scholarly journals Design, synthesis and evaluation of hydrazine and acyl hydrazone derivatives of 5-pyrrolidin-2-one as antifungal agents

2020 ◽  
Vol 30 (13) ◽  
pp. 127220
Author(s):  
Anca-Elena Dascalu ◽  
Alina Ghinet ◽  
Emmanuelle Lipka ◽  
Christophe Furman ◽  
Benoît Rigo ◽  
...  
Keyword(s):  
Antifungal Agents ◽  
Design Synthesis ◽  
Acyl Hydrazone ◽  
Derivatives Of

scholarly journals Antifungal Activity of New Eugenol-Benzoxazole Hybrids against Candida spp.

2017 ◽  
Vol 2017 ◽  
pp. 1-8 ◽  
Author(s):  
Larissa Incerti Santos de Carvalho ◽  
Dalila Junqueira Alvarenga ◽  
Letícia Cruz Ferreira do Carmo ◽  
Lucas Gomes de Oliveira ◽  
Naiara Chaves Silva ◽  
...  
Keyword(s):  
Antifungal Agents ◽  
Biological Activities ◽  
Antimicrobial Activities ◽  
Candida Spp ◽  
Design Synthesis ◽  
Human Blood Cells ◽  
Wide Range ◽  
Synthetic Sequence ◽  
Derivatives Of ◽  
Aromatic Nitration

Eugenol is a natural allylphenol responsible for a wide range of biological activities, especially antimicrobial. Benzoxazoles are heterocycles with recognized antimicrobial activities. This paper describes the design, synthesis, and the biological results for benzoxazole type derivatives of eugenol as antifungal agents. The products were obtained in good yields by a four-step synthetic sequence involving aromatic nitration, nitroreduction, amide formation, and cycle condensation. They were evaluated against species of Candida spp. in microdilution assays, and four products (5a, 5b′, 5c, and 5d′) were about five times more active than eugenol against C. albicans and C. glabrata. Two of them (5b′ and 5d′) showed good activity against C. krusei, a species which is naturally resistant to fluconazole. Furthermore, the active products were more selective than eugenol against human blood cells, showing that they are interesting substances for further optimization.

Design, Synthesis and Evaluation of Novel Derivatives of Orotic Acid Amide as Potent Glucokinase Activators

2017 ◽  
Vol 14 (3) ◽  
pp. 252-261 ◽  
Author(s):  
Leilei Zhang ◽  
Shengquan Hu ◽  
Lei Lei ◽  
Yuliang Zhang ◽  
Lijing Zhang ◽  
...  
Keyword(s):  
Orotic Acid ◽  
Acid Amide ◽  
Design Synthesis ◽  
Glucokinase Activators ◽  
Derivatives Of

Design, Synthesis and Biological Evaluation of Novel Aminosaccharide Derivatives of Combretastatin A-4

2013 ◽  
Vol 10 (10) ◽  
pp. 935-941
Author(s):  
Yan Tang ◽  
Zhewei Tu ◽  
Jing Sun ◽  
Xiong Zhu ◽  
Kun Liu ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

Hybridized Quinoline Derivatives as Anticancer Agents: Design, Synthesis, Biological Evaluation and Molecular Docking

2019 ◽  
Vol 19 (4) ◽  
pp. 439-452 ◽  
Author(s):  
Mohamed R. Selim ◽  
Medhat A. Zahran ◽  
Amany Belal ◽  
Moustafa S. Abusaif ◽  
Said A. Shedid ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Anticancer Agents ◽  
Caspase 3 ◽  
Biological Evaluation ◽  
Tubulin Polymerization ◽  
Design Synthesis ◽  
Chemical Structures ◽  
M Phase ◽  
Induced Apoptosis ◽  
Derivatives Of

Objective: Conjugating quinolones with different bioactive pharmacophores to obtain potent anticancer active agents. Methods: Fused pyrazolopyrimidoquinolines 3a-d, Schiff bases 5, 6a-e, two hybridized systems: pyrazolochromenquinoline 7 and pyrazolothiazolidinquinoline 8, different substituted thiazoloquinolines 13-15 and thiazolo[3,2-a]pyridine derivatives 16a-c were synthesized. Their chemical structures were characterized through spectral and elemental analysis, cytotoxic activity on five cancer cell lines, caspase-3 activation, tubulin polymerization inhibition and cell cycle analysis were evaluated. Results: Four compounds 3b, 3d, 8 and 13 showed potent activity than doxorubicin on HCT116 and three compounds 3b, 3d and 8 on HEPG2. These promising derivatives showed increase in the level of caspase-3. The trifloromethylphenyl derivatives of pyrazolopyrimidoquinolines 3b and 3d showed considerable tubulin polymerization inhibitory activity. Both compounds arrested cell cycle at G2/M phase and induced apoptosis. Conclusion: Compounds 3b and 3d can be considered as promising anticancer active agents with 70% of colchicine activity on tubulin polymerization inhibition and represent hopeful leads that deserve further investigation and optimization.

Three Amino Acid Derivatives of Valproic Acid: Design, Synthesis, Theoretical and Experimental Evaluation as Anticancer Agents

2014 ◽  
Vol 14 (7) ◽  
pp. 984-993 ◽  
Author(s):  
Gabriela Luna-Palencia ◽  
Federico Martinez-Ramos ◽  
Ismael Vasquez-Moctezuma ◽  
Manuel Fragoso-Vazquez ◽  
Jessica Mendieta-Wejebe ◽  
...  
Keyword(s):  
Valproic Acid ◽  
Amino Acid ◽  
Anticancer Agents ◽  
Experimental Evaluation ◽  
Amino Acid Derivatives ◽  
Design Synthesis ◽  
Derivatives Of

Azole derivatives of 1,4-benzothiazine as antifungal agents

1998 ◽  
Vol 6 (1) ◽  
pp. 103-108 ◽  
Author(s):  
Renata Fringuelli ◽  
Fausto Schiaffella ◽  
Francesco Bistoni ◽  
Lucia Pitzurra ◽  
Anna Vecchiarelli
Keyword(s):  
Antifungal Agents ◽  
Derivatives Of

Design, synthesis and agricultural evaluation of derivatives of N-Acyl-N-(m-fluoro-benzyl)-6-amino-coumarin

2020 ◽  
pp. 1-7
Author(s):  
Yan Jin ◽  
Yin-hao Ding ◽  
Jing-jing Dong ◽  
Yan Wei ◽  
Shuang-hong Hao ◽  
...  
Keyword(s):  
Design Synthesis ◽  
Derivatives Of

scholarly journals Synthesis, characterization and biological activity of organometallic derivatives of the antimalarial drug mefloquine as new antischistosomal drug candidates

MedChemComm ◽  
2018 ◽  
Vol 9 (11) ◽  
pp. 1905-1909 ◽  
Author(s):  
Faustine d'Orchymont ◽  
Jeannine Hess ◽  
Gordana Panic ◽  
Marta Jakubaszek ◽  
Lea Gemperle ◽  
...  
Keyword(s):  
Biological Activity ◽  
Antimalarial Drug ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Drug Candidates ◽  
Derivatives Of

The design, synthesis, characterization and biological evaluation of new ferrocenyl and ruthenocenyl derivatives of the antimalarial mefloquine is described.

Design, synthesis and evaluation of clinafloxacin triazole hybrids as a new type of antibacterial and antifungal agents

2012 ◽  
Vol 22 (17) ◽  
pp. 5363-5366 ◽  
Author(s):  
Yan Wang ◽  
Guri L.V. Damu ◽  
Jing-Song Lv ◽  
Rong-Xia Geng ◽  
Da-Cheng Yang ◽  
...  
Keyword(s):  
Antifungal Agents ◽  
Design Synthesis ◽  
New Type ◽  
Antibacterial And Antifungal
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