scholarly journals Synthesis and Biological Evaluation of Norcantharidin Derivatives Possessing an Aromatic Amine Moiety as Antifungal Agents

Molecules ◽  
2015 ◽  
Vol 20 (12) ◽  
pp. 21464-21480 ◽  
Author(s):  
Yang Wang ◽  
Wenbo Sun ◽  
Shunqing Zha ◽  
Huan Wang ◽  
Yalin Zhang
2019 ◽  
Vol 62 (3) ◽  
Author(s):  
Israel Bonilla Landa ◽  
Osvaldo León De la Cruz ◽  
Diana Sánchez Rangel ◽  
Randy Ortiz Castro ◽  
Benjamin Rodriguez Haas ◽  
...  

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.


2019 ◽  
Vol 24 (4) ◽  
pp. 1065-1075 ◽  
Author(s):  
Rui Yang ◽  
Wenhao Du ◽  
Huan Yuan ◽  
Tianhong Qin ◽  
Renxiao He ◽  
...  

2015 ◽  
Vol 86 (4) ◽  
pp. 459-465 ◽  
Author(s):  
Pedro Henrique O. Abrão ◽  
Rafael B. Pizi ◽  
Thiago B. de Souza ◽  
Naiara C. Silva ◽  
Antonio M. Fregnan ◽  
...  

2019 ◽  
Vol 4 (3) ◽  
pp. 152-158
Author(s):  
P.C. Burde ◽  
A.M. Rahatgaonkar

3-Cyclopropyl-5-(4-substituted)-1-phenyl-4,5-dihydro-1H-pyrazoles derived from corresponding chalcones were synthesized and evaluated for their biological activities. A convenient synthesis of a library of these compounds in 1-butyl-3-methylimidazolium hexafluorophosphate-water biphasic system at ambient temperature has been accomplished. The ionic liquid, [bmim][PF6] and water which are immiscible, has been easily recycled and reused after separation of the products without any noticeable diminution in its activity.


2014 ◽  
Vol 33 (7) ◽  
pp. 1594-1601 ◽  
Author(s):  
Jakob Kljun ◽  
Antony James Scott ◽  
Tea Lanišnik Rižner ◽  
Jennifer Keiser ◽  
Iztok Turel

2016 ◽  
Vol 71 (5-6) ◽  
pp. 133-140 ◽  
Author(s):  
Asma Mohamed Mahran ◽  
Nasser Abdelhamid Hassan ◽  
Dalia Ahmed A. Osman ◽  
Sherif Shaban Ragab ◽  
Allam Abdelhamid Hassan

Abstract Starting from 6-aryl-5-cyano-2-thiouracil derivative 1a–f, a series of novel thiazolo[3,2-a]pyrimidines 4a–f were synthesized. The mechanism and the regioselectivity of the studied reactions are discussed. In addition, a series of tetrahydro-4-H-pyrimido[2,1-b][1,3]thiazines 7a–e and 2-((ethoxymethyl)thio)-4-aryl-1,6-dihydropyrimidines 9b,c,e were synthesized. The anti-microbial activities of some of the prepared compounds were screened, and the results revealed that compounds 3c and 4c were more active than the standard (Ampicillin) against gram positive bacteria (Pseudomonas aeruginosa). Moreover, compounds 4b,e and 3f were found to be good antifungal agents against the studied fungal strains.


Sign in / Sign up

Export Citation Format

Share Document