Pyrrolo[2,3-d]pyrimidine derivatives in the synthesis of a novel heterocyclic system 2a,5a,7-triazaacenaphthylene

Muzychka, L. V.; Yaremchuk, I. O.; Verves, E. V.; Смолий, О. Б.

doi:10.1007/s10593-019-02471-z

Cited by 3 publications

(2 citation statements)

References 12 publications

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“…Alkaline hydrolysis of esters 3a-e gave substituted 1-alkyl-4-oxo-1,4-dihydropyrido[1,2-a]pyrrolo [2,3-d] pyrimidine-2-carboxylic acids 4a-e. It should be noted that the examples of synthesis of fused pyrrole derivatives were previously described in [26,27].…”

Section: Resultsmentioning

confidence: 99%

Synthesis and antibiofilm activity of novel 1,4-dihydropyrido[1,2-a]pyrrolo[2,3-d]pyrimidine-2-carboxamides

Muzychka,

Humeniuk,

Boiko

et al. 2024

Biopolym. Cell

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Synthesis of novel alkyl-substituted 4-oxo-1,4-dihydropyrido [1,2-a]pyrrolo [2,3-d]pyrimidine-2-carboxamides and evaluation of their antibiofilm activity in vitro. Methods. Organic synthesis, analytical and spectral methods, broth microilution method, biofilm formation on abiotic surface. Results. A simple and efficient method for the synthesis of new 1,4-dihydropyrido[1,2-a]pyrrolo[2,3-d]pyrimidine-2-carboxylic acid derivatives was developed. The results of antibiofilm activity screening showed that among the synthesized alkyl-substituted 1,4-dihydropyrido[1,2-a]pyrrolo[2,3-d]pyrimidine-2-carboxamides there are the compounds capable of disrupting the formation of biofilm of methicillin-resistant strain S. aureus 222, E. coli 311 and P. aeruginosa 449. Compound 6g is active against biofilms of E. coli 311, biomass decreases by 91.2 %, and against S. aureus 222 (reduction by 54.0 %). Compound 6d is active against biofilms of P. aeruginosa 449 and S. aureus 222 (reduction by 78.7 % and 50.2 %, respectively). Conclusions. A series of novel substituted 1-alkyl-4-oxo-1,4dihydropyrido[1,2-a]pyrrolo[2,3-d]pyrimidine-2-carboxamides were synthesized. The acti vity of the synthesized pyrido[1,2-a]pyrrolo [2,3-d]pyrimidines towards the S. aureus 222, E. coli 311 and P. aeruginosa 449 biofilm formation was investigated, and the compounds with pronounced antibiofilm activity were found. K e y w o r d s: pyrido[1,2-a]pyrrolo [2,3-d]pyrimidines, pyrido[1,2-a]pyrimidine-3-carbaldehydes, synthesis, antibiofilm activity.

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Section: Resultsmentioning

confidence: 99%

Synthesis and antibiofilm activity of novel 1,4-dihydropyrido[1,2-a]pyrrolo[2,3-d]pyrimidine-2-carboxamides

Muzychka,

Humeniuk,

Boiko

et al. 2024

Biopolym. Cell

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“…The synthesis of the target 5,6-dihydro-4H-1-deazapyrimido[1,2,3-cd]purine-7-ium salts 3, 6 was performed according to Scheme 1. For the synthesis of new derivatives of 1deazapyrimido[1,2,3-cd]purine, we used an approach based on the reaction of intramolecular cyclization of 7-substituted pyrrolo [2,3-d]pyrimidines [3]. The bromination of methyl 7-allyl-4- The ability of 1-deazapyrimido[1,2,3-cd]purine derivatives in subinhibitory concentrations 10 μg/mL and 50 μg/mL to prevent bacteria from biofilm formation has been tested on polystyrene plates by gentianvioletum sorption on biofilm structures, followed by its desorption with organic solvent [4].…”

Section: Resultsmentioning

confidence: 99%

Synthesis and antibiofilm activity of substituted 1-deazapyrimido[1,2,3-cd]purinium salts

2021

Chemical Technology and Engineering. Proceedings

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Synthesis and Acetylcholinesterase Inhibitory Activity of Novel Trilaciclib Analogs

Muzychka,

Smolii

2024

Chemistry & Biodiversity

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Trilaciclib is a CDK4/6 inhibitor, used to treat the bone marrow damage in chemotherapy patients. A series of thirteen novel structural trilaciclib analogs was obtained to evaluate their activity against acetylcholinesterase. An effective method for the synthesis of 4,7‐substituted 8,9‐dihydropyrazino[1',2':1,5]pyrrolo[2,3‐d]pyrimidine derivatives from a new methyl 4‐chloro‐7H‐pyrrolo[2,3‐d]pyrimidine‐6‐carboxylate was developed. Most of the synthesized pyrazino[1',2':1,5]pyrrolo[2,3‐d]pyrimidine derivatives inhibited acetylcholinesterase in the micromolar range. The obtained data can be used for designing more potent acetylcholinesterase inhibitors with the pyrazino[1',2':1,5]pyrrolo[2,3‐d]pyrimidine scaffold.

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Pyrrolo[2,3-d]pyrimidine derivatives in the synthesis of a novel heterocyclic system 2a,5a,7-triazaacenaphthylene

Cited by 3 publications

References 12 publications

Synthesis and antibiofilm activity of novel 1,4-dihydropyrido[1,2-a]pyrrolo[2,3-d]pyrimidine-2-carboxamides

Synthesis and antibiofilm activity of novel 1,4-dihydropyrido[1,2-a]pyrrolo[2,3-d]pyrimidine-2-carboxamides

Synthesis and antibiofilm activity of substituted 1-deazapyrimido[1,2,3-cd]purinium salts

Synthesis and Acetylcholinesterase Inhibitory Activity of Novel Trilaciclib Analogs

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