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Zsolt Nemethy

Explore the profile of Zsolt Nemethy including associated specialties, affiliations and a list of published articles. Areas
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Articles 16
Citations 206
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Recent Articles
1.
Nagy L, Bali Z, Ledneczki I, Nemethy Z, Lendvai B, Hernadi I
ASN Neuro . 2024 Jul; 16(1):2371160. PMID: 39024573
Promising new pharmacological strategies for the enhancement of cognition target either nicotinic acetylcholine receptors (nAChR) or N-methyl-D-aspartate receptors (NMDAR). There is also an increasing interest in low-dose combination therapies co-targeting...
2.
Ledneczki I, Tapolcsanyi P, Gabor E, Eles J, Barabas J, Beni Z, et al.
J Med Chem . 2024 Feb; 67(5):3643-3667. PMID: 38393759
Steroid-based histamine H receptor antagonists (d-homoazasteroids) were designed by combining distinct structural elements of HTS hit molecules. They were characterized, and several of them displayed remarkably high affinity for H...
3.
Ledneczki I, Nemethy Z, Molnar K, Tapolcsanyi P, Ilkei V, Vago I, et al.
J Med Chem . 2023 Nov; 66(23):16276-16302. PMID: 37989278
During optimization of a previously identified lead compound, attempts were made to optimize the reactive indole structural element, the suboptimal metabolic stability, as well as the low kinetic solubility. It...
4.
Nemethy Z, Kiss B, Lethbridge N, Chazot P, Hajnik T, Toth A, et al.
Eur J Pharmacol . 2021 Dec; 916:174621. PMID: 34965389
The histamine H receptor is a favourable target for the treatment of cognitive deficits. Here we report the in vitro and in vivo profile of RGH-235, a new potent, selective,...
5.
Roman V, Kedves R, Kelemen K, Nemethy Z, Sperlagh B, Lendvai B, et al.
Physiol Rep . 2021 Nov; 9(21):e15088. PMID: 34762352
Neuronal networks cause changes in behaviorally important information processing through the vesicular release of neurotransmitters governed by the rate and timing of action potentials (APs). Herein, we provide evidence that...
6.
Ledneczki I, Horvath A, Tapolcsanyi P, Eles J, Molnar K, Vago I, et al.
Eur J Med Chem . 2021 Jun; 222:113560. PMID: 34111828
HTS campaign of the corporate compound collection resulted in a novel, oxalic acid diamide scaffold of α7 nACh receptor positive allosteric modulators. During the hit expansion, several derivatives, such as...
7.
Ledneczki I, Tapolcsanyi P, Gabor E, Visegrady A, Vass M, Eles J, et al.
Eur J Med Chem . 2021 Feb; 214:113189. PMID: 33540354
The paper focuses on the scaffold hopping-based discovery and characterization of novel nicotinic alpha 7 receptor positive modulator (α7 nAChR PAM) ligands around the reference molecule (A-867744). First, substantial efforts...
8.
Kiss B, Nemethy Z, Fazekas K, Kurko D, Gyertyan I, Saghy K, et al.
Drug Des Devel Ther . 2019 Oct; 13:3229-3248. PMID: 31571826
Introduction: Cariprazine, a dopamine D-preferring D/D receptor partial agonist and serotonin 5-HT receptor partial agonist, has two major human metabolites, desmethyl-cariprazine (DCAR) and didesmethyl-cariprazine (DDCAR). The metabolite pharmacology was profiled...
9.
Ledneczki I, Nemethy Z, Tapolcsanyi P, Eles J, Greiner I, Gabor E, et al.
Bioorg Med Chem Lett . 2019 Sep; 29(20):126643. PMID: 31492518
To further proceed with our previous work, novel steroid-based histamine H receptor antagonists were identified and characterized. Using an 'amine-to-amide' modification strategy at position 17, in vitro and in vivo...
10.
Ledneczki I, Tapolcsanyi P, Gabor E, Eles J, Greiner I, Schmidt E, et al.
Bioorg Med Chem Lett . 2017 Sep; 27(19):4525-4530. PMID: 28888822
Emerging from an HTS campaign, novel steroid-based histamine H receptor antagonists were identified and characterized. Structural moieties of the hit compounds were combined to improve binding affinities which resulted in...