ABSTRACT
The discovery and development of novel inhibitors with activity against variants of human immunodeficiency virus type 1 (HIV-1) is pivotal for overcoming treatment failure. As our ongoing work on research of anti-HIV-1 inhibitors, 32 N-arylsulfonyl-3-acylindole benzoyl hydrazone derivatives were prepared by introduction of the hydrazone fragments on the N-arylsulfonyl-3-acylindolyl skeleton and preliminarily screened in vitro as HIV-1 inhibitors for the first time. Among of all the reported analogues, eight compounds exhibited significant anti-HIV-1 activity, especially N-(3-nitro)phenylsulfonyl-3-acetylindole benzoyl hydrazone (18) and N-(3-nitro)phenylsulfonyl-3-acetyl-6-methylindole benzoyl hydrazone (23) displayed the most potent anti-HIV-1 activity with EC50 values of 0.26 and 0.31 µg/mL, and TI values of >769.23 and >645.16, respectively. It is noteworthy that introduction of R3 as the methyl group and R2 as the hydrogen group could result in more potent compounds. This suggested that introduction of R3 as the methyl group could be taken into account for further preparation of these kinds of compounds as anti-HIV-1 agents
Subject(s)
Acquired Immunodeficiency Syndrome/drug therapy , HIV-1/classification , Anti-HIV Agents/analysis , HIV Fusion InhibitorsABSTRACT
Los microbicidas constituyen una nueva herramienta, todavía en proceso de investigación, que podrían ayudar en la prevención de la infección por los virus de la inmunodeficiencia humana (Human immunodeficiency virus: HIV) y de otras infecciones de transmisión sexual (ITS). Una serie de evidencias ha demostrado que la complejidad de la transmisión sexual de patógenos virales requiere de la identificación de compuestos capaces de bloquear los eventos tempranos del ciclo de infección viral. En este manuscrito hacemos una revisión exhaustiva de las diferentes estrategias que se han estudiado o se están considerando para prevenir ITS mediante el uso de microbicidas, haciendo particular énfasis en aquellos con el potencial de bloquear la infección por el HIV. También se revisa el proceso complejo de evaluación preclínica que se requiere para llegar a estudios en humanos y se concluye con un breve análisis de las estrategias que podrían formar parte del futuro inmediato en la investigación de microbicidas
Microbicides are a new tool, still under investigation, which could help prevent infection by the human immunodeficiency virus (HIV) and other sexually transmitted infections (STIs). Increasing evidence shows that the complexity of sexual transmission of viral pathogens requires the identification of compounds able to block the early events during the cycle of viral infection. In this manuscript we provide a comprehensive review of the different microbicide strategies that have been studied or are currently being considered for STI prevention, particularly emphasizing those having the potential to block HIV infection. The manuscript also reviews the complex process that is required to conduct future clinical studies in humans and concludes with a brief discussion of the strategies that could be part of the immediate future in microbicide research
Subject(s)
Sexually Transmitted Diseases/prevention & control , Anti-HIV Agents/analysis , Papillomavirus Vaccines/analysis , Antiviral Agents/therapeutic use , Sexually Transmitted Diseases/diagnosis , Sexually Transmitted Diseases/therapy , Herpesvirus 2, Human/drug effects , Anti-Infective Agents/therapeutic useABSTRACT
As reações falso-positivas em testes de ELISA(Enzima Linked Immuno Sorbent Assay) podem acontecer. O presente trabalho demonstra a existência de reações cruzadas no teste de ELISA anti-HIV em 33 pacientes de 0 - 15 anos com diagnóstico de calazar. Foram observados 5 casos positivos para o teste de ELISA anti-HIV na primeira reação e em 4 (12,12%)houve a permanência da positividade na segunda reação sorológica. Estes pacientes positivos apresentaram Western Blot anti-HIV negativos. Devido o estigma da infecção pelo HIV, fica imperativo, em zonas endêmicas de Leishmaniose Visceral Americana, nos pacientes que tenham apresentado ELISA anti-HIV positivo, a realização de outro teste comprobatório do HIV( Western Blot)