Design, synthesis, and biological evaluation of novel trifluoromethyl indoles as potent HIV-1 NNRTIs with an improved drug resistance profile

2014 ◽  
Vol 12 (21) ◽  
pp. 3446-3458 ◽  
Author(s):  
Hai-Xia Jiang ◽  
Dao-Min Zhuang ◽  
Ying Huang ◽  
Xing-Xin Cao ◽  
Jian-Hua Yao ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Resistance Profile ◽  
Drug Resistance Profile ◽  
Synthesis And Biological Evaluation ◽  
Anti Hiv ◽  
Hiv 1

A novel series of trifluoromethyl indoles have been designed, synthesized and evaluated for anti-HIV-1 activities.

Design, Synthesis, and Biological Evaluation of 1-(thiophen-2-yl)-9H-pyrido[3,4-b]indole Derivatives as Anti-HIV-1 Agents

2014 ◽  
Vol 85 (6) ◽  
pp. 722-728 ◽  
Author(s):  
Penta Ashok ◽  
Cui-Lin Lu ◽  
Subhash Chander ◽  
Yong-Tang Zheng ◽  
Sankarnarayanan Murugesan
Keyword(s):  
Biological Evaluation ◽  
Indole Derivatives ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Anti Hiv ◽  
Hiv 1

Design, Synthesis, and Biological Evaluation of Novel 2-(Pyridin-3-yloxy)acetamide Derivatives as Potential Anti-HIV-1 Agents

2015 ◽  
Vol 87 (2) ◽  
pp. 283-289 ◽  
Author(s):  
Boshi Huang ◽  
Xiao Li ◽  
Peng Zhan ◽  
Erik De Clercq ◽  
Dirk Daelemans ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Anti Hiv ◽  
Hiv 1

Design, Synthesis, and Biological Evaluation of Novel Benzoyl Diarylamine/ether Derivatives as Potential Anti-HIV-1 Agents

2015 ◽  
Vol 86 (3) ◽  
pp. 333-343
Author(s):  
Lingzi Zhang ◽  
Jian Guo ◽  
Xin Liu ◽  
Huiqing Liu ◽  
Erik De Clercq ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Anti Hiv ◽  
Hiv 1

Synthesis and Biological Evaluation of 8-Hydroxyquinoline-hydrazones for Anti-HIV-1 and Anticancer Potential

2018 ◽  
Vol 3 (38) ◽  
pp. 10727-10731 ◽  
Author(s):  
Purvi Shah ◽  
Leila F. Abadi ◽  
Shraddha Gaikwad ◽  
Dasharath Chaudhari ◽  
Varun Kushwah ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Synthesis And Biological Evaluation ◽  
Anti Hiv ◽  
Hiv 1

scholarly journals Design, synthesis and biological evaluation of novel fungicides for the management of Fusarium DieBack disease

2019 ◽  
Vol 62 (3) ◽  
Author(s):  
Israel Bonilla Landa ◽  
Osvaldo León De la Cruz ◽  
Diana Sánchez Rangel ◽  
Randy Ortiz Castro ◽  
Benjamin Rodriguez Haas ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Antifungal Activity ◽  
Fusarium Solani ◽  
Antifungal Agents ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Dieback Disease ◽  
Synthetic Chemist ◽  
Fusarium Dieback ◽  
Synthesis And Biological Evaluation

Abstract. Fusarium Dieback, a new and lethal insect-vectored disease can host over 300 tree species including the avocado trees. This problem has recently attracted the attention of synthetic chemist not only to develop new triazol antifungal agents but also due to severe drug resistance to “classic” triazol antifungal agents. Here, a series of novel antifungal triazoles with a p-trifluoromethylphenyl moiety were synthesized and characterized by spectroscopic and spectrometric methods. Most of the target compounds synthesized showed from modest to good inhibitory activity and less phytotoxicity in comparison with the commercially available propiconazol; in particular, compounds 7 and 13 were active against both Fusarium solani and Fusarium euwallaceae. The results showed that compounds 7, 13, and 4 have great potential to be developed as new antifungal agents because of both good antifungal activity and low phytotoxicity. SAR showed that free alcohols and not O-protected compounds significantly influence the activity. Hence, a-methyl-a-1,2,4-triazole emerged as novel compound to develop new ketone-triazole-type antifungal agents for the management of Fusarium Dieback disease Resumen. Fusarium Dieback es una nueva enfermedad letal transmitida por insectos que actúan como vectores y puede atacar a más de 300 especies de árboles, incluidos los árboles de aguacate. Recientemente, este problema ha atraído la atención de los químicos sintéticos para desarrollar nuevos agentes antifúngicos triazólicos debido a la resistencia severa que desarrollan los insectos a los agentes antifúngicos triazólicos "clásicos". Durante este trabajo, se sintetizaron nuevos triazoles antifúngicos que contienen un grupo p-trifluorometilfenilo y se caracterizaron por métodos espectroscópicos y espectrométricos. La mayoría de los compuestos diana sintetizados mostraron una actividad inhibidora de modesta a buena y menos fitotoxicidad en comparación con el propiconazol que es comercialmente disponible; en particular, los compuestos 7 y 13 mostraron ser activos contra Fusarium solani y Fusarium euwallaceae. Los resultados mostraron que los compuestos 7, 13 y 4 tienen un gran potencial para desarrollarse como nuevos agentes antifúngicos debido a la buena actividad antifúngica y su baja fitotoxicidad. SAR mostró que los alcoholes libres y no los compuestos O-protegidos influyen significativamente en la actividad. Por lo tanto, el α-metil-α-1,2,4-triazol surgió como un nuevo compuesto líder para desarrollar nuevos agentes antifúngicos tipo cetona-triazol para el tratamiento de la enfermedad Fusarium Dieback.

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