scholarly journals Design, synthesis and evaluation of anti-inflammatory, analgesic and antibacterial activity of 2, 4, 6-trisubstituted quinazoline derivatives

2018 ◽  
Vol 29 (2) ◽  
pp. 97-102
Author(s):  
Nivrati Jain ◽  
Harshita Jain ◽  
Ashish Jain ◽  
Veerasamy Ravichandran ◽  
Prateek Jain

Abstract We described here the synthesis and biological evaluation of a series of 2, 4, 6-trisubstituted quinazoline derivatives as potential anti-inflammatory, analgesic and antibacterial agents. The synthesized compounds were characterized by FTIR, 1H NMR and mass spectroscopy analysis. We found that the compounds 6b, 6e, 6g, 6h and 6j showed better anti-inflammatory activity than indomethacin. Compounds 6b, 6e, 6h, 6j and 6l were found to exhibit appreciable analgesic activity, and 6b, 6g and 6k showed good antibacterial activity against Gram (+) bacteria: B. subtilis, S. aureus, S. epidermis, and Gram (-) bacteria: E. coli, P. aeruginosa and K. pneumoniae. Compound 6b showed overall better anti-inflammatory, analgesic and antibacterial activity among the synthesized compounds. The results of the present study could be helpful for the designing of effective anti-inflammatory, analgesic and antibacterial agents.

2015 ◽  
Vol 13 (28) ◽  
pp. 7720-7735 ◽  
Author(s):  
Takeshi Nakaya ◽  
Akira Matsuda ◽  
Satoshi Ichikawa

Caprazamycin analogues, which were designed and synthesized via an aza-Prins–Ritter reaction, exhibit a good MraY and antibacterial activity without cytotoxicity against human cells.


Author(s):  
Asma D. Ambekari ◽  
Shrinivas K. Mohite

Series of novel substituted Synthesis of N-{[5-(substituted)-1,3,4-oxadiazole-2-yl] carbamothioyl} derivatives containing 1,3,4-oxadiazole moiety were synthesized by microwave as a green chemistry method and conventional method by using pyridine 3- carboxylic acid as a starting material. The structures of the synthesized compounds were characterized by physicochemical data, IR, Mass spectra and 1HNMR. All the newly synthesized compound screened for their antimicrobial and In-vivo and In-vitro Anti-inflammatory studies. Anti-inflammatory studies revealed that compound 4f showed significant in-vivo and in-vitro anti-inflammatory activity as well potent antimicrobial activity.


2019 ◽  
Vol 31 (10) ◽  
pp. 2389-2393
Author(s):  
Sravanthi Siliveri ◽  
Harinadha Babu Vamaraju ◽  
Shivaraj

In the present work, novel pyrazole fused dihydrofurans synthesized via a chronological addition of N-chloro succinimide and base piperidine to pyrano[3,2-c]pyrazole carbonitrile derivatives in methanol medium. Oxidative difunctionalization was done with the reagent N-chloro succinimide by the addition of both chlorine and alkoxy groups crosswise the chromene double bond. The addition of base results in the construction of dihydrofuran derivatives by ring contraction. The structures of newly synthesized compounds were characterized on the basis of physical and spectral data. Synthesized compounds were evaluated for antibacterial and anti-inflammatory activities. All the compounds exhibited significant antibacterial activity against all the four strains of bacteria and their MICs ranged between 1.56 and 12.55 μg/mL. In anti-inflammatory screening, among all the tested compounds, compounds 7, 8, 9, 11, 12, 13, 14, 16, 17 and 18 exhibited significant protection against the edema formation at a concentration of 100 mg/kg.


2019 ◽  
Vol 28 (6) ◽  
pp. 849-856 ◽  
Author(s):  
Chetan Kumar ◽  
Anil Kumar ◽  
Yedukondalu Nalli ◽  
Waseem I. Lone ◽  
Naresh K. Satti ◽  
...  

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