Herein, we describe the discovery and optimization of a series of propeller shaped PI3Kδ
inhibitors comprising a novel triaminopyrimidine hinge binder. Combinations of electronic and …

[HTML][HTML] A facile one-pot synthesis of aryl-substituted fused pyrimidinones

HJ Lee, YH Song - Heterocyclic Communications, 2016 - degruyter.com
CXCR3 antagonists [5–7]. The conventional methods previously reported for the synthesis
(Gould-Jacob type reaction) [8–10] and the functionalization (Suzuki-Miyaura reaction) [11] of …