scholarly journals Studies on the syntheses of heterocyclic compounds. DCCIX. A synthetic approach to kesselringine.

1977 ◽  
Vol 25 (5) ◽  
pp. 922-925 ◽  
Author(s):  
TETSUJI KAMETANI ◽  
YOSHINARI SATOH ◽  
KEIICHIRO FUKUMOTO
Keyword(s):  
Heterocyclic Compounds ◽  
Synthetic Approach

scholarly journals Polyhalonitrobutadienes as Versatile Building Blocks for the Biotargeted Synthesis of Substituted N-Heterocyclic Compounds

Molecules ◽  
2020 ◽  
Vol 25 (12) ◽  
pp. 2863 ◽  
Author(s):  
Viktor A. Zapol’skii ◽  
Ursula Bilitewski ◽  
Sören R. Kupiec ◽  
Isabell Ramming ◽  
Dieter E. Kaufmann
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Heterocyclic Compounds ◽  
Nitrogen Heterocycles ◽  
Building Blocks ◽  
Antibacterial Activities ◽  
Synthetic Approach ◽  
Selective Synthesis ◽  
Ic50 Values ◽  
Thiophene Derivatives

Substituted nitrogen heterocycles are structural key units in many important pharmaceuticals. A new synthetic approach towards heterocyclic compounds displaying antibacterial activity against Staphylococcus aureus or cytotoxic activity has been developed. The selective synthesis of a series of 64 new N-heterocycles from the three nitrobutadienes 2-nitroperchloro-1,3-butadiene, 4-bromotetrachloro-2-nitro-1,3-butadiene and (Z)-1,1,4-trichloro-2,4-dinitrobuta-1,3-diene proved feasible. Their reactions with N-, O- and S-nucleophiles provide rapid access to push-pull substituted benzoxazolines, benzimidazolines, imidazolidines, thiazolidinones, pyrazoles, pyrimidines, pyridopyrimidines, benzoquinolines, isothiazoles, dihydroisoxazoles, and thiophenes with unique substitution patterns. Antibacterial activities of 64 synthesized compounds were examined. Additionally, seven compounds (thiazolidinone, nitropyrimidine, indole, pyridopyrimidine, and thiophene derivatives) exhibited a significant cytotoxicity with IC50-values from 1.05 to 20.1 µM. In conclusion, it was demonstrated that polyhalonitrobutadienes have an interesting potential as structural backbones for a variety of highly functionalized, pharmaceutically active heterocycles.

scholarly journals Review on Synthesis of Thiazole Derivatives from α-Halo- ketones and Thiourea or N-Substituted Thiourea

2020 ◽  
pp. 221-225
Author(s):  
Sagar Ramdas Shrimandilkar
Keyword(s):  
Antifungal Activity ◽  
Carbonyl Compounds ◽  
Heterocyclic Compounds ◽  
Scientific Literature ◽  
Research Work ◽  
Synthetic Approach ◽  
Important Class ◽  
Thiazole Derivatives ◽  
Thiourea Derivatives ◽  
Methods Of Synthesis

Thiazole represents important class of heterocyclic compounds. Thiazole and its derivatives have been reported to possess antitubercular, antibacterial, anti-inflammatory, anticancer, antifungal activity. Several methods of synthesis of thiazole derivatives have been reported, but most widely used synthetic approach to obtained thiazole derivatives is Hantzsch process. It involved synthesis of thiazole derivative from ?-halo-carbonyl compounds and thiourea or thiourea derivatives. This review mainly focuses on the research work reported in the scientific literature on the different procedures of synthesis of 2-amino thiazole and their derivatives.

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