isoindoles

Summary

Summary: Benzopyrroles with the nitrogen at the number two carbon, in contrast to INDOLES which have the nitrogen adjacent to the six-membered ring.

Top Publications

  1. Yoon H, Hong J. Sulfatase activity assay using an activity-based probe by generation of N-methyl isoindole under reducing conditions. Anal Biochem. 2017;526:33-38 pubmed publisher
  2. Frlan R, Gobec S. Evaluation of US 2016/0115161 A1: isoindoline compounds and methods of their use. Expert Opin Ther Pat. 2017;27:637-641 pubmed publisher
    ..Results of biological tests, which are superior over those of presently used IMIDs lenalidomide and pomalidomide, make these compounds viable leads for future development of new anticancer drugs against blood and solid cancers. ..
  3. Azimi S, Zonouzi A, Firuzi O, Iraji A, Saeedi M, Mahdavi M, et al. Discovery of imidazopyridines containing isoindoline-1,3-dione framework as a new class of BACE1 inhibitors: Design, synthesis and SAR analysis. Eur J Med Chem. 2017;138:729-737 pubmed publisher
    ..These findings demonstrate that imidazopyridines-based compounds bearing phthalimide moiety have the potential to decrease amyloid-? levels and ameliorate the symptoms of Alzheimer's disease. ..
  4. Kimuro Y, Usui K, Karasawa S, Hirai G, Aso M. 7-Hydroxy-3-methyleneisoindolin-1-one as a New ESIPT-Fluorescent Probe to Monitor Aqueous Environments. Chem Pharm Bull (Tokyo). 2017;65:796-800 pubmed publisher
  5. Loebel A, Cucchiaro J, Silva R, Kroger H, Sarma K, Xu J, et al. Lurasidone as adjunctive therapy with lithium or valproate for the treatment of bipolar I depression: a randomized, double-blind, placebo-controlled study. Am J Psychiatry. 2014;171:169-77 pubmed publisher
    ..CONCLUSIONS In patients with bipolar I depression, treatment with lurasidone adjunctive to lithium or valproate significantly improved depressive symptoms and was generally well tolerated. ..
  6. Maehara S. [Pharmacological characterization of metabotropic glutamate-receptor 1 antagonist for the treatment of schizophrenia]. Nihon Yakurigaku Zasshi. 2013;142:280-4 pubmed
  7. Chiu Y, Ereshefsky L, Preskorn S, Poola N, Loebel A. Lurasidone drug-drug interaction studies: a comprehensive review. Drug Metabol Drug Interact. 2014;29:191-202 pubmed publisher
    ..Dose adjustment is not required for lithium, valproate, digoxin (a P-glycoprotein substrate), or midazolam or oral contraceptives (CYP3A4 substrates) when coadministered with lurasidone. ..
  8. Baker J, Gardiner S, Woolard J, Fromont C, Jadhav G, Mistry S, et al. Novel selective ?1-adrenoceptor antagonists for concomitant cardiovascular and respiratory disease. FASEB J. 2017;31:3150-3166 pubmed publisher
    ..M., Woolard, J., Fromont, C., Jadhav, G. P., Mistry, S. N., Thompson, K. S. J., Kellam, B., Hill, S. J., Fischer, P. M. Novel selective ?1-adrenoceptor antagonists for concomitant cardiovascular and respiratory disease. ..
  9. Davoren J, Garnsey M, Pettersen B, Brodney M, Edgerton J, Fortin J, et al. Design and Synthesis of ?- and ?-Lactam M1 Positive Allosteric Modulators (PAMs): Convulsion and Cholinergic Toxicity of an M1-Selective PAM with Weak Agonist Activity. J Med Chem. 2017;60:6649-6663 pubmed publisher
    ..These findings provide preliminary evidence that positive allosteric modulation of M1 is sufficient to elicit cholinergic AEs. ..

More Information

Publications13

  1. Curtin M, Heyman H, Clark R, Sorensen B, Doherty G, Hansen T, et al. SAR and characterization of non-substrate isoindoline urea inhibitors of nicotinamide phosphoribosyltransferase (NAMPT). Bioorg Med Chem Lett. 2017;27:3317-3325 pubmed publisher
    ..X-ray crystal structures of two inhibitors bound in the NAMPT active-site are discussed. ..
  2. Manchekar M, Kapil R, Sun Z, Segrest J, Dashti N. Relationship between Amphipathic ? Structures in the ?1 Domain of Apolipoprotein B and the Properties of the Secreted Lipoprotein Particles in McA-RH7777 Cells. Biochemistry. 2017;56:4084-4094 pubmed publisher
  3. Li H, Kim H, Shin S, Seo M, An J, Ha K, et al. The vasorelaxant effect of mitiglinide via activation of voltage-dependent K+ channels and SERCA pump in aortic smooth muscle. Life Sci. 2017;188:1-9 pubmed publisher
    ..However, the vasorelaxant effects of mitiglinide did not involve other K+ channels, Ca2+ channels, PKA/PKG signaling pathways, or the endothelium. ..
  4. Loebel A, Cucchiaro J, Silva R, Kroger H, Hsu J, Sarma K, et al. Lurasidone monotherapy in the treatment of bipolar I depression: a randomized, double-blind, placebo-controlled study. Am J Psychiatry. 2014;171:160-8 pubmed publisher
    ..Monotherapy with lurasidone in the dosage range of 20-120 mg/day significantly reduced depressive symptoms in patients with bipolar I depression. Lurasidone was well tolerated, with few changes in weight or metabolic parameters. ..