List of works - Ermanno Valoti

2,6-Difluorobenzamide Inhibitors of Bacterial Cell Division Protein FtsZ: Design, Synthesis, and Structure-Activity Relationships.

scientific article published on 6 June 2017

3-(Benzodioxan-2-ylmethoxy)-2,6-difluorobenzamides bearing hydrophobic substituents at the 7-position of the benzodioxane nucleus potently inhibit methicillin-resistant Sa and Mtb cell division.

scientific article

5-(2-Pyrrolidinyl)oxazolidinones and 2-(2-pyrrolidinyl)benzodioxanes: synthesis of all the stereoisomers and alpha4beta2 nicotinic affinity

scientific article

6-methoxy-7-benzofuranoxy and 6-methoxy-7-indolyloxy analogues of 2-[2-(2,6-Dimethoxyphenoxy)ethyl]aminomethyl-1,4-benzodioxane (WB4101):1 discovery of a potent and selective α1D-adrenoceptor antagonist.

scientific article

A selective alpha1D-adrenoreceptor antagonist inhibits human prostate cancer cell proliferation and motility "in vitro".

scientific article published on 24 November 2015

Affinity and activity profiling of unichiral 8-substituted 1,4-benzodioxane analogues of WB4101 reveals a potent and selective α1B-adrenoceptor antagonist.

scientific article

An investigation into the influence of counterion on the RS-propranolol and S-propranolol skin permeability.

scientific article published in March 2010

Behavioural and pharmacological characterization of a novel cannabinomimetic adamantane-derived indole, APICA, and considerations on the possible misuse as a psychotropic spice abuse, in C57bl/6J mice.

scientific article published on 6 January 2016

Benzamide Derivatives Targeting the Cell Division Protein FtsZ: Modifications of the Linker and the Benzodioxane Scaffold and Their Effects on Antimicrobial Activity

scientific article published on 04 April 2020

Benzodioxane-Benzamides as Antibacterial Agents: Computational and SAR Studies to Evaluate the Influence of the 7-Substitution in FtsZ Interaction

scientific article published on 11 December 2019

Benzodioxane-benzamides as new bacterial cell division inhibitors

scientific article published on 18 October 2014

Cardiovascular hybrid drugs: new benzazepinone derivatives as bradycardic agents endowed with selective beta1-non-competitive antagonism

scientific article published in April 2003

Characterization of in vitro metabolites of JWH-018, JWH-073 and their 4-methyl derivatives, markers of the abuse of these synthetic cannabinoids

scientific article published on 12 March 2014

Chemistry and Pharmacology of a Series of Unichiral Analogues of 2-(2-Pyrrolidinyl)-1,4-benzodioxane, Prolinol Phenyl Ether, and Prolinol 3-Pyridyl Ether Designed as α4β2-Nicotinic Acetylcholine Receptor Agonists

scientific article published on 30 July 2015

Construction of human ghrelin receptor (hGHS-R1a) model using a fragmental prediction approach and validation through docking analysis

scientific article published on June 2006

Corrigendum to “Synthesis and α4β2 nicotinic affinity of unichiral 5-(2-pyrrolidinyl)oxazolidinones and 2-(2-pyrrolidinyl)benzodioxanes” [Bioorg. Med. Chem. Lett. 16 (2006) 5610–5615]

scholarly article published in Bioorganic & Medicinal Chemistry Letters

Design, synthesis and binding affinity of acetylcholine carbamoyl analogues

scientific article published on 18 September 2013

Enhanced oral bioavailability of a novel folate salt: comparison with folic acid and a calcium folate salt in a pharmacokinetic study in rats.

scientific article

Exploring the space of histidine containing dipeptides in search of novel efficient RCS sequestering agents

scientific article published on 30 May 2013

Farnesyltransferase inhibitors: CAAX mimetics based on different biaryl scaffolds

scientific article published on 30 April 2014

From 2-aminomethyl-1,4-benzodioxane enantiomers to unichiral 2-cyano- and 2-carbonyl-substituted benzodioxanes via dichloroamine

scientific article published on 26 June 2014

How Reaction Conditions May Influence the Regioselectivity in the Synthesis of 2,3-Dihydro-1,4-benzoxathiine Derivatives

scientific article published on 11 October 2018

How do reaction conditions affect the enantiopure synthesis of 2-substituted-1,4-benzodioxane derivatives?

scientific article published on 12 May 2018

Identification of 1-butyl-3-(1-(4-methyl)naphtoyl)indole detected for the first time in “herbal high” products on the Italian market

article

Modelling of full-length human alpha4beta2 nicotinic receptor by fragmental approach and analysis of its binding modes

scientific article

New Ras CAAX mimetics: design, synthesis, antiproliferative activity, and RAS prenylation inhibition

scientific article published on 17 July 2009

Oral Bioavailability and Pharmacokinetics of Nonanimal Chondroitin Sulfate and Its Constituents in Healthy Male Volunteers

scientific article published on 24 July 2018

Peptidomimetic inhibitors of farnesyltransferase with high in vitro activity and significant cellular potency

scientific article published on 8 September 2007

Predicting the physicochemical profile of diastereoisomeric histidine-containing dipeptides by property space analysis

scientific article published on 8 May 2012

QSAR study for a novel series of ortho disubstituted phenoxy analogues of alpha1-adrenoceptor antagonist WB4101.

scientific article published on 5 June 2006

QSAR study for a novel series of ortho monosubstituted phenoxy analogues of alpha1-adrenoceptor antagonist WB4101.

scientific article

Stressed degradation studies of domiphen bromide by LC-ESI-MS/MS identify a novel promising antimicrobial agent

scientific article published on 30 June 2018

Structure-affinity studies for a novel series of homochiral naphtho and tetrahydronaphtho analogues of alpha 1 antagonist WB-4101.

scientific article published in September 2004

Synthesis and alpha4beta2 nicotinic affinity of 2-pyrrolidinylmethoxyimines and prolinal oxime ethers

scientific article published in December 2004

Synthesis and α4β2 nicotinic affinity of unichiral 5-(2-pyrrolidinyl)oxazolidinones and 2-(2-pyrrolidinyl)benzodioxanes

scientific article published in 2006

Synthesis of homochiral 5- and 8-substituted 2-[((2-(2,6-dimethoxyphenoxy)-ethyl)amino)methyl]-1,4-benzodioxanes and electrophoretic determination of their enantiomeric excess

scientific article published on 01 February 2001

Thiazole- and imidazole-containing peptidomimetic inhibitors of protein farnesyltransferase

scientific article published on 13 July 2011

Unichiral 2-(2'-pyrrolidinyl)-1,4-benzodioxanes: the 2R,2'S diastereomer of the N-methyl-7-hydroxy analogue is a potent α4β2- and α6β2-nicotinic acetylcholine receptor partial agonist

scientific article published on 11 October 2011

WB4101-related compounds: new, subtype-selective alpha1-adrenoreceptor antagonists (or inverse agonists?).

scientific article published in November 2006

List of works by Ermanno Valoti

2,6-Difluorobenzamide Inhibitors of Bacterial Cell Division Protein FtsZ: Design, Synthesis, and Structure-Activity Relationships.

3-(Benzodioxan-2-ylmethoxy)-2,6-difluorobenzamides bearing hydrophobic substituents at the 7-position of the benzodioxane nucleus potently inhibit methicillin-resistant Sa and Mtb cell division.

5-(2-Pyrrolidinyl)oxazolidinones and 2-(2-pyrrolidinyl)benzodioxanes: synthesis of all the stereoisomers and alpha4beta2 nicotinic affinity

6-methoxy-7-benzofuranoxy and 6-methoxy-7-indolyloxy analogues of 2-[2-(2,6-Dimethoxyphenoxy)ethyl]aminomethyl-1,4-benzodioxane (WB4101):1 discovery of a potent and selective α1D-adrenoceptor antagonist.

A selective alpha1D-adrenoreceptor antagonist inhibits human prostate cancer cell proliferation and motility "in vitro".

Affinity and activity profiling of unichiral 8-substituted 1,4-benzodioxane analogues of WB4101 reveals a potent and selective α1B-adrenoceptor antagonist.

An investigation into the influence of counterion on the RS-propranolol and S-propranolol skin permeability.

Behavioural and pharmacological characterization of a novel cannabinomimetic adamantane-derived indole, APICA, and considerations on the possible misuse as a psychotropic spice abuse, in C57bl/6J mice.

Benzamide Derivatives Targeting the Cell Division Protein FtsZ: Modifications of the Linker and the Benzodioxane Scaffold and Their Effects on Antimicrobial Activity

Benzodioxane-Benzamides as Antibacterial Agents: Computational and SAR Studies to Evaluate the Influence of the 7-Substitution in FtsZ Interaction

Benzodioxane-benzamides as new bacterial cell division inhibitors

Cardiovascular hybrid drugs: new benzazepinone derivatives as bradycardic agents endowed with selective beta1-non-competitive antagonism

Characterization of in vitro metabolites of JWH-018, JWH-073 and their 4-methyl derivatives, markers of the abuse of these synthetic cannabinoids

Chemistry and Pharmacology of a Series of Unichiral Analogues of 2-(2-Pyrrolidinyl)-1,4-benzodioxane, Prolinol Phenyl Ether, and Prolinol 3-Pyridyl Ether Designed as α4β2-Nicotinic Acetylcholine Receptor Agonists

Construction of human ghrelin receptor (hGHS-R1a) model using a fragmental prediction approach and validation through docking analysis

Corrigendum to “Synthesis and α4β2 nicotinic affinity of unichiral 5-(2-pyrrolidinyl)oxazolidinones and 2-(2-pyrrolidinyl)benzodioxanes” [Bioorg. Med. Chem. Lett. 16 (2006) 5610–5615]

Design, synthesis and binding affinity of acetylcholine carbamoyl analogues

Enhanced oral bioavailability of a novel folate salt: comparison with folic acid and a calcium folate salt in a pharmacokinetic study in rats.

Exploring the space of histidine containing dipeptides in search of novel efficient RCS sequestering agents

Farnesyltransferase inhibitors: CAAX mimetics based on different biaryl scaffolds

From 2-aminomethyl-1,4-benzodioxane enantiomers to unichiral 2-cyano- and 2-carbonyl-substituted benzodioxanes via dichloroamine

How Reaction Conditions May Influence the Regioselectivity in the Synthesis of 2,3-Dihydro-1,4-benzoxathiine Derivatives

How do reaction conditions affect the enantiopure synthesis of 2-substituted-1,4-benzodioxane derivatives?

Identification of 1-butyl-3-(1-(4-methyl)naphtoyl)indole detected for the first time in “herbal high” products on the Italian market

Modelling of full-length human alpha4beta2 nicotinic receptor by fragmental approach and analysis of its binding modes

New Ras CAAX mimetics: design, synthesis, antiproliferative activity, and RAS prenylation inhibition

Oral Bioavailability and Pharmacokinetics of Nonanimal Chondroitin Sulfate and Its Constituents in Healthy Male Volunteers

Peptidomimetic inhibitors of farnesyltransferase with high in vitro activity and significant cellular potency

Predicting the physicochemical profile of diastereoisomeric histidine-containing dipeptides by property space analysis

QSAR study for a novel series of ortho disubstituted phenoxy analogues of alpha1-adrenoceptor antagonist WB4101.

QSAR study for a novel series of ortho monosubstituted phenoxy analogues of alpha1-adrenoceptor antagonist WB4101.

Stressed degradation studies of domiphen bromide by LC-ESI-MS/MS identify a novel promising antimicrobial agent

Structure-affinity studies for a novel series of homochiral naphtho and tetrahydronaphtho analogues of alpha 1 antagonist WB-4101.

Synthesis and alpha4beta2 nicotinic affinity of 2-pyrrolidinylmethoxyimines and prolinal oxime ethers

Synthesis and α4β2 nicotinic affinity of unichiral 5-(2-pyrrolidinyl)oxazolidinones and 2-(2-pyrrolidinyl)benzodioxanes

Synthesis of homochiral 5- and 8-substituted 2-[((2-(2,6-dimethoxyphenoxy)-ethyl)amino)methyl]-1,4-benzodioxanes and electrophoretic determination of their enantiomeric excess

Thiazole- and imidazole-containing peptidomimetic inhibitors of protein farnesyltransferase

Unichiral 2-(2'-pyrrolidinyl)-1,4-benzodioxanes: the 2R,2'S diastereomer of the N-methyl-7-hydroxy analogue is a potent α4β2- and α6β2-nicotinic acetylcholine receptor partial agonist

WB4101-related compounds: new, subtype-selective alpha1-adrenoreceptor antagonists (or inverse agonists?).