4021-23-2Relevant academic research and scientific papers
Synthesis, antimicrobial and chitinase inhibitory activities of 3-amidocoumarins
Butcher, R. J.,Katiyar, Diksha,Sharma, Rajesh Kumar,Singh, Vineeta,Tiwari, Neha
, (2020/03/11)
A series of 3-amidocoumarins has been synthesized and tested in vitro for their anitimicrobial and chitinase inhibitory activities. Among these, compounds 5k, 5l, 8b–8d, 8f and 8g exhibited good antibacterial activity with MIC values in the range of 6.25–25 μg/mL against some of the tested strains while compounds 5l, 8b, 8c and 8f showed good activity against at least one or two fungal strains. Some of the assayed compounds 5d, 5k, 5l, 8b and 8c displayed significant chitinase inhibitory activity with IC50 values in the range of 3.74–5.6 μM. Among them, 5l proved to be potent chitinase inhibitor with IC50 value of 3.74 μM. To better understand the enzyme-inhibitor interactions molecular docking study of all the synthesized compounds was carried out on Aspergillus fumigatus chitinase 1W9U. The compound 5l showed high binding affinity with the receptor with binding energy value of ?8.44 Kcal/mol. This study also provides structure activity relationship (SAR) of synthesized compounds.
Design, synthesis and antifungal activity evaluation of coumarin-3-carboxamide derivatives
Yu, Xiang,Teng, Peng,Zhang, Ya-Ling,Xu, Zhao-Jun,Zhang, Ming-Zhi,Zhang, Wei-Hua
, p. 387 - 395 (2018/04/19)
A series of coumarin-3-carboxamides/hydrazides have been designed and synthesized, all the target compounds were evaluated in vitro for their antifungal activity against Botrytis cinerea, Alternaria solani, Gibberella zeae, Rhizoctorzia solani, Cucumber anthrax and Alternaria leaf spot, some of the designed compounds 4a-4g exhibited potential activity in the primary assays, this highlighted by the compounds 4a, 4d, 4e and 4f, EC50 values of which against Rhizoctorzia solani were as low as 1.80 μg/mL, 2.50 μg/mL, 2.25 μg/mL and 2.10 μg/mL, respectively, exhibiting more effective control with that of the positive control than Boscalid. Furthermore, compounds 4a and 4e represented equivalent antifungal activity with Boscalid against Botrytis cinerea.
An efficient three-component synthesis of coumarin-3-carbamides by use of Ni-NiO nanoparticles as magnetically separable catalyst
Sepay, Nayim,Guha, Chayan,Kool, Arpan,Mallik, Asok K.
, p. 70718 - 70725 (2015/09/08)
An efficient and ecofriendly synthesis of coumarin-3-carbamides, a class of compounds known for their remarkable biological activities and fluorescent properties, has been developed by a three-component reaction of 2-hydroxybenzaldehydes, aliphatic primar
One-step synthesis of chromene-3-carboxamide, bis-chromene, chromeno[3,4-c]pyridine and bischromeno[3,4-c]pyridine derivatives for antimicrobial evaluation
Helal, Mohamed H.,El-Hag Ali, Gameel A. M.,Ali, Ahmed A.,Ammar, Yousry A.
experimental part, p. 465 - 469 (2011/01/12)
Cyanoacetamide derivatives were reacted with salicylaldehyde under different conditions afforded chromenes and coumarin derivatives respectively. A number of chromeno[3,4-c]pyridine derivatives were prepared from the reaction of N-cyclohexyl-2-imino-2H-chromene-3-carboxamide with malononitrile and/or cynaothiocatemaide. Bischromeno[3,4-c]pyridine derivatives were prepared from the reaction of N,N'-(ethane-1,2-diyl)bis(2-imino-2Hchromene-3-carboxamide) with malononitrile and/or N-alkyl-2-cyanoacetamide derivative with 2-iminochroemen derivative, respectively. Some of these compounds were screened for their antimicrobial activities.
