2-(1H-吡唑-4-基)乙酸作为 CRTh2 拮抗剂。
2-(1H-Pyrazol-4-yl)acetic acids as CRTh2 antagonists.
机构信息
Almirall R&D Centre, Laureano Miró, 408-410, 08980 Sant Feliu de Llobregat, Barcelona, Spain.
出版信息
Bioorg Med Chem Lett. 2013 Jun 1;23(11):3349-53. doi: 10.1016/j.bmcl.2013.03.093. Epub 2013 Apr 2.
PMID:23601708
Abstract
High throughput screening identified the pyrazole-4-acetic acid substructure as CRTh2 receptor antagonists. Optimisation of the compounds uncovered a tight SAR but also identified some low nanomolar inhibitors.
摘要
高通量筛选鉴定出吡唑-4-乙酸结构为 CRTh2 受体拮抗剂。化合物的优化揭示了严格的 SAR，但也鉴定出一些低纳摩尔抑制剂。
相似文献
1
2-(1H-Pyrazol-4-yl)acetic acids as CRTh2 antagonists.2-(1H-吡唑-4-基)乙酸作为 CRTh2 拮抗剂。
Bioorg Med Chem Lett. 2013 Jun 1;23(11):3349-53. doi: 10.1016/j.bmcl.2013.03.093. Epub 2013 Apr 2.
2
2-(1H-Pyrazol-1-yl)acetic acids as chemoattractant receptor-homologous molecule expressed on Th2 lymphocytes (CRTh2) antagonists.2-(1H-吡唑-1-基)乙酸作为 Th2 淋巴细胞表达的趋化因子受体同源物分子 (CRTh2) 拮抗剂。
Eur J Med Chem. 2014 Jan;71:168-84. doi: 10.1016/j.ejmech.2013.10.072. Epub 2013 Nov 9.
3
Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of pyrrolopiperidinone acetic acids as CRTh2 antagonists.作为CRTh2拮抗剂的吡咯并哌啶酮乙酸的构效关系（SAR）和构动关系（SKR）
Bioorg Med Chem Lett. 2014 Nov 1;24(21):5111-7. doi: 10.1016/j.bmcl.2014.08.026. Epub 2014 Aug 18.
4
Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of bicyclic heteroaromatic acetic acids as potent CRTh2 antagonists I.双环杂芳基乙酸作为强效CRTh2拮抗剂的构效关系（SAR）和构动关系（SKR）I
Bioorg Med Chem Lett. 2014 Nov 1;24(21):5118-22. doi: 10.1016/j.bmcl.2014.09.005. Epub 2014 Oct 15.
5
Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of bicyclic heteroaromatic acetic acids as potent CRTh2 antagonists II: lead optimization.双环杂芳基乙酸作为强效CRTh2拮抗剂的构效关系（SAR）和构动关系（SKR）II：先导化合物优化
Bioorg Med Chem Lett. 2014 Nov 1;24(21):5123-6. doi: 10.1016/j.bmcl.2014.08.029. Epub 2014 Aug 19.
6
Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of bicyclic heteroaromatic acetic acids as potent CRTh2 antagonists III: the role of a hydrogen-bond acceptor in long receptor residence times.双环杂芳基乙酸作为强效CRTh2拮抗剂的构效关系（SAR）和构动关系（SKR）III：氢键受体在长受体驻留时间中的作用
Bioorg Med Chem Lett. 2014 Nov 1;24(21):5127-33. doi: 10.1016/j.bmcl.2014.08.028. Epub 2014 Aug 19.
7
Novel 2-(2-(benzylthio)-1H-benzo[d]imidazol-1-yl)acetic acids: discovery and hit-to-lead evolution of a selective CRTh2 receptor antagonist chemotype.新型 2-(2-(苄硫基)-1H-苯并[d]咪唑-1-基)乙酸类化合物：选择性 CRTh2 受体拮抗剂类化合物的发现和从苗头化合物到先导化合物的优化。
Bioorg Med Chem Lett. 2012 Jul 15;22(14):4660-4. doi: 10.1016/j.bmcl.2012.05.087. Epub 2012 Jun 1.
8
7-Azaindole-3-acetic acid derivatives: potent and selective CRTh2 receptor antagonists.7-氮杂吲哚-3-乙酸衍生物：强效且选择性的CRTh2受体拮抗剂。
Bioorg Med Chem Lett. 2009 Aug 15;19(16):4794-8. doi: 10.1016/j.bmcl.2009.06.042. Epub 2009 Jun 14.
9
Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 1.新型选择性噻唑乙酸类化合物作为 CRTH2 拮抗剂的开发：基于计算机虚拟筛选的命中化合物。第 1 部分。
Bioorg Med Chem Lett. 2010 Feb 1;20(3):1177-80. doi: 10.1016/j.bmcl.2009.12.008. Epub 2009 Dec 4.
10
Evolution of novel tricyclic CRTh2 receptor antagonists from a (E)-2-cyano-3-(1H-indol-3-yl)acrylamide scaffold.从（E）-2-氰基-3-（1H-吲哚-3-基）丙烯酰胺支架上开发新型三环 CRTh2 受体拮抗剂的进展。
Bioorg Med Chem Lett. 2013 Feb 15;23(4):944-8. doi: 10.1016/j.bmcl.2012.12.050. Epub 2012 Dec 25.
引用本文的文献
1
Indole-Based and Cyclopentenylindole-Based Analogues Containing Fluorine Group as Potential F-Labeled Positron Emission Tomography (PET) G-Protein Coupled Receptor 44 (GPR44) Tracers.含氟基团的基于吲哚和环戊烯基吲哚的类似物作为潜在的F标记正电子发射断层扫描（PET）G蛋白偶联受体44（GPR44）示踪剂
Pharmaceuticals (Basel). 2023 Aug 24;16(9):1203. doi: 10.3390/ph16091203.
2
CsCO catalyzed direct aza-Michael addition of azoles to α,β-unsaturated malonates.碳酸铯催化唑类与α,β-不饱和丙二酸酯的直接氮杂-Michael加成反应。
RSC Adv. 2022 Jul 1;12(30):19265-19269. doi: 10.1039/d2ra02314h. eCollection 2022 Jun 29.
Zotero 插件