Twenty-five new hydroxy-and methoxy-substituted 4,6-diarylpyrimidin-2(1H)-ol (20-34) and 4,6-diarylpyrimidine-2(1H)-thiol derivatives (35-44) were synthesized from the reaction of the corresponding 1,3-diaryl-2-propene-1one compounds (1-19) with urea or thiourea using the solid-phase microwave method. All the new synthetic compounds (20-44) were evaluated with regard to their α-glucosidase activity. However, only compounds 22-25, 27, 31, 34, 35, 37, and 40 exhibited a greater inhibitory effect than standard acarbose. The IC 50 values of the active compounds ranged between 2.36 and 13.34 µ M. The 25 new compounds were also screened for their in vitro pancreatic lipase activity and compounds 20-27 and 35-39 were found to be active. Of these compounds 26, 27, and 39 exhibited the best antilipase activities at concentrations of 0.40 ± 0.06, 0.26 ± 0.07, and 0.29 ± 0.026 µ M. All the new compounds (20-44) were evaluated for their in vitro antimicrobial activity for nine test microorganisms. Compounds 20-24 and 35-39 were determined to possess a significant broad spectrum against the gram-positive bacteria Escherichia faecalis, Staphylococcus aureus, and Bacillus cereus among the tested bacterial agents. Compounds 20-24 and 35-39 exhibit the best activity against Mycobacterium smegmatis, with minimum inhibitory concentrations of 62.5-500 µ g/mL, indicating their potential use as antituberculous agents.
The aim of the present study was to determine the chemical analysis, antimicrobial and antioxidant effects of the Eurhynchium angustirete (Broth.) and Isothecium alopecuroides (Lam. Ex Dubois) essential oil obtained by distillation method (Clevenger apparatus hydrodistillation). Obtained volatile oils were identified by gas chromatography-mass spectrometry (GC/MS) which revealed the presence of twenty-two components analyzed in the essential oil of E. angustirete representing 95.7% of the total identified compounds and twenty compounds were determined in the essential oil of I. alopecuroides representing 94.3% of the total identified compounds. Trans-pinocarveol and myrtenal as major constituents were 23.0% and 14.1% in E. angustirete and the main components were: biformene (9.9%), α-pinene (9.1%), bornyl acetate (8.4%) in I. alopecuroides. The essential oils from E. angustirete and I. alopecuroides showed higher metal-ion chelating activities which were 65.93±0.39% and 31.01±2.75, respectively. There was no significant difference results DPPH activity of essential oils 16.8±6.98 and 22.8%±8.91, respectively. The antimicrobial activity was investigated by microdiution method. The isolated essential oils were showed effective antimicrobial activities against Escherichia coli ATCC25922, Enterococcus faecalis ATCC29212, Staphylococcus aureus ATCC25923, Pseudomonas aeruginosa ATCC2785 and Streptococcus mutans. Antimicrobial effect values were found ranging of 90.76-95.38%. According to antimicrobial effect value against to microorganism, essential oil of E. angustirete was higher than I. alopecuroides.
The aim of this study is to analyze the volatile composition and antimicrobial and antioxidant activities of the essential oils of Polytrichum commune and Antitrichia curtipendula. The essential oils obtained by hydrodistillation (HD) from each species were identified by GC-MS/FID. The main components were biformene (13.06%), α-pinene (6.53%), and bornyl acetate (8.10%) in P. commune. Nonanal and tetradecanal as major compounds were 19.96% and 20.23% in A. curtipendula essential oils, respectively. Antioxidant activity of obtained essential oils was evaluated using in-vitro antioxidant models. There was no significant difference within the groups according to DPPH activity. Also, the essential oil from P. commune showed higher metal-ion chelating activities than that of the essential oil of A. curtipendula. Metal-ion chelating activities varied between 4.1% and 67.4% at the 800 µg/mL concentration, respectively. The antimicrobial activity was tested by a minimal inhibition concentration test. Each moss species showed good antimicrobial activity against microorganisms according to the results of minimal inhibition concentration experiments.
Bichalcones are obtained naturally from the genus Rhus. Bichalcones have attracted attention not only from a synthetic perspective but also because of their broad-spectrum biological activities. A series of methoxy-substituted chalcones (1-9) yielded C-C linked bichalcones (10-18) by the Ullmann coupling method, and their antimicrobial and antioxidant activities were assessed in this study. The confirmation of the synthesized compounds' structures was performed by NMR ( 1 H, 13 C, APT, and COSY), FT-IR, UV, and HRESI-TOF-MS data. According to the preliminary results, a number of the said compounds exhibited an interesting activity against Candida tropicalis. Moreover, the antioxidant activities of bichalcones (10-18) were evaluated according to DPPH and FRAP methods. Concerning antioxidant activities, compounds 15 and 16 were the most active compared to Trolox used as a standard. Of all the synthesized new bichalcone derivatives, compounds 10, 11, 12, 14, and 17 displayed higher activity against to fungal microorganism Candida tropicalis. Compounds 15 and 16 were found to have the highest antioxidant activity according to both DPPH and FRAP methods.
he chemical composition of the essential oils of Dianthus carmelitarum Reut. ex Boiss. and Dianthus calocephalus Boiss. were identified by GC-FID and GC-MS. Essential oils of D. carmelitarum and D. calocephalus were obtained from the whole part of fresh plant by Clevenger-type distillation. Analyses of the essential oils gave 40 and 35 compounds, constituting over 86.58% and 76.45% in the total, respectively. Main components in D. carmelitarum were heneicosane (11.69%), docosane (10.52%), tetracosane (9.20%) and pyhtol (4.62%). Whereas, 4,4dimethyl-2-pentene (17.65%), phytol (15.47%), pentacosane (4.38%) and hexahydrofarnesyl acetone (3.08%) were the major constituents in D. calocephalus. Antimicrobial activity of the essential oils obtained from D. carmelitarum and D. calocephalus were evaluated against nine gram positive, gram negative bacteria and the yeast-like fungi using disc diffusion and broth microdilution methods. The essential oils of D. carmelitarum and D. calocephalus showed good antimycotic activity against Candida albicans having the MIC values of 668 μg/mL and 1041 μg/mL, respectively. ÖZET Ianthus carmelitarum Reut. ex Boiss. ve Dianthus calocephalus Boiss. bitkilerinin uçucu yağlarının kimyasal bileşimleri GC-FID ve GC-MS ile aydınlatılmıştır. Taze bitkilerin uçucu yağları Clevenger tip destilasyon ile elde edilmiştir. Bitkilere ait uçucu yağ analizinde 40 ve 35 bileşik aydınlatılmış olup, bitkilerin toplam uçucu yağlarının sırasıyla %86.58 ve %76.45 kısmı aydınlatılmıştır. D. carmelitarum. bitkisinin ana bileşikleri, heneikosan (%11.69), dokosan (%10.52), tetrakosan (%9.20) ve Fitol (%4.62) olarak bulunmuştur. D. calocephalus bitkisinin ana bileşenleri ise; (4,4)-dimetil-2-penten (%17.65), fitol (%15.47), pentakosan (%4.38) ve hekzahidrofarnesil aseton (%3.08) bileşikleri bulundu. Elde edilen uçucu yağların dokuz adet gram pozitif, gram negatif bakteriler ve mayalara karşı antimikrobial aktivite tayinleri yapılmıştır. D. carmelitarum ve D. calocephalus bitkilerinin uçucu yağlarının Candida albicans bakterisine karşı antimikotik aktivite değerleri MIK olarak sırasıyla 668 μg/mL ve 1041 μg/mL gösterdiği tespit edilmiştir.
Özet Bu çalışmada, Lotus corniculatus L. var. corniculatus bitkisinin uçucu yağı, mikrodalga aparatlı destilasyon ile elde edilmiştir. Elde edilen uçucu yağın kimyasal bileşimi GC/MS, GC/FID cihazı ile aydınlatılmış ve Minimum İnhibisyon Konsantrasyon yöntemi (MIC) kullanılarak antimikrobiyal aktivitesi tayin edilmiştir. Uçucu yağ analizinde, bitkinin % 80.24'lük kısmı tanımlanmış olup, toplam 56 bileşik yapısı aydınlatılmıştır. Ana bileşen sınıfı olarak %30.60 oranında terpen ve terpen benzeri bileşikler, %16.89 oranında hidrokarbonlar, %12.49 aldehitlerden oluştuğu tespit edilmiştir. β-ionon (%4.83), (2E,4E) dekadienal (%4.13), β-pinen (%3.76), karahanoenon (%3.53) bileşikleri uçucu yağ içinde en fazla bulunan bileşikler olarak tespit edilmiştir. Lotus corniculatus bitkisinden ekstrakte edilen uçucu yağın hekzan çözücüsü içinde 51600 μg/mL konsantrasyonunda hazırlanan stok çözeltisinin; Escherichia coli (E. coli) ATCC35218, Yersinia pseudotuberculosis (Y. pseudotuberculosis) ATCC911, Pseudomonas aeruginosa (P. aeruginosa) ATCC43288, Enterococcus faecalis (E. faecalis) ATCC29212, Staphylococcus aureus (S. aureus) ATCC25923, Bacillus cereus (B. cereus) 709 Roma, Mycobacterium smegmatis (M. smegmatis) ATCC607 Gram pozitif, Gram negatif bakterilere ve Candida albicans (C. albicans) ATCC60193 maya mantarına karşı antimikrobiyal aktivite testi yapılmış ve uçucu yağın sadece maya mantarı üzerinde 645 μg/mL etkin değer gösterdiği tespit edilmiştir.
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