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Literature DB >> 16483774

Identification of potent phenyl imidazoles as opioid receptor agonists.

Henry J Breslin¹, Chaozhong Cai, Tamara A Miskowski, Santosh V Coutinho, Sui-Po Zhang, Pamela Hornby, Wei He.

Abstract

Using previously reported opioid receptor (OR) agonist analogs 4a-c as starting points, the structure-activity relationship (SAR) for their related series has been further refined. This SAR study has led to the identification of 2,6-di-Me-Tyr (DMT) analogs 4h and 4j as the most potent OR agonist within the series. In addition, it was discovered that 4-(aminocarbonyl)-2,6-dimethyl-Phe is a reasonable bioisostere surrogate for the DMT moiety, as supported by the OR activities of compounds 4x and 4y.

Entities: Chemical Gene

Mesh：

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Year: 2006 PMID： 16483774 DOI： 10.1016/j.bmcl.2006.01.082

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

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Cited

6 in total

5. Design of a new multi-functional catalytic system Ni/SO₃H@zeolite-Y for three-component synthesis of N-benzo-imidazo- or -thiazole-1,3-thiazolidinones.

Authors: Mehdi Kalhor; Soodabeh Banibairami
Journal: RSC Adv Date: 2020-11-12 Impact factor: 4.036

6. Sonochemical synthesis of 1,2,4,5-tetrasubstituted imidazoles using nanocrystalline MgAl2O4 as an effective catalyst.

Authors: Javad Safari; Soheila Gandomi-Ravandi; Zahra Akbari
Journal: J Adv Res Date: 2012-12-21 Impact factor: 10.479

6 in total

Identification of potent phenyl imidazoles as opioid receptor agonists.

Review 1. Endogenous opiates and behavior: 2006.

2. Modulation of gastrointestinal function by MuDelta, a mixed µ opioid receptor agonist/ µ opioid receptor antagonist.

3. Insights into subtype selectivity of opioid agonists by ligand-based and structure-based methods.

4. Rapid Synthesis of Boc-2',6'-dimethyl-l-tyrosine and Derivatives and Incorporation into Opioid Peptidomimetics.

5. Design of a new multi-functional catalytic system Ni/SO₃H@zeolite-Y for three-component synthesis of N-benzo-imidazo- or -thiazole-1,3-thiazolidinones.

6. Sonochemical synthesis of 1,2,4,5-tetrasubstituted imidazoles using nanocrystalline MgAl2O4 as an effective catalyst.

Identification of potent phenyl imidazoles as opioid receptor agonists.

Review 1. Endogenous opiates and behavior: 2006.

2. Modulation of gastrointestinal function by MuDelta, a mixed µ opioid receptor agonist/ µ opioid receptor antagonist.

3. Insights into subtype selectivity of opioid agonists by ligand-based and structure-based methods.

4. Rapid Synthesis of Boc-2',6'-dimethyl-l-tyrosine and Derivatives and Incorporation into Opioid Peptidomimetics.

5. Design of a new multi-functional catalytic system Ni/SO3H@zeolite-Y for three-component synthesis of N-benzo-imidazo- or -thiazole-1,3-thiazolidinones.

6. Sonochemical synthesis of 1,2,4,5-tetrasubstituted imidazoles using nanocrystalline MgAl2O4 as an effective catalyst.

5. Design of a new multi-functional catalytic system Ni/SO₃H@zeolite-Y for three-component synthesis of N-benzo-imidazo- or -thiazole-1,3-thiazolidinones.