The effect of the water-soluble furoxan derivatives on platelet aggregation has been estimated using a series of inducers.The most active compound, 3-carbamoyl-4-(hydroxymethyl)furoxan (CAS-1609), effectively inhibits aggregate formation induced by ADP and adrenaline.This result is a good basis for the search of new structures with antiaggregant activity among furoxancarboxylic acid amides.

26 Oct 2017·Journal of Medicinal ChemistryQ1 · MEDICINE

Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity

Q1 · MEDICINE

Article

Author: Paucar, Rocio ; Lazzarato, Loretta ; Ribeiro, Camila Maríngolo ; Hunt, Debbie M. ; de Souza, Paula Carolina ; Fruttero, Roberta ; dos Santos, Jean Leandro ; Franzblau, Scott Gary ; Cho, Sang Hyun ; da Silva, Patricia Bento ; Guglielmo, Stefano ; Santivañez-Veliz, Mery ; Chorilli, Marlus ; Silva, Caio Sander Paiva ; de Carvalho, Luiz Pedro S. ; Pérez-Silanes, Silvia ; Pavan, Fernando Rogério ; de Souza Costa, Carlos Alberto ; Man Chin, Chung ; Solcia, Mariana Cristina ; Chegaev, Konstantin ; Bosquesi, Priscila Longhin ; Wang, Yuehong ; dos Santos Fernandes, Guilherme Felipe ; Marino, Leonardo Biancolino ; Moreno-Viguri, Elsa

Tuberculosis, caused by Mycobacterium tuberculosis (Mtb), is the infectious disease responsible for the highest number of deaths worldwide. Herein, 22 new N-oxide-containing compounds were synthesized followed by in vitro and in vivo evaluation of their antitubercular potential against Mtb. Compound 8 was found to be the most promising compound, with MIC₉₀ values of 1.10 and 6.62 μM against active and nonreplicating Mtb, respectively. Additionally, we carried out in vivo experiments to confirm the safety and efficacy of compound 8; the compound was found to be orally bioavailable and highly effective, leading to a reduction of Mtb to undetectable levels in a mouse model of infection. Microarray-based initial studies on the mechanism of action suggest that compound 8 blocks translation. Altogether, these results indicate that benzofuroxan derivative 8 is a promising lead compound for the development of a novel chemical class of antitubercular drugs.

01 Feb 2017·Bioorganic & Medicinal Chemistry LettersQ4 · MEDICINE

New furoxan derivatives for the treatment of ocular hypertension

Q4 · MEDICINE

Article

Author: Lazzarato, Loretta ; Bastia, Elena ; Blangetti, Marco ; Guglielmo, Stefano ; Impagnatiello, Francesco ; Durante, Mariaconcetta ; Fruttero, Roberta ; Rolando, Barbara ; Gasco, Alberto ; Chegaev, Konstantin ; Masini, Emanuela ; Almirante, Nicoletta

A small series of water-soluble NO-donor furoxans bearing a basic center at the 4-position, having a wide lipophilic-hydrophilic balance range, and endowed with different NO-release capacities, were synthesized and characterized. Selected members were studied for their IOP-lowering activity in the transient ocular hypertensive rabbit model at 1% dose. The most effective IOP-lowering products were compounds 3 and 7, whose activity 60min after administration was similar to that of Timolol. Notably, 7 was characterized by a long-lasting action. The IOP-lowering activity in this series of products appeared to be modulated by the lipophilic-hydrophilic balance rather than by the NO-donor capacity.

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Indication	Highest Phase	Country/Location	Organization	Date
Angina Pectoris	Preclinical	Germany	Cassella GmbH	-
Heart Failure	Preclinical	Germany	Cassella GmbH	-

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