Michael Czarniecki
Overview
Explore the profile of Michael Czarniecki including associated specialties, affiliations and a list of published articles.
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Articles
18
Citations
145
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0
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Recent Articles
1.
Lucke A, Liesegang A, Kummerlen D, Czarniecki M, Wichert B
Heliyon
. 2024 Jul;
10(12):e33300.
PMID: 39022019
In-vitro studies are widely used in nutrition research. Two major challenges using in-vitro models in animal nutrition research are the individual adaptation of in-vitro digestion models to varying physiological conditions...
2.
McKittrick B, Caldwell J, Bara T, Boykow G, Chintala M, Clader J, et al.
Bioorg Med Chem Lett
. 2015 Mar;
25(7):1592-6.
PMID: 25728416
The development of renin inhibitors with favorable oral pharmacokinetic profiles has been a longstanding challenge for the pharmaceutical industry. As part of our work to identify inhibitors of BACE1, we...
3.
Huang X, Zhou W, Liu X, Li H, Sun G, Mandal M, et al.
ACS Med Chem Lett
. 2014 Jun;
3(11):931-5.
PMID: 24900409
Fused oxadiazines (3) were discovered as selective and orally bioavailable γ-secretase modulators (GSMs) based on the structural framework of oxadiazoline GSMs. Although structurally related, initial modifications showed that structure-activity relationships...
4.
Li H, Qin J, Dhondi P, Zhou W, Vicarel M, Bara T, et al.
Bioorg Med Chem Lett
. 2012 Dec;
23(2):466-71.
PMID: 23253441
In an attempt to further improve overall profiles of the oxadiazine series of GSMs, in particular the hERG activity, conformational modifications of the core structure resulted in the identification of...
5.
Sun Z, Asberom T, Bara T, Bennett C, Burnett D, Chu I, et al.
J Med Chem
. 2011 Nov;
55(1):489-502.
PMID: 22098494
Cyclic hydroxyamidines were designed and validated as isosteric replacements of the amide functionality. Compounds with these structural motifs were found to be metabolically stable and to possess highly desirable pharmacokinetic...
6.
Brumfield S, Matasi J, Tulshian D, Czarniecki M, Greenlee W, Garlisi C, et al.
Bioorg Med Chem Lett
. 2011 Nov;
21(24):7287-90.
PMID: 22078214
Novel P2X(7) antagonists were developed using a purine scaffold. These compounds were potent and selective at the P2X(7) receptor in human and rodent as well as efficacious in rodent pain...
7.
Smith E, Sorota S, Kim H, McKittrick B, Nechuta T, Bennett C, et al.
Bioorg Med Chem Lett
. 2010 Jun;
20(15):4602-6.
PMID: 20580233
A series of spiro-azetidines and azetidinones has been evaluated as novel blockers of the T-type calcium channel (Ca(V)3.2) which is a new therapeutic target for the potential treatment of both...
8.
Wang Y, Strickland C, Voigt J, Kennedy M, Beyer B, Senior M, et al.
J Med Chem
. 2010 Jan;
53(3):942-50.
PMID: 20043700
Fragment-based NMR screening, X-ray crystallography, structure-based design, and focused chemical library design were used to identify novel inhibitors for BACE-1. A rapid optimization of an initial NMR hit was achieved...
9.
Zhu Z, Sun Z, Ye Y, Voigt J, Strickland C, Smith E, et al.
J Med Chem
. 2010 Jan;
53(3):951-65.
PMID: 20043696
A number of novel amidine containing heterocycles were designed to reproduce the unique interaction pattern, revealed by X-ray crystallography, between the BACE-1 catalytic diad and a weak NMR screening hit...
10.
Sun Z, Zhu Z, Ye Y, McKittrick B, Czarniecki M, Greenlee W, et al.
Bioorg Med Chem Lett
. 2009 Oct;
19(23):6801-5.
PMID: 19864135
A class of novel 2-aminobenzothiazoles have been identified as NPY Y(1) antagonists. Various N-heterocyclic substituted aminophenethyl-2-aminobenzothiazole analogs were synthesized to explore the SAR. Isothiourea analogs and ligands with high potency...