ArticleBioorganic & medicinal chemistry2013
Cyclopropyl- and methyl-containing inhibitors of neuronal nitric oxide synthase.
Article in Bioorganic & medicinal chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
4 citing papers in PubMed, 13 citations in OpenAlex.
- Cyclopropyl-containing positive allosteric modulators of metabotropic glutamate receptor subtype 5.Bioorganic & medicinal chemistry letters · 2015Article
- Novel 2,4-disubstituted pyrimidines as potent, selective, and cell-permeable inhibitors of neuronal nitric oxide synthase.Journal of medicinal chemistry · 2015Article
- Development of nitric oxide synthase inhibitors for neurodegeneration and neuropathic pain.Chemical Society reviews · 2014Review
- Simplified 2-aminoquinoline-based scaffold for potent and selective neuronal nitric oxide synthase inhibition.Journal of medicinal chemistry · 2014Article
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Authors and funding
11 authors at 3 institutions in 2 countries.
Funding
Abstract
Inhibitors of neuronal nitric oxide synthase have been proposed as therapeutics for the treatment of different types of neurological disorders. On the basis of a cis-3,4-pyrrolidine scaffold, a series of trans-cyclopropyl- and methyl-containing nNOS inhibitors have been synthesized. The insertion of a rigid electron-withdrawing cyclopropyl ring decreases the basicity of the adjacent amino group, which resulted in decreased inhibitory activity of these inhibitors compared to the parent compound. Nonetheless, three of them exhibited double-digit nanomolar inhibition with high nNOS selectivity on the basis of in vitro enzyme assays. Crystal structures of nNOS and eNOS with these inhibitors bound provide a basis for detailed structure-activity relationship (SAR) studies. The conclusions from these studies will be used as a guide in the future development of selective NOS inhibitors.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.