Antimicrobial activity of some substituted triazoloquinazolines

Abstract

Fifteen substituted 1,2,4-triazolo[4,3-c]quinazolines were tested for antibacterial and antifungal effects. The most effective derivatives had the triazoloquinazoline skeleton substituted with the pharmacologically active chromophores--morpholine, chlorine and nitro group. The broadest antimicrobial activity was found with 5-morpholin-4-yl-3-(5-nitrothien-2-yl)[1,2,4]triazolo[4,3-c]quinazoline in concentration of 10 mg/L for B. subtilis, 50 mg/L for S. aureus and 100 mg/L for C. tropicalis. The highest tested concentration of derivative caused 83% growth inhibition of R. nigricans.

Synthesis of New 2-Thio-[1,2,4]triazolo[1,5-c]quinazoline Derivatives and Its Antimicrobial Activity

“…Triazoloquinazoline derivatives were of considerable interest due to their prominent biological properties. Recently, fifteen substituted [1,2,4]triazolo [4,3-c]quinazolines were tested for antibacterial and antifungal effects. As a result it was established that 9-chloro-5-morpholin-4-yl-3-(5-nitrothien-2-yl)- [1,2,4]triazolo [4,3-c]quinazoline A was the most effective compound, which has caused growth inhibition of Bacillus subtilis, Staphylococcus aureus, Candida tropicalis and Rickettsia nigricans.…”

“…Recently, fifteen substituted [1,2,4]triazolo [4,3-c]quinazolines were tested for antibacterial and antifungal effects. As a result it was established that 9-chloro-5-morpholin-4-yl-3-(5-nitrothien-2-yl)- [1,2,4]triazolo [4,3-c]quinazoline A was the most effective compound, which has caused growth inhibition of Bacillus subtilis, Staphylococcus aureus, Candida tropicalis and Rickettsia nigricans. 1) Two novel series of imidazo[2,1:5,1]-1,2,4-triazolo [4,3-c]quinazoline bearing 5-thioxo-1,2,4-triazoles and 4-oxothiazolidines were evaluated for antibacterial activity against representative Gram-positive and Gram-negative microorganisms.…”

Quinazoline pharmacophore in therapeutic medicine

“…In addition, the substitution on the pyrimidine ring shows more of an antimalarial activity variation of a quinazoline derivative (Khan et al, 2014). Triazolofused quinazoline 31 with morpholinyl in 2-position and chloro on 6-position was the most potent antimicrobial scaffold among the series synthesized by Jantova et al, (2005). Presence of electron donating diamine at 4-position increased the anti-inflammatory efficacy of 32 (Lin et al, 2010).…”

Synthesis and modification of 2-[8-R1-9-R2-10-R3-3-R-2-oxo-2H-[1,2,4]triazino[2,3-c]quinazoline-6-yl)thio]acetic acids aimed at searching effective substances with the antibacterial and antifungal activity

“…[3]. Some recent publications are devoted to the search of chemotherapeutics among condensed quinazolines, in particular benzimidazo [1,2-c]-, benzthiadiazolimidazo [1,2-c]-, triazolo [1,5-c]-, imidazo, [1,2,4]triazolo [4,3-c]-, triazino [2,3-c]quinazolines [1,2,4,5,7,8,10,[13][14][15][16][17][18]. Highly effective antimicrobial, antifungal, anticancer agents have been found among the compounds mentioned.…”