Discovery and in vitro and in vivo profiles of 4-fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide as novel class of an orally active metabotropic glutamate receptor 1 (mGluR1) antagonist.

doi:10.1016/j.bmcl.2009.07.097

Paper

DOI: 10.1016/j.bmcl.2009.07.097

Discovery and in vitro and in vivo profiles of 4-fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide as novel class of an orally active metabotropic glutamate receptor 1 (mGluR1) antagonist.

Published Sep 15, 2009 · A. Satoh, Yasushi Nagatomi, Y. Hirata

Bioorganic & medicinal chemistry letters

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In Vitro Study

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Study Snapshot

4-fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide 27] is a potent mGluR1 antagonist with potential for development as a PET trace

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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References

DOI: 10.1016/j.bmcl.2009.07.145

Discovery and biological profile of isoindolinone derivatives as novel metabotropic glutamate receptor 1 antagonists: a potential treatment for psychotic disorders.

Isoindolinone derivatives show potential as novel mGluR1 antagonists, with the most advanced analog showing an oral antipsychotic-like effect at a dose of 1 mg/kg in an animal model.

2009·46citations·S. Ito et al.·Bioorganic & medicinal chemistry letters

Bioorganic & medicinal chemistry letters

DOI: 10.1124/jpet.109.151118

Unique Antipsychotic Activities of the Selective Metabotropic Glutamate Receptor 1 Allosteric Antagonist 2-Cyclopropyl-5-[1-(2-fluoro-3-pyridinyl)-5-methyl-1H-1,2,3-triazol-4-yl]-2,3-dihydro-1H-isoindol-1-one

CFMTI is a potent and selective mGluR1 antagonist with unique antipsychotic activities, showing potential for treating schizophrenia and bipolar disorder.

2009·50citations·A. Satow et al.·Journal of Pharmacology and Experimental Therapeutics

Journal of Pharmacology and Experimental Therapeutics

DOI: 10.1016/j.bmcl.2009.02.106

In vitro and in vivo SAR of pyrido[3,4-d]pyramid-4-ylamine based mGluR1 antagonists.

Novel pyrido[3,4-d]pyramid-4-ylamine mGluR1 antagonists show promising analgesic effects and show potential for CNS penetration through their unique structure.

2009·17citations·S. Mantell et al.·Bioorganic & medicinal chemistry letters

Bioorganic & medicinal chemistry letters

DOI: 10.1016/j.bmc.2008.09.060

Discovery and biological profile of 4-(1-aryltriazol-4-yl)-tetrahydropyridines as an orally active new class of metabotropic glutamate receptor 1 antagonist.

4-(1-aryltriazol-4-yl)-tetrahydropyridines show potential as an oral mGluR1 antagonist with improved in vivo antagonistic activities.

2008·44citations·S. Ito et al.·Bioorganic & medicinal chemistry

Bioorganic & medicinal chemistry

DOI: 10.1124/jpet.108.138107

Pharmacological Effects of the Metabotropic Glutamate Receptor 1 Antagonist Compared with Those of the Metabotropic Glutamate Receptor 5 Antagonist and Metabotropic Glutamate Receptor 2/3 Agonist in Rodents: Detailed Investigations with a Selective Allosteric Metabotropic Glutamate Receptor 1 Antago

Blockade of mGluR1 in rodents showed antipsychotic-like effects without impairing motor functions, while blockade of mGluR5 and activation of mGluR2/3 did not show such activities.

2008·71citations·A. Satow et al.·Journal of Pharmacology and Experimental Therapeutics

Journal of Pharmacology and Experimental Therapeutics

Citations

DOI: 10.1002/slct.202401009

Deep Eutectic Solvent (DES)‐Mediated Green Approach for Synthesis of Benzothiazole Tethered Pyrazoles: Antimicrobial Properties and Molecular Docking Insights

This study presents a green, efficient method for synthesizing novel benzothiazole-tethered pyrazole derivatives with promising antimicrobial activity against pathogenic microorganisms.

2024·0citations·E. Hussein et al.·ChemistrySelect

ChemistrySelect

DOI: 10.33263/lianbs132.092

Synthesis of (Z)-2-((5-(2-chlorobenzylidene)-4-oxo-4,5-dihydrothiazol-2-yl)amino)butanoic Acid as Antimicrobial Agent

This study synthesized compounds with good to moderate antimicrobial activity against bacteria B. subtilis, S. aureus, and E. Coli, and some showed selective activity against C. albicans, A. flavus, and A. niger.

2024·0citations·Rahul B. Shinde et al.·Letters in Applied NanoBioScience

Letters in Applied NanoBioScience

DOI: 10.1021/acsomega.4c01552

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2024·0citations·E. Hussein et al.·ACS Omega

ACS Omega

DOI: 10.1002/slct.202302960

Development of New 5‐(Oxazol‐2‐yl)Pyrimidine Derivatives with Promising Anticancer Activities

New oxazolyl-pyrimidine derivatives show promising anticancer activities, with compounds 11 a and 11 b showing superior potency against cervical and lung cancer cell lines, and methoxy substituted derivatives showing excellent to good cytotoxic properties.

2023·1citation·Gajula Shyam Kumar et al.·ChemistrySelect

ChemistrySelect

DOI: 10.3390/biom13121694

Thiazole Derivatives as Modulators of GluA2 AMPA Receptors: Potent Allosteric Effects and Neuroprotective Potential

Thiazole derivatives, particularly MMH-5, show potential as safe neuroprotective agents targeting GluA2 AMPA receptors, potentially enhancing tailored treatments for neurological disorders.

2023·4citations·Mohammed Hawash·Biomolecules

Biomolecules

DOI: 10.1080/10406638.2023.2209257

Synthesis and Anti-Tubercular Screening of 8-Benzyloxy-5-[2-(Substituted-Phenyl)-Thiazol-4-yl]-1H-Quinolin-2-One Derivatives

Novel 8-Benzyloxy-5-[2-(substituted-phenyl)-thiazol-4-yl]-1H-quinolin-2-one derivatives show significant anti-tuberculosis activity against Mycobacterium tuberculosis H37Rv stains

2023·1citation·Vijay T. Kadam et al.·Polycyclic Aromatic Compounds

Polycyclic Aromatic Compounds

DOI: 10.1016/j.xcrm.2023.100960

A 211At-labelled mGluR1 inhibitor induces cancer senescence to elicit long-lasting anti-tumor efficacy

211 At-AITM, a targeted radiopharmaceutical, effectively eradicates mGluR1+ cancers, including breast, pancreatic, melanoma, and colon cancers, with minimal toxicity.

2023·9citations·Lin Xie et al.·Cell Reports Medicine

Cell Reports Medicine

DOI: 10.1080/07391102.2022.2064915

Targeting EGFR, RSK1, RAF1, PARP2 and LIN28B for several cancer type therapies with newly synthesized pyrazole derivatives via a computational study

Newly synthesized pyrazole derivatives M33, M36, M76, and M77 show promising potential as cancer therapeutic candidates due to their selective binding interactions and non-toxic characteristics.

2022·4citations·F. E. Bennani et al.·Journal of Biomolecular Structure and Dynamics

Journal of Biomolecular Structure and Dynamics