Unknown

Dataset Information

0

Synthesis and antimicrobial activity of some novel 1,2-dihydro-[1,2,4]triazolo[1,5-a]pyrimidines bearing amino acid moiety.

ABSTRACT: A new series of [1,2,4]-triazole bearing amino acid derivatives 2a-d-9a-d were synthesized under green chemistry conditions via multicomponent reaction using lemon juice as an acidic catalyst. The obtained compounds were characterized by different spectral and elemental analyses. The obtained candidates showed promising antibacterial activity against some standard bacteria and multidrug resistant (MDR) clinical isolates. In contrast to the reference drugs cephalothin and chloramphenicol, the tested compounds showed substantial better MIC values towards the tested MDR strains. The most active compounds 3c, 8a and 9d against MDR bacteria were tested for MBC and MIC index, the results indicted the bacteriostatic activity of these compounds. The most active compounds 2c, 2d, 3c, 8a, 8b, 9a, 9b, 9c and 9d showed a high selectivity index towards antimicrobial activity against K. pneumoniae and MRSA1 compared to mammalian cells, suggesting a good safety profile.

SUBMITTER: Mohamed MAA 

PROVIDER: S-EPMC8693849 | biostudies-literature | 2021 Jan

REPOSITORIES: biostudies-literature

Json Xml
altmetric image

Publications

Synthesis and antimicrobial activity of some novel 1,2-dihydro-[1,2,4]triazolo[1,5-<i>a</i>]pyrimidines bearing amino acid moiety.

Mohamed Mounir A A MAA   Bekhit Adnan A AA   Abd Allah Omyma A OA   Kadry Asmaa M AM   Ibrahim Tamer M TM   Bekhit Salma A SA   Amagase Kikuko K   El-Saghier Ahmed M M AMM  

RSC advances 20210113 5

A new series of [1,2,4]-triazole bearing amino acid derivatives 2a-d-9a-d were synthesized under green chemistry conditions <i>via</i> multicomponent reaction using lemon juice as an acidic catalyst. The obtained compounds were characterized by different spectral and elemental analyses. The obtained candidates showed promising antibacterial activity against some standard bacteria and multidrug resistant (MDR) clinical isolates. In contrast to the reference drugs cephalothin and chloramphenicol,  ...[more]

Similar Datasets

Unknown 1,2,4-Triazolo[1,5-a]pyrimidines in drug design.
| S-EPMC6394845 | biostudies-literature
Unknown Synthesis and evaluation of 1,2,4-triazolo[1,5-a]pyrimidines as antibacterial agents against Enterococcus faecium.
| S-EPMC4633020 | biostudies-literature
Unknown Design, synthesis and evaluation of photoactivatable derivatives of microtubule (MT)-active [1,2,4]triazolo[1,5-a]pyrimidines.
| S-EPMC5993642 | biostudies-literature
Unknown Ethyl 2-(2-amino-5-methyl-1,2,4-triazolo[1,5-a]pyrimidin-7-yl)acetate.
| S-EPMC3254570 | biostudies-literature
Unknown Design, Synthesis, and Antifungal Activity of Novel 1,2,4-Triazolo[4,3-c]trifluoromethylpyrimidine Derivatives Bearing the Thioether Moiety
| S-EPMC9344801 | biostudies-literature
Unknown 7-Dimethyl-amino-2-phenyl-1,2,4-triazolo[1,5-a][1,3,5]triazin-5-amine methanol solvate.
| S-EPMC2959306 | biostudies-literature
Unknown New protocols for the synthesis of 5-amino-7-(4-phenyl)-4,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidine-6-carboxylate esters using an efficient additive.
| S-EPMC7751900 | biostudies-literature
Unknown 5-Chloro-2-methyl-sulfonyl-1,2,4-triazolo[1,5-a]quinazoline.
| S-EPMC3379383 | biostudies-other
Unknown 2-Phenyl-7-(4-pyridyl-methyl-amino)-1,2,4-triazolo[1,5-a][1,3,5]triazin-5(4H)-one.
| S-EPMC3050179 | biostudies-literature
Unknown Ethyl 5-chloro-methyl-2-methyl-sulfanyl-7-phenyl-4,7-dihydro-1,2,4-triazolo[1,5-a]pyrimidine-6-carboxyl-ate.
| S-EPMC2915003 | biostudies-literature