Christa C Chrovian
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Explore the profile of Christa C Chrovian including associated specialties, affiliations and a list of published articles.
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11
Citations
74
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Recent Articles
1.
Gelin C, Stenne B, Coate H, Hiscox A, Soyode-Johnson A, Wall J, et al.
J Med Chem
. 2023 Feb;
66(4):2877-2892.
PMID: 36757100
Herein, we describe a series of substituted 1-((1,2,3-triazol-4-yl)methoxy)pyrimidines as potent GluN2B negative allosteric modulators. Exploration of several five- and six-membered heterocycles led to the identification of O-linked pyrimidine analogues that...
2.
Chrovian C, Soyode-Johnson A, Stenne B, Pippel D, Schoellerman J, Lord B, et al.
J Med Chem
. 2020 Aug;
63(17):9181-9196.
PMID: 32787105
Selective inhibitors of the GluN2B subunit of -methyl-d-aspartate receptors in the ionotropic glutamate receptor superfamily have been targeted for the treatment of mood disorders. We sought to identify structurally novel,...
3.
Chrovian C, Soyode-Johnson A, Wall J, Rech J, Schoellerman J, Lord B, et al.
ACS Med Chem Lett
. 2019 Mar;
10(3):261-266.
PMID: 30891123
Herein, we disclose a series of selective GluN2B negative allosteric modulators containing a 1-pyrrolo[3,2-]pyridine core. Lead optimization efforts included increasing brain penetration as well as decreasing cytochrome P450 inhibition and...
4.
Chrovian C, Soyode-Johnson A, Peterson A, Gelin C, Deng X, Dvorak C, et al.
J Med Chem
. 2017 Dec;
61(1):207-223.
PMID: 29211470
A single pot dipolar cycloaddition reaction/Cope elimination sequence was developed to access novel 1,4,6,7-tetrahydro-5H-[1,2,3]triazolo[4,5-c]pyridine P2X7 antagonists that contain a synthetically challenging chiral center. The structure-activity relationships of the new compounds...
5.
Chrovian C, Soyode-Johnson A, Ao H, Bacani G, Carruthers N, Lord B, et al.
ACS Chem Neurosci
. 2016 Jan;
7(4):490-7.
PMID: 26752113
Novel 5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazine P2X7 antagonists were optimized to allow for good blood-brain barrier permeability and high P2X7 target engagement in the brain of rats. Compound 25 (huP2X7 IC50 = 9 nM;...
6.
Rudolph D, Alcazar J, Ameriks M, Anton A, Ao H, Bonaventure P, et al.
Bioorg Med Chem Lett
. 2015 Jun;
25(16):3157-63.
PMID: 26099534
The optimization efforts that led to a novel series of methyl substituted 1-(5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanones that are potent rat and human P2X7 antagonists are described. These efforts resulted in the discovery of...
7.
Chrovian C, Rech J, Bhattacharya A, Letavic M
Prog Med Chem
. 2014 Jan;
53:65-100.
PMID: 24418608
The use of P2X7 antagonists to treat inflammatory disorders has garnered considerable interest in recent years. An increasing number of literature reports support the role of P2X7 in inflammatory pathways...
8.
Eccles W, Blevitt J, Booker J, Chrovian C, Crawford S, de Leon A, et al.
Bioorg Med Chem Lett
. 2012 Dec;
23(3):811-5.
PMID: 23260350
Leukotrienes (LT's) are known to play a physiological role in inflammatory immune response. Leukotriene A(4) hydrolase (LTA(4)H) is a cystolic enzyme that stereospecifically catalyzes the transformation of LTA(4) to LTB(4)....
9.
Tanis V, Bacani G, Blevitt J, Chrovian C, Crawford S, De Leon A, et al.
Bioorg Med Chem Lett
. 2012 Nov;
22(24):7504-11.
PMID: 23127888
Previously, benzthiazole containing LTA(4)H inhibitors were discovered that were potent (1-3), but were associated with the potential for a hERG liability. Utilizing medicinal chemistry first principles (e.g., introducing rigidity, lowering...
10.
Chrovian C, Knapp-Reed B, Montgomery J
Org Lett
. 2008 Feb;
10(5):811-4.
PMID: 18254635
The total synthesis of aigialomycin D was carried out using a nickel-catalyzed ynal macrocyclization as a key step. This key step allowed macrocycle assembly and formation of a disubstituted alkene...