Facile Synthesis of Azaarene-Substituted Hydroxycoumarins Possessing High Biological Activities via Three-Component C(sp3)–H Functionalization

2016 ◽  
Vol 18 (9) ◽  
pp. 604-610 ◽  
Author(s):  
Haoxun Dong ◽  
Lubin Xu ◽  
Shuai-Shuai Li ◽  
Liang Wang ◽  
Chang-Lun Shao ◽  
...  
2018 ◽  
Vol 42 (21) ◽  
pp. 17533-17537
Author(s):  
Sorour Ramezanpour ◽  
Mohammad Nasim Rezaei ◽  
Aref Vaezghaemi ◽  
Frank Rominger

An innovative strategy for synthesis of a library of complex multi-substituted 1,2,4-triazine-6-ones. These structures are analogues of pyrimidine bases with possible enhanced biological activities.


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.


2021 ◽  
Vol 11 (1) ◽  
pp. 2996-3005

Using a recyclable catalyst, facile synthesis of pyrimidine derivatives (4a-e) is attributed through the one-pot multi-component reaction of 2-amino benzimidazole (1) substituted aromatic aldehydes (2a-e) with malononitrile (3) under ultrasonic irradiations. Synthesized derivatives might help society in getting more active pharmaceutical constituents. In this present work, series of substituted pyrimidine (4a-e) were synthesized and confirmed with different spectra characterization methods. The ZnCr2O4 nano-particles play a vital role in eco-friendly, highly efficient, recyclable heterogeneous nanocatalyst. Furthermore, synthesized pyrimidine derivatives showed significant biological activities. Advantages of this handy route are less reaction time, simple isolation, and highly yielded products.


2018 ◽  
Vol 14 (5) ◽  
pp. 451-459 ◽  
Author(s):  
Muhammad Saleem ◽  
Muhammad Rafiq ◽  
Yeon Ki Jeong ◽  
Dae Won Cho ◽  
Chong-Hyeak Kim ◽  
...  

Author(s):  
Priyanka Bhatt ◽  
S. Deepthi ◽  
Ch. Ravi Shankar Kumar ◽  
Anjali Jha

Objective: A facile synthesis of some novel Schiff base derivatives of 2-substituted-5-amino-thiadiazoles along with their Ni (II), Cu (II), and Pd (II) complexes were achieved by sonication and the conventional method. In addition to establish the structure by DFT studies and to explore antimicrobial and anticancer activities of these novel compounds.Methods: The precursor 2-substituted-5-amino-thiadiazoles (T1-T3), target ligands and their metal complexes were synthesized by ultra-sonication and conventional means. The isolated products were thoroughly characterized by physical and spectroscopic techniques including 1H-NMR, [13]C-NMR and IR spectroscopy. All characterized compounds were screened for antimicrobial activities using well diffusion method, and MTT assay was performed for cytotoxicity.Results: All novel compounds were synthesized by a green route i.e. ultra sonication and a noticeable improvement in yield with shorter reaction time than the conventional method were observed. The octahedral geometry was proposed for Ni (II)/Cu (II) complexes whereas square planar for Pd (II) complexes on the basis of the spectral techniques which were supported by DFT analysis by Gaussian03. On the analysis of antimicrobial activities, the compound T7 and T10 showed maximum antibacterial and antifungal activities respectively. However, compounds T25, T37, T31 found to be a potential cytotoxic compound with IC50 value 0.469, 0.865 and 1.131 μM respectively.Conclusion: Analysis of synthetic protocol, it could be concluded that ultra-sonication is the better method to synthesize these potential biological active moiety. On the whole Cu (II) and Ni (II) complexes showed promising activity towards all microorganisms while Pd (II) complex emerged an excellent moiety in carcinoma cell line.


2017 ◽  
Vol 79 (5) ◽  
Author(s):  
Lina Mardiana ◽  
Bayu Ardiansah ◽  
Ridla Bakri ◽  
Antonius Herry Cahyana ◽  
Yulia Anita ◽  
...  

A simple preparation of sodium impregnated on activated chicken eggshells (Na-ACE) as a solid base material for substituted chalcones synthesis is presented. After characterization using FTIR, XRD, SEM, EDS and total basicity, the catalyst was applied in Aldol condensation to produce corresponding chalcones 3a-3j. Confirmation of products structure has been done by FTIR, UV-Vis and MS instruments. Reaction can be carried out in relative short time with ethanol as the best solvent and gave the highest yield of 95 %. This research presented a facile synthesis of chalcone derivatives, the prominent class of organic compounds with interesting biological activities. 


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