Synthesis and Biological Evaluation of Some New Fused Quinazoline Derivatives

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

“…3) Furthermore, [1,2,4]triazolo [1,5-c]quinazolin-2-thiones D substituted at C(5) with (sulfo)alkyl group has been found to exhibit moderate antibacterial activity. [4][5][6][7] Thus, considering the fact of antimicrobial agents existence among 1,2,4-triazoloquinazolines, we were aimed to provide simple synthetic protocols of obtaining novel 2-thio- [1,2,4]triazolo [1,5-c]quinazoline derivatives in order to evaluate their antimicrobial and bioluminescence properties.…”

“…2) A certain antibacterial effect against Bacillus subtilis was manifested by N-aryl- (4- [1,2,4]triazolo [1,5-c]quinazolin-2-yl-thiazol-2-yl)acetamides (C). 3) Furthermore, [1,2,4]triazolo [1,5-c]quinazolin-2-thiones D substituted at C(5) with (sulfo)alkyl group has been found to exhibit moderate antibacterial 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.…”

Synthesis of Novel a-Amino Acids Bearing 1,2,4-triazinone and Steroidal Moieties as Enzymetic Affect (Cellobiase Activity) Part I

“…The released reducing sugar was estimated calorimetrically at 540 nm (Ibrahim et al, 1997;Abdel-Rahman, Morsy, Allimon & Abd El-Monem, 1999;Ibrahim et al, 2009) Compounds 6a and 6b both showed a higher amount of activity over the compounds when compared against the other tested fungi, thus, the introducing of fluorine atoms and / or sulfa-drug moiety resulted in high order of activity in comparison with the corresponding α-amino acids. Additionally, the presence of fluorine substituted α-amino acids bearing 1,2,4-trizine and steroidal moieties led to increases the net-electronegativity, which improve the dielectric constant and enhances the hydrophobic properties.…”