Synthesis, In Silico and In Vivo Toxicity Assessment of Functionalized Pyridophenanthridinones via Sequential MW-Assisted Intramolecular Friedel-Crafts Alkylation and Direct C-H Arylation.

A rapid, efficient, and original synthesis of novel pyrido[3,2,1-de]phenanthridin-6-ones is reported. First, the key cinnamamide intermediates 8a-f were easily prepared from commercial substituted anilines, cinnamic acid, and 2-bromobenzylbromide in a tandem amidation and N-alkylation protocol. Then, these N-aryl-N-(2-bromobenzyl) cinnamamides 8a-f were subjected to a TFA-mediated intramolecular Friedel-Crafts alkylation followed by a Pd-catalyzed direct C-H arylation to obtain a series of potentially bioactive 4-phenyl-4,5-dihydro-6H,8H-pyrido[3,2,1-de]phenanthridin-6-one derivatives 4a-f in good yields. Finally, the toxicological profile of the prepared final compounds, including their corresponding intermediates, was explored through in silico computational methods, while the acute toxicity toward zebrafish embryos (96 hpf-LC50, 50% lethal concentration) was also determined in the present study.

Exantema laterotorácico unilateral de la infancia, una enfermedad poco diagnosticada: An infrequently diagnosed disease entity / Unilateral laterothoracic exanthema of childhood

El exantema laterotorácico unilateral, también conocido como exantema asimétrico periflexural de la infancia, es una erupción eritemato-papulosa, poco o nada pruriginosa, de causa desconocida, aun cuando la mayoría de las evidencias apuntan hacia etiología viral. Se presenta en un lado del tórax, habitualmente cercano a la axila, progresa en forma centrífuga en ese lado del cuerpo y contralateralmente, para desaparecer sin secuelas en un período de 4 a 6 semanas. Se han reportado aproximadamente 300 casos en la literatura; sin embargo, la mayoría de los autores coinciden en que la falta de diagnóstico se relaciona con el desconocimiento de la enfermedad.

The unilateral laterothoracic exanthema, also known as asymmetric peri flexural exanthema of childhood, is an erythematosus papular eruption, slightly or non pruriginous, of unknown etiology, even when most of the evidence support a probable viral origin. Clinically, it initiates on one side of the thorax, generally near the axilla, progressing centrifugally on the ipsilateral side of body and contra lateral side and eventually disappears without sequelae in a period of 4 to 6 weeks. There have been reports of approximately 300 cases in the literature. However, the majority of the authors agree that the lack of diagnosis is result of the lack of knowledge about this entity.