The Experts below are selected from a list of 309 Experts worldwide ranked by ideXlab platform
Ramon Mercè - One of the best experts on this subject based on the ideXlab platform.
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Identification of novel indanylsulfonamide guanylhydrazones as potent 5-HT6 serotonin receptor antagonists.
Journal of Medicinal Chemistry, 2009Co-Authors: Neus Mesquida, Sara López-pérez, Ramon Mercè, Jordi Frigola, Immaculada Dinarès, Jörg Holenz, Raquel Pérez, Javier Burgueño, Ermitas AlcaldeAbstract:Changing the N,N-(dimethylamino)ethyl side chain in the N-[3-(aminoethyl)inden-5-yl]sulfonamide 5-HT6 serotonin receptor agonists 1 by a conformationally rigid guanylhydrazone moiety at the Indene 3-position led to the identification of the title indanylguanylhydrazones 6, which exhibited excellent binding affinities and an antagonistic response at the 5-HT6 receptor, with Ki and IC50 values in the nanomolar range (Ki ≥ 1.2 nM, IC50 ≥ 47 nM, and Imax ≤ 173%).
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Indene-Based Scaffolds. 2. An Indole−Indene Switch: Discovery of Novel Indenylsulfonamides as 5-HT6 Serotonin Receptor Agonists†
Journal of Medicinal Chemistry, 2009Co-Authors: Ermitas Alcalde, Neus Mesquida, Sara López-pérez, Jordi Frigola, Ramon MercèAbstract:Scaffold selection involving an indole-to-Indene core change led to the discovery of a series of indenylsulfonamides that act as 5-HT6 serotonin receptor agonists. The variety of the targeted ligands and their synthetic complexity required multistep synthetic approaches. The novel indenylsulfonamides exhibited variable binding affinities for the 5-HT6 receptor, and the in vitro primary binding profiles of the preferred compounds revealed them to be 5-HT6 receptor agonists with Ki values ≥4.5 nM. The structural changes responsible for enhancing the affinities indicated a directing effect modulated by the nature of the Indene core, the substitution at the aminoethyl side chain, and especially by the aryl(heteroaryl)sulfonyl group on the Indene 5-position. A representative of the family, the N-(inden-5-yl)imidazothiazole-5-sulfonamide (43), exhibited a high affinity and functioned as a potent full agonist for the 5-HT6 receptor (Ki = 4.5 nM, EC50 = 0.9 nM, Emax = 98%).
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Indene-based scaffolds. 2. An indole-Indene switch: discovery of novel indenylsulfonamides as 5-HT6 serotonin receptor agonists.
Journal of Medicinal Chemistry, 2009Co-Authors: Ermitas Alcalde, Neus Mesquida, Sara López-pérez, Jordi Frigola, Ramon MercèAbstract:Scaffold selection involving an indole-to-Indene core change led to the discovery of a series of indenylsulfonamides that act as 5-HT6 serotonin receptor agonists. The variety of the targeted ligands and their synthetic complexity required multistep synthetic approaches. The novel indenylsulfonamides exhibited variable binding affinities for the 5-HT6 receptor, and the in vitro primary binding profiles of the preferred compounds revealed them to be 5-HT6 receptor agonists with Ki values ≥4.5 nM. The structural changes responsible for enhancing the affinities indicated a directing effect modulated by the nature of the Indene core, the substitution at the aminoethyl side chain, and especially by the aryl(heteroaryl)sulfonyl group on the Indene 5-position. A representative of the family, the N-(inden-5-yl)imidazothiazole-5-sulfonamide (43), exhibited a high affinity and functioned as a potent full agonist for the 5-HT6 receptor (Ki = 4.5 nM, EC50 = 0.9 nM, Emax = 98%).
Ermitas Alcalde - One of the best experts on this subject based on the ideXlab platform.
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Identification of novel indanylsulfonamide guanylhydrazones as potent 5-HT6 serotonin receptor antagonists.
Journal of Medicinal Chemistry, 2009Co-Authors: Neus Mesquida, Sara López-pérez, Ramon Mercè, Jordi Frigola, Immaculada Dinarès, Jörg Holenz, Raquel Pérez, Javier Burgueño, Ermitas AlcaldeAbstract:Changing the N,N-(dimethylamino)ethyl side chain in the N-[3-(aminoethyl)inden-5-yl]sulfonamide 5-HT6 serotonin receptor agonists 1 by a conformationally rigid guanylhydrazone moiety at the Indene 3-position led to the identification of the title indanylguanylhydrazones 6, which exhibited excellent binding affinities and an antagonistic response at the 5-HT6 receptor, with Ki and IC50 values in the nanomolar range (Ki ≥ 1.2 nM, IC50 ≥ 47 nM, and Imax ≤ 173%).
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Indene-Based Scaffolds. 2. An Indole−Indene Switch: Discovery of Novel Indenylsulfonamides as 5-HT6 Serotonin Receptor Agonists†
Journal of Medicinal Chemistry, 2009Co-Authors: Ermitas Alcalde, Neus Mesquida, Sara López-pérez, Jordi Frigola, Ramon MercèAbstract:Scaffold selection involving an indole-to-Indene core change led to the discovery of a series of indenylsulfonamides that act as 5-HT6 serotonin receptor agonists. The variety of the targeted ligands and their synthetic complexity required multistep synthetic approaches. The novel indenylsulfonamides exhibited variable binding affinities for the 5-HT6 receptor, and the in vitro primary binding profiles of the preferred compounds revealed them to be 5-HT6 receptor agonists with Ki values ≥4.5 nM. The structural changes responsible for enhancing the affinities indicated a directing effect modulated by the nature of the Indene core, the substitution at the aminoethyl side chain, and especially by the aryl(heteroaryl)sulfonyl group on the Indene 5-position. A representative of the family, the N-(inden-5-yl)imidazothiazole-5-sulfonamide (43), exhibited a high affinity and functioned as a potent full agonist for the 5-HT6 receptor (Ki = 4.5 nM, EC50 = 0.9 nM, Emax = 98%).
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Indene-based scaffolds. 2. An indole-Indene switch: discovery of novel indenylsulfonamides as 5-HT6 serotonin receptor agonists.
Journal of Medicinal Chemistry, 2009Co-Authors: Ermitas Alcalde, Neus Mesquida, Sara López-pérez, Jordi Frigola, Ramon MercèAbstract:Scaffold selection involving an indole-to-Indene core change led to the discovery of a series of indenylsulfonamides that act as 5-HT6 serotonin receptor agonists. The variety of the targeted ligands and their synthetic complexity required multistep synthetic approaches. The novel indenylsulfonamides exhibited variable binding affinities for the 5-HT6 receptor, and the in vitro primary binding profiles of the preferred compounds revealed them to be 5-HT6 receptor agonists with Ki values ≥4.5 nM. The structural changes responsible for enhancing the affinities indicated a directing effect modulated by the nature of the Indene core, the substitution at the aminoethyl side chain, and especially by the aryl(heteroaryl)sulfonyl group on the Indene 5-position. A representative of the family, the N-(inden-5-yl)imidazothiazole-5-sulfonamide (43), exhibited a high affinity and functioned as a potent full agonist for the 5-HT6 receptor (Ki = 4.5 nM, EC50 = 0.9 nM, Emax = 98%).
Neus Mesquida - One of the best experts on this subject based on the ideXlab platform.
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Identification of novel indanylsulfonamide guanylhydrazones as potent 5-HT6 serotonin receptor antagonists.
Journal of Medicinal Chemistry, 2009Co-Authors: Neus Mesquida, Sara López-pérez, Ramon Mercè, Jordi Frigola, Immaculada Dinarès, Jörg Holenz, Raquel Pérez, Javier Burgueño, Ermitas AlcaldeAbstract:Changing the N,N-(dimethylamino)ethyl side chain in the N-[3-(aminoethyl)inden-5-yl]sulfonamide 5-HT6 serotonin receptor agonists 1 by a conformationally rigid guanylhydrazone moiety at the Indene 3-position led to the identification of the title indanylguanylhydrazones 6, which exhibited excellent binding affinities and an antagonistic response at the 5-HT6 receptor, with Ki and IC50 values in the nanomolar range (Ki ≥ 1.2 nM, IC50 ≥ 47 nM, and Imax ≤ 173%).
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Indene-Based Scaffolds. 2. An Indole−Indene Switch: Discovery of Novel Indenylsulfonamides as 5-HT6 Serotonin Receptor Agonists†
Journal of Medicinal Chemistry, 2009Co-Authors: Ermitas Alcalde, Neus Mesquida, Sara López-pérez, Jordi Frigola, Ramon MercèAbstract:Scaffold selection involving an indole-to-Indene core change led to the discovery of a series of indenylsulfonamides that act as 5-HT6 serotonin receptor agonists. The variety of the targeted ligands and their synthetic complexity required multistep synthetic approaches. The novel indenylsulfonamides exhibited variable binding affinities for the 5-HT6 receptor, and the in vitro primary binding profiles of the preferred compounds revealed them to be 5-HT6 receptor agonists with Ki values ≥4.5 nM. The structural changes responsible for enhancing the affinities indicated a directing effect modulated by the nature of the Indene core, the substitution at the aminoethyl side chain, and especially by the aryl(heteroaryl)sulfonyl group on the Indene 5-position. A representative of the family, the N-(inden-5-yl)imidazothiazole-5-sulfonamide (43), exhibited a high affinity and functioned as a potent full agonist for the 5-HT6 receptor (Ki = 4.5 nM, EC50 = 0.9 nM, Emax = 98%).
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Indene-based scaffolds. 2. An indole-Indene switch: discovery of novel indenylsulfonamides as 5-HT6 serotonin receptor agonists.
Journal of Medicinal Chemistry, 2009Co-Authors: Ermitas Alcalde, Neus Mesquida, Sara López-pérez, Jordi Frigola, Ramon MercèAbstract:Scaffold selection involving an indole-to-Indene core change led to the discovery of a series of indenylsulfonamides that act as 5-HT6 serotonin receptor agonists. The variety of the targeted ligands and their synthetic complexity required multistep synthetic approaches. The novel indenylsulfonamides exhibited variable binding affinities for the 5-HT6 receptor, and the in vitro primary binding profiles of the preferred compounds revealed them to be 5-HT6 receptor agonists with Ki values ≥4.5 nM. The structural changes responsible for enhancing the affinities indicated a directing effect modulated by the nature of the Indene core, the substitution at the aminoethyl side chain, and especially by the aryl(heteroaryl)sulfonyl group on the Indene 5-position. A representative of the family, the N-(inden-5-yl)imidazothiazole-5-sulfonamide (43), exhibited a high affinity and functioned as a potent full agonist for the 5-HT6 receptor (Ki = 4.5 nM, EC50 = 0.9 nM, Emax = 98%).
Jordi Frigola - One of the best experts on this subject based on the ideXlab platform.
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Identification of novel indanylsulfonamide guanylhydrazones as potent 5-HT6 serotonin receptor antagonists.
Journal of Medicinal Chemistry, 2009Co-Authors: Neus Mesquida, Sara López-pérez, Ramon Mercè, Jordi Frigola, Immaculada Dinarès, Jörg Holenz, Raquel Pérez, Javier Burgueño, Ermitas AlcaldeAbstract:Changing the N,N-(dimethylamino)ethyl side chain in the N-[3-(aminoethyl)inden-5-yl]sulfonamide 5-HT6 serotonin receptor agonists 1 by a conformationally rigid guanylhydrazone moiety at the Indene 3-position led to the identification of the title indanylguanylhydrazones 6, which exhibited excellent binding affinities and an antagonistic response at the 5-HT6 receptor, with Ki and IC50 values in the nanomolar range (Ki ≥ 1.2 nM, IC50 ≥ 47 nM, and Imax ≤ 173%).
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Indene-Based Scaffolds. 2. An Indole−Indene Switch: Discovery of Novel Indenylsulfonamides as 5-HT6 Serotonin Receptor Agonists†
Journal of Medicinal Chemistry, 2009Co-Authors: Ermitas Alcalde, Neus Mesquida, Sara López-pérez, Jordi Frigola, Ramon MercèAbstract:Scaffold selection involving an indole-to-Indene core change led to the discovery of a series of indenylsulfonamides that act as 5-HT6 serotonin receptor agonists. The variety of the targeted ligands and their synthetic complexity required multistep synthetic approaches. The novel indenylsulfonamides exhibited variable binding affinities for the 5-HT6 receptor, and the in vitro primary binding profiles of the preferred compounds revealed them to be 5-HT6 receptor agonists with Ki values ≥4.5 nM. The structural changes responsible for enhancing the affinities indicated a directing effect modulated by the nature of the Indene core, the substitution at the aminoethyl side chain, and especially by the aryl(heteroaryl)sulfonyl group on the Indene 5-position. A representative of the family, the N-(inden-5-yl)imidazothiazole-5-sulfonamide (43), exhibited a high affinity and functioned as a potent full agonist for the 5-HT6 receptor (Ki = 4.5 nM, EC50 = 0.9 nM, Emax = 98%).
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Indene-based scaffolds. 2. An indole-Indene switch: discovery of novel indenylsulfonamides as 5-HT6 serotonin receptor agonists.
Journal of Medicinal Chemistry, 2009Co-Authors: Ermitas Alcalde, Neus Mesquida, Sara López-pérez, Jordi Frigola, Ramon MercèAbstract:Scaffold selection involving an indole-to-Indene core change led to the discovery of a series of indenylsulfonamides that act as 5-HT6 serotonin receptor agonists. The variety of the targeted ligands and their synthetic complexity required multistep synthetic approaches. The novel indenylsulfonamides exhibited variable binding affinities for the 5-HT6 receptor, and the in vitro primary binding profiles of the preferred compounds revealed them to be 5-HT6 receptor agonists with Ki values ≥4.5 nM. The structural changes responsible for enhancing the affinities indicated a directing effect modulated by the nature of the Indene core, the substitution at the aminoethyl side chain, and especially by the aryl(heteroaryl)sulfonyl group on the Indene 5-position. A representative of the family, the N-(inden-5-yl)imidazothiazole-5-sulfonamide (43), exhibited a high affinity and functioned as a potent full agonist for the 5-HT6 receptor (Ki = 4.5 nM, EC50 = 0.9 nM, Emax = 98%).
Sara López-pérez - One of the best experts on this subject based on the ideXlab platform.
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Identification of novel indanylsulfonamide guanylhydrazones as potent 5-HT6 serotonin receptor antagonists.
Journal of Medicinal Chemistry, 2009Co-Authors: Neus Mesquida, Sara López-pérez, Ramon Mercè, Jordi Frigola, Immaculada Dinarès, Jörg Holenz, Raquel Pérez, Javier Burgueño, Ermitas AlcaldeAbstract:Changing the N,N-(dimethylamino)ethyl side chain in the N-[3-(aminoethyl)inden-5-yl]sulfonamide 5-HT6 serotonin receptor agonists 1 by a conformationally rigid guanylhydrazone moiety at the Indene 3-position led to the identification of the title indanylguanylhydrazones 6, which exhibited excellent binding affinities and an antagonistic response at the 5-HT6 receptor, with Ki and IC50 values in the nanomolar range (Ki ≥ 1.2 nM, IC50 ≥ 47 nM, and Imax ≤ 173%).
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Indene-Based Scaffolds. 2. An Indole−Indene Switch: Discovery of Novel Indenylsulfonamides as 5-HT6 Serotonin Receptor Agonists†
Journal of Medicinal Chemistry, 2009Co-Authors: Ermitas Alcalde, Neus Mesquida, Sara López-pérez, Jordi Frigola, Ramon MercèAbstract:Scaffold selection involving an indole-to-Indene core change led to the discovery of a series of indenylsulfonamides that act as 5-HT6 serotonin receptor agonists. The variety of the targeted ligands and their synthetic complexity required multistep synthetic approaches. The novel indenylsulfonamides exhibited variable binding affinities for the 5-HT6 receptor, and the in vitro primary binding profiles of the preferred compounds revealed them to be 5-HT6 receptor agonists with Ki values ≥4.5 nM. The structural changes responsible for enhancing the affinities indicated a directing effect modulated by the nature of the Indene core, the substitution at the aminoethyl side chain, and especially by the aryl(heteroaryl)sulfonyl group on the Indene 5-position. A representative of the family, the N-(inden-5-yl)imidazothiazole-5-sulfonamide (43), exhibited a high affinity and functioned as a potent full agonist for the 5-HT6 receptor (Ki = 4.5 nM, EC50 = 0.9 nM, Emax = 98%).
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Indene-based scaffolds. 2. An indole-Indene switch: discovery of novel indenylsulfonamides as 5-HT6 serotonin receptor agonists.
Journal of Medicinal Chemistry, 2009Co-Authors: Ermitas Alcalde, Neus Mesquida, Sara López-pérez, Jordi Frigola, Ramon MercèAbstract:Scaffold selection involving an indole-to-Indene core change led to the discovery of a series of indenylsulfonamides that act as 5-HT6 serotonin receptor agonists. The variety of the targeted ligands and their synthetic complexity required multistep synthetic approaches. The novel indenylsulfonamides exhibited variable binding affinities for the 5-HT6 receptor, and the in vitro primary binding profiles of the preferred compounds revealed them to be 5-HT6 receptor agonists with Ki values ≥4.5 nM. The structural changes responsible for enhancing the affinities indicated a directing effect modulated by the nature of the Indene core, the substitution at the aminoethyl side chain, and especially by the aryl(heteroaryl)sulfonyl group on the Indene 5-position. A representative of the family, the N-(inden-5-yl)imidazothiazole-5-sulfonamide (43), exhibited a high affinity and functioned as a potent full agonist for the 5-HT6 receptor (Ki = 4.5 nM, EC50 = 0.9 nM, Emax = 98%).
