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Literature DB >> 19631529

Imidazo-pyrazine derivatives as potent CXCR3 antagonists.

Xiaohui Du¹, Darin J Gustin, Xiaoqi Chen, Jason Duquette, Lawrence R McGee, Zhulun Wang, Karen Ebsworth, Kirk Henne, Bryan Lemon, Ji Ma, Shichang Miao, Emmanuel Sabalan, Timothy J Sullivan, George Tonn, Tassie L Collins, Julio C Medina.

Abstract

A general way of improving the potency of CXCR3 antagonists with fused hetero-bicyclic cores was identified. Optimization efforts led to the discovery of a series of imidazo-pyrazine derivatives with improved pharmacokinetic properties in addition to increased potency. The efficacy of the lead compound 21 is evaluated in a mouse lung inflammation model.

Entities: Chemical Disease Gene Species

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Year: 2009 PMID： 19631529 DOI： 10.1016/j.bmcl.2009.07.021

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

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Cited

13 in total

Review 1. A concise review on hPXR ligand-recognizing residues and structure-based strategies to alleviate hPXR transactivation risk.

Authors: Tao Liu; James P Beck; Junliang Hao
Journal: RSC Med Chem Date: 2022-01-19

2. N'-[1-(4-Amino-phen-yl)ethyl]pyrazine-2-carbohydrazide.

Authors: Zhi-Yong Xing; De-Cheng Yu; Lai-Jun Li; Hai-Yan Liu; Jian-Fei Zhang
Journal: Acta Crystallogr Sect E Struct Rep Online Date: 2010-02-06

3. N-tert-Butyl-2-(2,6-di-chloro-phen-yl)imidazo[1,2-a]pyrazin-3-amine.

Authors: Zeenat Fatima; Thothadri Srinivasan; Suman Koorathota; Sathiah Thennarasu; Devadasan Velmurugan
Journal: Acta Crystallogr Sect E Struct Rep Online Date: 2013-05-25

4. A selective and potent CXCR3 antagonist SCH 546738 attenuates the development of autoimmune diseases and delays graft rejection.

Authors: Chung-Her Jenh; Mary Ann Cox; Long Cui; Eva-Pia Reich; Lee Sullivan; Shu-Cheng Chen; David Kinsley; Shiguang Qian; Seong Heon Kim; Stuart Rosenblum; Joseph Kozlowski; Jay S Fine; Paul J Zavodny; Daniel Lundell
Journal: BMC Immunol Date: 2012-01-10 Impact factor: 3.615

Imidazo-pyrazine derivatives as potent CXCR3 antagonists.

Review 1. A concise review on hPXR ligand-recognizing residues and structure-based strategies to alleviate hPXR transactivation risk.

2. N'-[1-(4-Amino-phen-yl)ethyl]pyrazine-2-carbohydrazide.

3. N-tert-Butyl-2-(2,6-di-chloro-phen-yl)imidazo[1,2-a]pyrazin-3-amine.

4. A selective and potent CXCR3 antagonist SCH 546738 attenuates the development of autoimmune diseases and delays graft rejection.

5. Defining the chemokine basis for leukocyte recruitment during viral encephalitis.

6. Methyl 3,5-bis-[(3-chloro-pyrazin-2-yl)-oxy]benzoate.

7. 1,3-Bis[(3-chloro-pyrazin-2-yl)-oxy]benzene.

8. 1,4-Bis(3-chloro-pyrazin-2-yl-oxy)benzene.

9. 8,15-Dioxa-10,13-di-aza-tetra-cyclo-[14.4.0.0(2,7).0(9,14)]icosa-1(16),2,4,6,9(14),10,12,17,19-nona-ene.

10. N-tert-Butyl-2-[4-(dimethyl-amino)-phen-yl]imidazo[1,2-a]pyrazin-3-amine.