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Hit-to-lead optimization of mouse Trace Amine Associated Receptor 1 (mTAAR1) agonists with a diphenylmethane-scaffold: Design, Synthesis, and biological study. / Chiellini, G; Nesi, G; Sestito, S; Chiarugi, S; Runfola, M; Espinoza, S; Sabatini, M; Bellusci, L; Laurino, A; Cichero, E; Gainetdinov, RR; Fossa, P; Raimondi, L; Zucchi, R; Rapposelli, S.

In: Journal of Medicinal Chemistry, 2016.

Research output: Contribution to journalArticle

Harvard

Chiellini, G, Nesi, G, Sestito, S, Chiarugi, S, Runfola, M, Espinoza, S, Sabatini, M, Bellusci, L, Laurino, A, Cichero, E, Gainetdinov, RR, Fossa, P, Raimondi, L, Zucchi, R & Rapposelli, S 2016, 'Hit-to-lead optimization of mouse Trace Amine Associated Receptor 1 (mTAAR1) agonists with a diphenylmethane-scaffold: Design, Synthesis, and biological study.', Journal of Medicinal Chemistry. <https://www.ncbi.nlm.nih.gov/pubmed/27731647>

APA

Chiellini, G., Nesi, G., Sestito, S., Chiarugi, S., Runfola, M., Espinoza, S., Sabatini, M., Bellusci, L., Laurino, A., Cichero, E., Gainetdinov, RR., Fossa, P., Raimondi, L., Zucchi, R., & Rapposelli, S. (2016). Hit-to-lead optimization of mouse Trace Amine Associated Receptor 1 (mTAAR1) agonists with a diphenylmethane-scaffold: Design, Synthesis, and biological study. Journal of Medicinal Chemistry. https://www.ncbi.nlm.nih.gov/pubmed/27731647

Vancouver

Chiellini G, Nesi G, Sestito S, Chiarugi S, Runfola M, Espinoza S et al. Hit-to-lead optimization of mouse Trace Amine Associated Receptor 1 (mTAAR1) agonists with a diphenylmethane-scaffold: Design, Synthesis, and biological study. Journal of Medicinal Chemistry. 2016.

Author

Chiellini, G ; Nesi, G ; Sestito, S ; Chiarugi, S ; Runfola, M ; Espinoza, S ; Sabatini, M ; Bellusci, L ; Laurino, A ; Cichero, E ; Gainetdinov, RR ; Fossa, P ; Raimondi, L ; Zucchi, R ; Rapposelli, S. / Hit-to-lead optimization of mouse Trace Amine Associated Receptor 1 (mTAAR1) agonists with a diphenylmethane-scaffold: Design, Synthesis, and biological study. In: Journal of Medicinal Chemistry. 2016.

BibTeX

@article{35232ff5df2d45f6b8dc766bcc9b1415,
title = "Hit-to-lead optimization of mouse Trace Amine Associated Receptor 1 (mTAAR1) agonists with a diphenylmethane-scaffold: Design, Synthesis, and biological study.",
abstract = "The trace amine-associated receptor 1 (TAAR1) is a G-protein-coupled receptors (GPCR) potently activated by a variety of molecules besides trace amines (TAs), including thyroid hormone-derivatives like 3-iodothyronamine (T1AM), catechol-O-methyltransferase products like 3-methoxytyramine, and amphetamine-related compounds. Accordingly, TAAR1 is considered a promising target for medicinal development. To gain more insights into TAAR1 physiological functions and validation of its therapeutic potential we recently developed a new class of thyronamine-like derivatives. Among them compound SG2 showed high affinity and potent agonist activity at mouse TAAR1. In the present work we describe design, the synthesis and SAR study of a new series of compounds (1-16) obtained by introducing specific structural changes at key points of our lead-compound SG2 skeleton. Five of the newly synthesized compounds displayed mTAAR1 agonist activity higher than both SG2 and T1AM. Selected diphenylmethane analogs, namely 1 and 2, sho",
author = "G Chiellini and G Nesi and S Sestito and S Chiarugi and M Runfola and S Espinoza and M Sabatini and L Bellusci and A Laurino and E Cichero and RR Gainetdinov and P Fossa and L Raimondi and R Zucchi and S. Rapposelli",
year = "2016",
language = "не определен",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
publisher = "American Chemical Society",

}

RIS

TY - JOUR

T1 - Hit-to-lead optimization of mouse Trace Amine Associated Receptor 1 (mTAAR1) agonists with a diphenylmethane-scaffold: Design, Synthesis, and biological study.

AU - Chiellini, G

AU - Nesi, G

AU - Sestito, S

AU - Chiarugi, S

AU - Runfola, M

AU - Espinoza, S

AU - Sabatini, M

AU - Bellusci, L

AU - Laurino, A

AU - Cichero, E

AU - Gainetdinov, RR

AU - Fossa, P

AU - Raimondi, L

AU - Zucchi, R

AU - Rapposelli, S.

PY - 2016

Y1 - 2016

N2 - The trace amine-associated receptor 1 (TAAR1) is a G-protein-coupled receptors (GPCR) potently activated by a variety of molecules besides trace amines (TAs), including thyroid hormone-derivatives like 3-iodothyronamine (T1AM), catechol-O-methyltransferase products like 3-methoxytyramine, and amphetamine-related compounds. Accordingly, TAAR1 is considered a promising target for medicinal development. To gain more insights into TAAR1 physiological functions and validation of its therapeutic potential we recently developed a new class of thyronamine-like derivatives. Among them compound SG2 showed high affinity and potent agonist activity at mouse TAAR1. In the present work we describe design, the synthesis and SAR study of a new series of compounds (1-16) obtained by introducing specific structural changes at key points of our lead-compound SG2 skeleton. Five of the newly synthesized compounds displayed mTAAR1 agonist activity higher than both SG2 and T1AM. Selected diphenylmethane analogs, namely 1 and 2, sho

AB - The trace amine-associated receptor 1 (TAAR1) is a G-protein-coupled receptors (GPCR) potently activated by a variety of molecules besides trace amines (TAs), including thyroid hormone-derivatives like 3-iodothyronamine (T1AM), catechol-O-methyltransferase products like 3-methoxytyramine, and amphetamine-related compounds. Accordingly, TAAR1 is considered a promising target for medicinal development. To gain more insights into TAAR1 physiological functions and validation of its therapeutic potential we recently developed a new class of thyronamine-like derivatives. Among them compound SG2 showed high affinity and potent agonist activity at mouse TAAR1. In the present work we describe design, the synthesis and SAR study of a new series of compounds (1-16) obtained by introducing specific structural changes at key points of our lead-compound SG2 skeleton. Five of the newly synthesized compounds displayed mTAAR1 agonist activity higher than both SG2 and T1AM. Selected diphenylmethane analogs, namely 1 and 2, sho

M3 - статья

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

SN - 0022-2623

ER -

ID: 7598887