Sürdürülebilir Kalkınma Amaçları

• 2

• MakaleYalnız künye2023Scopus SJRQ3/r/bayburt/11835
  Methoxy-activated indole-7-carbohydrazides; synthesis, antioxidant, and anticancer properties

  Kandemir, Hakan; İzgi, Samet; Cınar, Irfan; Cebeci, Fatma; Dirican, Ebubekir; Saglam, Mehmet F.; Sengul, Ibrahim F.

  Indole has been known as a key heterocyclic motif in the development of new structures for both chemical and biological properties. In this current study, a new range of indole-7-carbohydrazides has been successfully synthesized starting from the readily available 3-phenyl and 2,3-diphenyl 4,6-dimethoxyindoles. The structures of the novel compounds were confirmed by utilizing 1H NMR, 13C NMR, FT-IR, high-resolution mass spectrometry, and single crystal X- ray diffraction techniques. In addition, the indole-7-carbohydrazides showed promising antioxidant results in preliminary screens. Some of the new compounds generated from dimethoxy indoles were also screened for their anticancer activity against SH-SHY5Y (human neuroblastoma), AGS (human gastric adenocarcinoma), and MDA-MB-231 (human breast adenocarcinoma) cell lines. The results revealed that the compound 12 was the promising candidate, showing cytotoxic effects on both neuroblastoma, stomach, and breast cancer cells.

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  AtıfScopus4·WoS4·OpenAlex6

  İncele
• MakaleYalnız künye2019Scopus SJRQ3/r/bayburt/13362
  Biocatalyzed Enantiomerically Pure Production of (S)-Phenyl(thiophen-2-yl)methanol

  Şahin, Engin; Dertli, Enes

  Chiral aryl heteroaryl methanols are important precursors for the synthesis of pharmaceutically important molecules. The aims of this study were to use a biocatalyst that could efficiently bioreduce phenyl(thiophen2- yl) methanone 1 to (S)-phenyl(thiophen-2-yl) methanol 2, to identify the impact of the physicochemical factors that might affect the bioreduction by the biocatalyst, and to obtain multigram production of aryl heteroaryl secondary alcohol 2 with the biocatalyst under optimized conditions. Over the years, the (S)phenyl( thiophen-2-yl) methanol was synthesized on a small scale using a chemical catalyst without its enantiomerically pure form. In this study, Lactobacillus paracasei BD101 was used for the asymmetric reduction of phenyl(thiophen-2-yl) methanone to (S)-phenyl(thiophen-2-yl) methanol in the large-scale production. The asymmetric bioreduction conditions were systematically optimized, and the production of 3.77 g of (S)-phenyl(thiophen-2-yl) methanol was carried out in enantiomerically pure form > 99% enantiomeric excess (ee), > 99% conversion, and 90% yield. This method obtained with this biocatalyst is a process that can be used industrially in terms of conversion, ee, and yield. This study provides guidance for the application of L. paracasei BD101 in the production of optically active aryl heteroaryl alcohols.

  AtıfScopus12·WoS12·OpenAlex12

  İncele
• MakaleYalnız künye2019Scopus SJRQ3/r/bayburt/12567
  Synthesis and Biological Evaluation of Novel Tricyclic Pyrrolidinyl (R)-Alcohols and Amines

  Şahin, Engin; Kılıç, Hamdullah; Törnük, Fatih; Dertli, Enes

  Three new tricyclic pyrrolidinyl alcohols and three tricyclic pyrrolidinyl amines were synthesized, and the antibacterial activities of these compounds were tested against Salmonella enterica subsp. enterica serovar Typhimurium, Escherichia coli O157:H7, Staphylococcus aureus, and Listeria monocytogenes. All tested pyrrolidinyl alcohols and amines showed antibacterial activity to the tested pathogens, but this activity was dependent on the final concentration of the tested compound, and the structure of these compounds were also important for this antibacterial activity. Of the tested compounds, (2R)-2-(octahydro-4,8-ethanocyclohepta[c] pyrrol2(1H)-yl)-2-phenylethanamine (2c) was the most effective compound among the tested pyrrolidinyl alcohols and amines. This study shows a good example of finding new antimicrobials in order to control pathogenic bacteria.

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  AtıfScopus1·WoS1·OpenAlex1

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