Search

Your search keyword '"G. Szántó"' showing total 4 results
Start Over Author "G. Szántó" Journal bioorganic medicinal chemistry letters
4 results on '"G. Szántó"'

1. New V1a receptor antagonist. Part 1. Synthesis and SAR development of urea derivatives.

Author

Szántó G, Makó A, Baska F, Bozó É, Domány-Kovács K, Kurkó D, Cselenyák A, Mohácsi R, Kordás KS, and Bata I

Subjects
Antidiuretic Hormone Receptor Antagonists pharmacology, High-Throughput Screening Assays, Humans, Inhibitory Concentration 50, Piperazine chemistry, Protein Binding, Pyridines chemistry, Quinolines chemistry, Structure-Activity Relationship, Urea pharmacology, Antidiuretic Hormone Receptor Antagonists chemical synthesis, Receptors, Vasopressin metabolism, Social Behavior Disorders drug therapy, Urea chemical synthesis
Abstract

Solid preclinical evidence links vasopressin to social behavior in animals, so, extensive work has been initiated to find new vasopressin V1a receptor antagonists which can improve deteriorated social behavior in humans and can treat the core symptoms of autistic behavior, as well. Our aim was to identify new chemical entities with antagonizing effects on vasopressin V1a receptors. Starting from a moderately potent HTS hit (7), we identified a molecule (49) having nanomolar binding strength and functional activity, which is in the same range as the potency of clinically tested V1a antagonists., Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2020 Elsevier Ltd. All rights reserved.)

Published
2020
Full Text
View/download PDF

2. New V1a receptor antagonist. Part 2. Identification and optimization of triazolobenzazepines.

Author

Bozó É, Baska F, Lövei K, Szántó G, Domány-Kovács K, Kurkó D, Szondiné Kordás K, Szokoli T, and Bata I

Subjects
Animals, Antidiuretic Hormone Receptor Antagonists pharmacology, Benzazepines pharmacology, Humans, Inhibitory Concentration 50, Isomerism, Mice, Microsomes, Liver metabolism, Protein Binding, Quinolones chemistry, Rats, Structure-Activity Relationship, Antidiuretic Hormone Receptor Antagonists chemical synthesis, Benzazepines chemical synthesis, Receptors, Vasopressin metabolism, Social Behavior Disorders drug therapy
Abstract

Solid preclinical evidence links vasopressin to social behavior in animals, so, extensive work has been initiated to find new vasopressin V1a receptor antagonists which can improve deteriorated social behavior in humans and can treat the core symptoms of autistic behavior, as well. Our aim was to identify new chemical entities with antagonizing effects on vasopressin V1a receptors. Continuing our previous work, we found an in vitro and in vivo orally active V1a selective antagonist molecule (40) among [1,2,4]triazolo[4,3-a][1]benzazepines., Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2020 Elsevier Ltd. All rights reserved.)

Published
2020
Full Text
View/download PDF

3. New P2X3 receptor antagonists. Part 2: Identification and SAR of quinazolinones.

Author

Szántó G, Makó A, Vágó I, Hergert T, Bata I, Farkas B, Kolok S, and Vastag M

Subjects
4-Quinolones chemical synthesis, 4-Quinolones metabolism, Adenosine Triphosphate metabolism, Humans, Inhibitory Concentration 50, Protein Binding, Purinergic P2X Receptor Antagonists chemical synthesis, Purinergic P2X Receptor Antagonists metabolism, Quinazolinones metabolism, Receptors, Purinergic P2X3 chemistry, Structure-Activity Relationship, 4-Quinolones chemistry, Purinergic P2X Receptor Antagonists chemistry, Quinazolinones chemistry, Receptors, Purinergic P2X3 metabolism
Abstract

Numerous potent P2X3 antagonists have been discovered and the therapeutic potential of P2X3 antagonism already comprises proof-of-concept data obtained in clinical trials with the most advanced compound. We have lately reported the discovery and optimization of thia-triaza-tricycle compounds with potent P2X3 antagonistic properties. This Letter describes the SAR of a back-up series containing a 4-oxo-quinazoline central ring. The discovery of the highly potent compounds 51 is presented., (Copyright © 2016 Elsevier Ltd. All rights reserved.)

Published
2016
Full Text
View/download PDF

4. New P2X3 receptor antagonists. Part 1: Discovery and optimization of tricyclic compounds.

Author

Szántó G, Makó A, Bata I, Farkas B, Kolok S, Vastag M, and Cselenyák A

Subjects
Adenosine Triphosphate metabolism, Drug Evaluation, Preclinical, Heterocyclic Compounds, 3-Ring chemistry, Humans, Inhibitory Concentration 50, Mesylates chemistry, Microsomes metabolism, Protein Binding, Purinergic P2X Receptor Antagonists chemical synthesis, Purinergic P2X Receptor Antagonists metabolism, Receptors, Purinergic P2X3 chemistry, Structure-Activity Relationship, Heterocyclic Compounds chemistry, Heterocyclic Compounds, 3-Ring chemical synthesis, Mesylates chemical synthesis, Purinergic P2X Receptor Antagonists chemistry, Receptors, Purinergic P2X3 metabolism
Abstract

Purinergic P2X3 receptors are trimeric ligand-gated ion channels whose antagonism is an appealing yet challenging and not fully validated drug development idea. With the aim of identification of an orally active, potent human P2X3 receptor antagonist compound that can penetrate the central nervous system, the compound collection of Gedeon Richter was screened. A hit series of tricyclic compounds was subjected to a rapid, two-step optimization process focusing on increasing potency, improving metabolic stability and CNS penetrability. Attempts resulted in compound 65, a potential tool compound for testing P2X3 inhibitory effects in vivo., (Copyright © 2016 Elsevier Ltd. All rights reserved.)

Published
2016
Full Text
View/download PDF

Catalog

Books, media, physical & digital resources
See catalog results