Synthesis of 1,2,4-triazole derivatives: Binding properties on endothelin receptors

L. Salerno; F. Guerrera; M. Modica; G. Romeo; V. Pittalà; M. A. Siracusa; I. Mereghetti; A. Cagnotto; T. Mennini

doi:10.2174/157340607782360281

Synthesis of 1,2,4-triazole derivatives: Binding properties on endothelin receptors

L. Salerno, F. Guerrera, M. Modica, G. Romeo, V. Pittalà, M. A. Siracusa, I. Mereghetti, A. Cagnotto, T. Mennini

Istituto di Ricerche Farmacologiche "Mario Negri"

Research output: Contribution to journal › Article › peer-review

Abstract

In the present study we describe the synthesis of a new series of 1,2,4-triazoles: [3-(arylmethyl)thio-5-aryl-4H-[1,2,4] triazol-4-y1]acetic acids 5a-g, [5-(arylmethyl)thio-3-aryl-1H-[1,2,4]triazol-1-y1]acetic acids 8a-d, and [3-(aryl-methyl) thio-5-aryl-1H-[1,2,4]triazol-1-y1] acetic acids 9a-d. These compounds were tested in binding assays to evaluate their ability as ligands for human ET_A and ET_B receptors stably expressed in CHO cells; some of the tested compounds showed affinity in the micromolar range.

Original language	English
Pages (from-to)	551-560
Number of pages	10
Journal	Medicinal Chemistry
Volume	3
Issue number	6
DOIs	https://doi.org/10.2174/157340607782360281
Publication status	Published - Nov 2007

Keywords

1,2,4-triazoles
Binding assays
Endothelins
ET receptors
Hypertension
Regioisomers

ASJC Scopus subject areas

Drug Discovery

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title = "Synthesis of 1,2,4-triazole derivatives: Binding properties on endothelin receptors",

abstract = "In the present study we describe the synthesis of a new series of 1,2,4-triazoles: [3-(arylmethyl)thio-5-aryl-4H-[1,2,4] triazol-4-y1]acetic acids 5a-g, [5-(arylmethyl)thio-3-aryl-1H-[1,2,4]triazol-1-y1]acetic acids 8a-d, and [3-(aryl-methyl) thio-5-aryl-1H-[1,2,4]triazol-1-y1] acetic acids 9a-d. These compounds were tested in binding assays to evaluate their ability as ligands for human ETA and ETB receptors stably expressed in CHO cells; some of the tested compounds showed affinity in the micromolar range.",

keywords = "1,2,4-triazoles, Binding assays, Endothelins, ET receptors, Hypertension, Regioisomers",

author = "L. Salerno and F. Guerrera and M. Modica and G. Romeo and V. Pittal{\`a} and Siracusa, {M. A.} and I. Mereghetti and A. Cagnotto and T. Mennini",

year = "2007",

month = nov,

doi = "10.2174/157340607782360281",

language = "English",

volume = "3",

pages = "551--560",

journal = "Medicinal Chemistry",

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T2 - Binding properties on endothelin receptors

AU - Salerno, L.

AU - Guerrera, F.

AU - Modica, M.

AU - Romeo, G.

AU - Pittalà, V.

AU - Siracusa, M. A.

AU - Mereghetti, I.

AU - Cagnotto, A.

AU - Mennini, T.

PY - 2007/11

Y1 - 2007/11

N2 - In the present study we describe the synthesis of a new series of 1,2,4-triazoles: [3-(arylmethyl)thio-5-aryl-4H-[1,2,4] triazol-4-y1]acetic acids 5a-g, [5-(arylmethyl)thio-3-aryl-1H-[1,2,4]triazol-1-y1]acetic acids 8a-d, and [3-(aryl-methyl) thio-5-aryl-1H-[1,2,4]triazol-1-y1] acetic acids 9a-d. These compounds were tested in binding assays to evaluate their ability as ligands for human ETA and ETB receptors stably expressed in CHO cells; some of the tested compounds showed affinity in the micromolar range.

AB - In the present study we describe the synthesis of a new series of 1,2,4-triazoles: [3-(arylmethyl)thio-5-aryl-4H-[1,2,4] triazol-4-y1]acetic acids 5a-g, [5-(arylmethyl)thio-3-aryl-1H-[1,2,4]triazol-1-y1]acetic acids 8a-d, and [3-(aryl-methyl) thio-5-aryl-1H-[1,2,4]triazol-1-y1] acetic acids 9a-d. These compounds were tested in binding assays to evaluate their ability as ligands for human ETA and ETB receptors stably expressed in CHO cells; some of the tested compounds showed affinity in the micromolar range.

KW - 1,2,4-triazoles

KW - Binding assays

KW - Endothelins

KW - ET receptors

KW - Hypertension

KW - Regioisomers

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