A series of hydrazones, azoles, and azines bearing a 4-dimethylaminophenyl-5-oxopyrrolidine scaffold was synthesized. Their cytotoxic effect against human pancreatic carcinoma Panc-1 triple-negative breast cancer MDA-MB-231 cell lines established by MTT assay. Pyrrolidinone derivatives 3c 3d, with incorporated 5-chloro 5-methylbenzimidazole fragments; hydrazone 5k 5-nitrothien-2-yl substitution; 5l naphth-1-yl fragment in the structure significantly decreased viability both lines. Compounds...

It is well-known that thiazole derivatives are usually found in lead structures, which demonstrate a wide range of pharmacological effects. The aim this research was to explore the antiviral, antioxidant, and antibacterial activities novel, substituted compounds find potential agents could have biological one single biomolecule. A series novel aminothiazoles were synthesized, their activity characterized. obtained results compared with those standard anticancer agents. compound bearing...

Infections caused by multidrug-resistant bacterial and fungal pathogens represent a significant global health concern, contributing to increased morbidity mortality rates. Therefore, it is crucial develop novel compounds targeting drug-resistant microbial strains. Herein, we report the synthesis of amino acid derivatives bearing an incorporated 4-hydroxyphenyl moiety with various substitutions. The resultant 3-((4-hydroxyphenyl)amino)propanoic 2–37 exhibited structure-dependent antimicrobial...

A series of new derivatives based on sulfamethoxazole were designed and synthesized in this study. The structures the compounds confirmed a comprehensive characterization spectral data by applied IR 1 H as well 13 C NMR spectroscopy. prepared tested for their anticancer antimicrobial properties. Hydrazone 16b demonstrated convincing effect against all cell cultures such human prostate carcinoma PPC-1 kidney CaKi-1 lines, fibroblasts HF, n = 3. most promising compound showed higher activity...

The p-aminobenzoic acid was applied for the synthesis of substituted 1-phenyl-5-oxopyrrolidine derivatives containing benzimidazole, azole, oxadiazole, triazole, dihydrazone, and dithiosemicarbazide moieties in structure. All obtained compounds were evaluated their vitro antimicrobial activity against Staphylococcus aureus, Bacillus cereus, Listeria monocytogenes, Salmonella enteritidis, Escherichia coli, Pseudomonas aeruginosa by using MIC MBC assays. This study showed a good bactericidal...

Rapidly growing antimicrobial resistance among clinically important bacterial and fungal pathogens accounts for high morbidity mortality worldwide. Therefore, it is critical to look new small molecules targeting multidrug-resistant pathogens. Herein, in this paper we report a synthesis, ADME properties, vitro activity characterization of novel thiazole derivatives bearing β-amino acid, azole, aromatic moieties. The silico revealed that compounds 1-9 meet at least 2 Lipinski drug-like...

Novel functionalized thiazoles were prepared by the Hantzsch reaction from 3-[(4hydroxyphenyl)carbamothioylamino]-2-methylpropanoic acid and corresponding α-halocarbonyl compounds in good yields.A series of chemical transformations obtained products carried out, new thiazole derivatives with aliphatic, aromatic heterocyclic substituents synthesized.4-Phenyl-substituted N-(4-hydroxyphenyl)-N-carboxyalkylaminothiazoles used as precursors for synthesis bis(thiazol-5-yl)methane derivatives,...

Abstract A series of substituted thiazoles bearing different functional groups, such as carboxyethylamino, carboxyl, chloromethyl, (phenylamino)methyl, ethoxyoxoethyl, methoxyoxoethylidene, ethoxycarbonyl, (methoxy or hydrazinyl)oxopropyl, carbohydrazinyl, formyl, and ((phenyl, carbamothioyl isonicotinoyl)hydrazono)methyl, incorporated into their structure were synthesized. The synthesized compounds tested for antimicrobial activity against Escherichia coli , Staphylococcus aureus...

The 1-(4-acetamidophenyl)-5-oxopyrrolidine carboxylic acid was applied for synthesizing derivatives bearing azole, diazole, and hydrazone moieties in the molecule. Modification of an acetamide fragment to free amino group afforded compounds with two functional groups, which enabled provide a series 4-substituted-1-(4-substituted phenyl)pyrrolidine-2-ones. resulted 2 4-22 were subjected vitro anticancer antimicrobial activity determination. 18-22 exerted most potent against A549 cells....

Increasing antimicrobial resistance among Gram-positive pathogens and pathogenic fungi remains one of the major public healthcare threats. Therefore, novel candidates scaffolds are critically needed to overcome in drug-resistant fungal pathogens. In this study, we explored 1-(2-hydroxyphenyl)-5-oxopyrrolidine-3-carboxylic acid its 3,5-dichloro-2-hydroxyphenyl analogue for their vitro activity against multidrug-resistant The compounds showed structure-dependent (S. aureus, E. faecalis, C....

In this study, we have synthesized novel 4-acetophenone moiety-bearing functionalized imidazole derivatives containing S-, and N-ethyl substituents evaluated their anticancer activity. Their activity was studied against human breast carcinoma (MDA-MB-231), prostate (PPC-1), glioblastoma (U-87). Compounds 4, 9, 14, 22 were identified as the most promising agents from a series of derivatives. They showed highest cytotoxicity by MTT assay MDA-MB-231, PPC-1 U-87 cell lines. 14 selective lines,...

The growing antimicrobial resistance to last-line antimicrobials among Gram-positive pathogens remains a major healthcare emergency worldwide. Therefore, the search for new small molecules targeting multidrug-resistant of great importance. In this paper, we report synthesis and in vitro activity characterisation novel thiazole derivatives using representative Gram-negative strains, including tedizolid/linezolid-resistant S. aureus, as well emerging fungal pathogens. 4-substituted thiazoles...

Abstract A series of novel 1,2‐bissubstituted disulfanes bearing beta‐amino acid, dihydropyrimidine‐2,4‐(1 H ,3 )‐dione, hydrazide, hydrazone and azole moieties were synthesized. The antibacterial activity was evaluated by determining minimum inhibition (by broth microdilution) bactericidal growth on agar) concentrations. assessment revealed that MIC values for L. monocytogenes varied between 3.9 62.5 μg/mL as well S. aureus ranged 7.8 250 μg/mL, with the exception one compound much weaker...

A series of 1-aryl substituted dihydro-, 5-methyl-dihydro- and 6-methyl-dihydro-2,4(1H,3H)pyrimidinediones their 2-thio analogues were obtained by reaction the corresponding beta-alanines or alpha-methyl- beta-methyl-beta-alanines with urea potassium thiocyanate. The N-(2,3- 3,5-dimethylphenyl)-alpha-methyl-beta-alanines ethyl acetoacetate gave 1-(2,3- 3,5-dimethylphenyl)-2,5-dimethyl-1,4,5,6-tetrahydro-4(1H)pyridones. combined spectral data (1)H-, (13)C-,(1)H/(13)C (HETCOR) NMR IR provided...

A series of novel N-(4-fluorophenyl)-N-carboxyethylaminothiazoles and thiazolones with aliphatic, aromatic heterocyclic substituents were obtained in good to excellent overall yields.The synthesized compounds screened for their antimicrobial antifungal activity.The antibacterial tests indicated that the functionalized aminothiazole derivatives exhibit a higher activity as compared thiazolone derivatives.

A new potentially biologically active N ‐(4‐chloro/iodophenyl)‐ ‐carboxyethyl‐β‐alanine derivatives ( 2 , 2a 2b 3 3a 3b 4 4a 4b 8 8a 8b 9 9a 9b ) and products of their cyclization 6 6a 6b 7 7a 7b 10 10a 10b 11 11a 11b were obtained characterized by the methods 1 H‐NMR, 13 C‐NMR, IR, mass spectroscopy, elemental analysis.