Small molecule antagonists of the CCR2b receptor. Part 2: Discovery process and initial structure–activity relationships of diamine derivatives

Moree, Wilna J.; Kataoka, Ken-ichiro; Ramirez‐Weinhouse, Michele M.; Shiota, Tadashi; Imai, Minoru; Sudo, Masaki; Tsutsumi, Takaharu; Endo, Noriaki; Muroga, Yumiko; Hada, Takahiko; Tanaka, Hiroko; Morita, Takuya; Greene, Jonathan; Barnum, Doug; Saunders, John; Kato, Yoshinori; Myers, Peter L.; Tarby, Christine M.

doi:10.1016/j.bmcl.2004.08.009

Cited by 40 publications

(16 citation statements)

References 22 publications

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“…Nitrogen-containing heterocyclic compounds are pharmaceutically important [122,123]. Intensive attention was concentrated on the manufacture of this type of compounds over a half century.…”

Section: Cyclizationmentioning

confidence: 99%

Applications and Preparation Methods of Copper Chromite Catalysts: A Review

Прасад

2011

Bull. Chem. React. Eng. Catal.

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In this review article various applications and preparation methods of copper chromite catalysts have been discussed. While discussing it is concluded that copper chromite is a versatile catalyst which not only catalyses numerous processes of commercial importance and national program related to defence and space research but also finds applications in the most concerned problem worldwide i.e. environmental pollution control. Several other very useful applications of copper chromite catalysts are in production of clean energy, drugs and agro chemicals, etc. Various preparation methods about 15 have been discussed which depicts clear idea about the dependence of catalytic activity and selectivity on way of preparation of catalyst. In view of the globally increasing interest towards copper chromite catalysis, reexamination on the important applications of such catalysts and their useful preparation methods is thus the need of the time. This review paper encloses 369 references including a well-conceivable tabulation of the newer state of the art.

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“…Nitrogen-containing heterocyclic compounds are pharmaceutically important [122,123]. Intensive attention was concentrated on the manufacture of this type of compounds over a half century.…”

Section: Cyclizationmentioning

confidence: 99%

Applications and Preparation Methods of Copper Chromite Catalysts: A Review

Прасад

2011

Bull. Chem. React. Eng. Catal.

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“…700-7400 nM. To further improve the activity, alternative structural series were investigated using a virtual screening approach [51]. Screening data from the homopiperazine series, together with data obtained from about 200 GPCR ligands, were used to generate a computational model, composed of an ensemble of pharmacophore hypotheses, referred to as a method for lead evolution [52].…”

Section: Virtual Screening and Lead Evolution: Ccr2b Antagonistsmentioning

confidence: 99%

Role of Chemistry in Lead Discovery

Dolle

Worm

2010

Lead Generation Approaches in Drug Discovery

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“…Studies show that MCP-1 involves in the pathophysiology of the acute or chronic inflammatory conditions such as rheumatoid arthritis, atherosclerosis, asthma, obesity, and type-2 diabetes. Therefore, CCR2 receptor is an attractive target for the drug discovery [7][8][9] . CCR5 belongs to family of rhodopsin G-protein coupled receptor which is characterized by 7 transmembrane domains [10] .…”

Section: Introductionmentioning

confidence: 99%

In-silico Modeling of Chemokine Receptor CCR2 And CCR5 to Assist the Design of Effective and Selective Antagonists

Kothandan¹,

Cho²

2012

Journal of the Chosun Natural Science

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Chemokine receptor antagonists have potential applications in field of drug discovery. Although the chemokine receptors are G-protein-coupled receptors, their cognate ligands are small proteins (8 to 12 kDa), and so inhibiting the ligand/receptor interaction has been challenging. The application of structure-based in-silico methods to drug discovery is still considered a major challenge, especially when the x-ray structure of the target protein is unknown. Such is the case with human CCR2 and CCR5, the most important members of the chemokine receptor family and also a potential drug target. Herein, we review the success stories of combined receptor modeling/mutagenesis approach to probe the allosteric nature of chemokine receptor binding by small molecule antagonists for CCR2 and CCR5 using Rhodopsin as template. We also urged the importance of recently available β2-andrenergic receptor as an alternate template to guide mutagenesis. The results demonstrate the usefulness and robustness of in-silico 3D models. These models could also be useful for the design of novel and potent CCR2 and CCR5 antagonists using structure based drug design.

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Small molecule antagonists of the CCR2b receptor. Part 2: Discovery process and initial structure–activity relationships of diamine derivatives

Cited by 40 publications

References 22 publications

Applications and Preparation Methods of Copper Chromite Catalysts: A Review

Applications and Preparation Methods of Copper Chromite Catalysts: A Review

Role of Chemistry in Lead Discovery

In-silico Modeling of Chemokine Receptor CCR2 And CCR5 to Assist the Design of Effective and Selective Antagonists

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