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Öğe Aminopyrazole-substituted metallophthalocyanines: Preparation, aggregation behavior, and investigation of metabolic enzymes inhibition properties(Wiley-V C H Verlag Gmbh, 2019) Guzel, Emre; Kocyigit, Umit M.; Arslan, Baris S.; Atas, Mehmet; Taslimi, Parham; Gokalp, Faik; Gulcin, IlhamiThe synthesis, characterization, aggregation behavior, theoretical studies, and investigation of antimicrobial, antidiabetic, and anticholinergic properties of 4-(2-(5-amino-4-(4-bromophenyl)-3-methyl-1H-pyrazol-1-yl)ethoxy)phthalonitrile (2) and its soluble aminopyrazole-substituted peripheral metallo (Mn, Co, and Ni)-phthalocyanine complexes (3-5) are reported for the first time. The synthesized compounds and phthalocyanine complexes were characterized spectroscopically. The new phthalonitrile derivative (2) and its peripheral metallophthalocyanine complexes (3-5) were found to be effective inhibitors of alpha-glycosidase, acetylcholinesterase (AChE), human carbonic anhydrase I and II isoforms (hCA I and II), and butyrylcholinesterase (BChE) with K-i values in the range of 1.55 +/- 0.47 to 10.85 +/- 3.43 nM for alpha-glycosidase, 8.44 +/- 0.32 to 21.31 +/- 7.91 nM for hCA I, 11.73 +/- 2.82 to 31.03 +/- 4.81 nM for hCA II, 101.62 +/- 26.58 to 326.54 +/- 89.67 nM for AChE, and 68.68 +/- 11.15 to 109.53 +/- 19.55 nM for BChE. This is the first study of peripherally substituted phthalocyanines containing an aminopyrazole group as potential carbonic anhydrase enzyme inhibitor. Also, the antimicrobial activities of the synthesized compounds were evaluated against six microorganisms (four bacteria and two Candida species) using the broth microdilution method. The gram-positive bacteria were detected to be more sensitive than gram-negative bacteria and yeasts in the synthesized compounds.Öğe Arylated Quinoline and Tetrahydroquinolines: Synthesis, Characterization and Their Metabolic Enzyme Inhibitory and Antimicrobial Activities(Wiley-V C H Verlag Gmbh, 2022) Kocyigit, Ümit Muhammet; Ökten, Salih; Çakmak, Osman; Burhan, Gizem; Ataş, Mehmet; Taslimi, Parham; Gülçin, İlhamiThe aims of this study are to synthesize and characterize some new phenyl quinoline derivatives and to determine the activities of them and the recently prepared substituted phenyl quinolines against Acetylcholinesterase (AChE) and Charbonic anyhydrase (CA) enzymes and some microorganisms. The 6-phenyl- (3a) and 6,8-diphenyl-(4a) tetrahydroquinolines were prepared by treatment of 6-bromo and 6,8-dibromo-1,2,3,4-tetrahydroquinoline with phenylboronic acids in the presence of Pd catalyze in high yields with respect to our reported procedure. Then, bromination of the 6-phenyl- (3a) and 6,8-diphenyl-(4a) tetrahydroquinolines furnished novel 3-bromo phenyl substituted quinolines 14 and 11 and 8-bromo-6-pheyltetrahydroquinoline (13) in excellent yields (91, 99 and 92 %, respectively). Structures of all prepared compounds were characterized by H-1 NMR,C-13 NMR, FTIR spectroscopy and elemental analysis. Both novel prepared and recent synthesized phenyl substituted tetrahydroquinolines and quinolines were screened for human carbonic anhydrase I, II isoenzymes (hCAs I and II) and AChE inhibitory and antimicrobial activities. Results indicated that all the synthetic compounds exhibited potent inhibitory activities against all targets as compared to the standard inhibitors, revealed by IC50 values. K-i values of novel substituted (trifluoromethoxy, thiomethyl and methoxy) phenyl quinolines 3a-d, 4a-c, 8-12, and 14 for hCA I, hCA II and AChE enzymes were obtained in the ranges 0.31-12.44, 0.92-12.45, and 8.56-27.05 mu M, respectively. Moreover, phenyl quinolines 3a-b, 10, 11, 14 displayed antifungal effect against yeasts in the range of 125-15.62 mu g/mL.Öğe Composition characterization and biological activity study of Thymbra spicata l. var. spicata essential oil(2021) Eruygur, Nuraniye; Kocyıgıt, Umit M.; Atas, Mehmet; Cevık, Ozge; Gökalp, Faik; Taslimi, Parham; Gulcın, İlhamiThe current research aimed to determine and report in vitro antioxidant, antimicrobial, antibiofilm, cytotoxic, anti-cholinesterase, and anti-diabetic properties and the stability of the major component of basic oil of Thymbra spicata var. spicata through different phases as theoretically. Essential oil exhibits potential biological activities because of the multiple components it contains.In the current research, the evaluation of Thymbra spicata essential oil antioxidant properties was conducted utilizing 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2- azinobis[3-ethylbenzthiazoline]-6-sulfonic acid (ABTS) radical scavenging activity.Antimicrobial activity was assessed from minimum inhibition concentration (MIC) using the technique of microdilution and cytotoxicity activity was evaluated by MTT assay through MCF-7 and PC3 human cancer cell lines.Consequently, Cytotoxic activity was evaluated by means of MTT assay utilized. The essential oil was detected to have 340 ?g/mL inhibiting influence on the growth of PC3 prostate cancer cells with IC50 value. Also, the T. spicata plant was observed to significantly repress the enzymes, namely acetylcholinesterase (AChE), butyrylcholinesterase (BChE), ?-glycosidase. IC50 values of enzymes were obtained 0.23 ?g/mL for AChE, 1.64 ?g/mL for BChE, 7.78 ?g/mL for ?-glycosidase. It was concluded that this plant may be used for Alzheimer's and diabetes disease.Öğe Evaluation of Anticholinergic, Antidiabetic and Antioxidant Activity of Astragalus dumanii, an Endemic Plant(Kahramanmaras Sutcu Imam Univ Rektorlugu, 2022) Koçyiğit, Ümit Muhammet; Eruygur, Nuraniye; Ataş, Mehmet; Tekin, Mehmet; Taslimi, Parham; Gökalp, Faik; Gülçin, İlhamiThe research was conducted to separately evaluate and detect the possible in vitro antioxidant, antimicrobial activity of ethanol extracts prepared from aerial parts and roots of Astragalus dumanii and anti-cholinesterase and alpha-glucosidase inhibitory activity from only aerial parts of its The antioxidant capacity was tested by scavenging of DPPH and ABTS free radicals. Compared with the standard antioxidant compound gallic acid; Root and aerial part extract showed lower DPPH radical scavenging activity, however aerial part extract demonstrated higher ABTS radical scavenging activity. The phenolic contents were detected as 5.31 +/- 0.03 and 13.23 +/- 0.05 mg gallic acid equivalent g-1 extract, flavonoid contents were found as 8.26 +/- 0.004 and 7.93 +/- 0.005 mg Qercetin equivalent g-1 extract. In addition, the effects of the extracts obtained from aerial parts of the plant on acetylcholinesterase, butyrylcholinesterase and a-glycosidase enzymes were investigated in vitro and IC50 values were obtained as 1.47, 0.83 and 0.48 mu g mL-1, respectively. When these values were compared with standard substances, it was seen that Astragalus dumanii could be a good enzyme inhibitory agent. Antimicrobial activity of the plant extracts were determined using the microdilution method and the extracts was not observed to have any antimicrobial activities..Öğe Novel piperazine and morpholine substituted quinolines: Selective synthesis through activation of 3,6,8-tribromoquinoline, characterization and their some metabolic enzymes inhibition potentials(ELSEVIER, 2020) Cakmak, Osman; Okten, Salih; Alimli, Dilek; Ersanli, Cem Cuneyt; Taslimi, Parham; Kocyigit, Umit MuhammetRegioselective routes are described for convenient preparation of novel piperazine/morpholine substituted quinoline derivatives at C-3, C-6 and C-8 starting with 3,6,8-tribromoquinoline (6) by nucleophilic substitution via conventional heating or microwave assisted reaction conditions. 3,6,8-Tribromoquinoline (6) was treated with piperazine and morpholine under microvawe irradiation, which selectively furnished 3-mopholinyl and 3-piperazinyl quinoline derivatives 7 and 8 in yields of 58% and 60%, respectively. On the other hand, the activation of benzene cycle of quinoline by nitration of 3,6,8-tribromoquinoline, giving 5-nitro-3,6,8-tribromoquinoline (18) in quantitative yield, was enabled. Then, the bromines at C-6 and C-8 were selectively exchanged by morpholine and piperazine via SNAr reactions. Thus, 6,8-dimopholinylquinoline (22) and 5-nitro-6,8-dipiperazinylquinoline (24), biologically valuable derivatives, were prepared in high yields (82% and 72%, respectively). The synthesized compounds were fully characterizated by H-1 NMR, C-13 NMR, 2D NMR, XRD, HRMS and IR spectra. The novel molecules had effective inhibition profiles against some metabolic enzymes. Also, they have the potential of drug candidates to treat of some diseases including glaucoma, epilepsy, Alzheimer's disease (AD), leukemia, and type-2 diabetes mellitus (T2DM). (C) 2020 Elsevier B.V. All rights reserved.Öğe Quinoline-based promising anticancer and antibacterial agents, and some metabolic enzyme inhibitors(WILEY-V C H VERLAG GMBH, 2020) Ökten, Salih; Aydın, Ali; Koçyiğit, Ümit M.; Çakmak, Osman; Erkan, Sultan; Andaç, Cenk A.; Taslimi, ParhamA series of substituted quinolines was screened for their antiproliferative, cytotoxic, antibacterial activities, DNA/protein binding affinity, and anticholinergic properties by using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide cell proliferation, lactate dehydrogenase cytotoxicity, and microdilution assays, the Wolfe-Shimmer equality method, the Ellman method, and the esterase assay, respectively. The results of the cytotoxic and anticancer activities of the compounds displayed that 6-bromotetrahydroquinoline (2), 6,8-dibromotetrahydroquinoline (3), 8-bromo-6-cyanoquinoline (10), 5-bromo-6,8-dimethoxyquinoline (12), the novelN-nitrated 6,8-dimethoxyquinoline (13), and 5,7-dibromo-8-hydroxyquinoline (17) showed a significant antiproliferative potency against the A549, HeLa, HT29, Hep3B, and MCF7 cancer cell lines (IC50 = 2-50 mu g/ml) and low cytotoxicity (similar to 7-35%) as the controls, 5-fluorouracil and cisplatin. The compound-DNA linkages are hyperchromic or hypochromic, causing variations in their spectra. This situation shows that they can be bound to DNA with the groove-binding mode, withK(b)value in the range of 2.0 x 10(3)-2.2 x 10(5) M-1. Studies on human Gram(+) and Gram(-) pathogenic bacteria showed that the substituted quinolines exhibited selective antimicrobial activities with MIC values of 62.50-250 mu g/ml. All tested quinoline derivatives were found to be effective inhibitors of acetylcholinesterase (AChE) and the human carbonic anhydrase I and II isoforms (hCA I and II), withK(i)values of 46.04-956.82 nM for hCA I, 54.95-976.93 nM for hCA II, and 5.51-155.22 nM for AChE. As a result, the preliminary data showed that substituted quinolines displayed effective pharmacological features. Molecular docking studies were performed to investigate the binding modes and interaction energies for compounds2-17with AChE (PDB ID: 4EY6), hCA I (PDB ID: 1BMZ), and hCA II (PDB ID: 2ABE).Öğe Synthesis, characterization, and SAR of arylated indenoquinoline-based cholinesterase and carbonic anhydrase inhibitors(Wiley-V C H Verlag Gmbh, 2018) Ekiz, Makbule; Tutar, Ahmet; Okten, Salih; Butun, Burcu; Kocyigit, Umit M.; Taslimi, Parham; Topcu, GuelactiWe report the synthesis of bromoindenoquinolines (15a-f) by Friedlander reactions in low yields (13-50%) and the conversion of the corresponding phenyl-substituted indenoquinoline derivatives 16-21 in high yields (80-96%) by Suzuki coupling reactions. To explore the structure-activity relationship (SAR), their inhibition potentials to inhibit acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and human carbonic anhydrase cyctosolic (hCA I and II) enzymes were determined. Monophenyl (16-18) indenoquinolines significantly inhibited the AChE and BChE enzymes in ranges of IC50 37-57nM and 84-93nM, respectively, compared with their starting materials 15a-c and reference compounds (galanthamine and tacrine). On the other hand, these novel arylated indenoquinoline-based derivatives were effective inhibitors of the BChE, hCA I and II, BChE and AChE enzymes with K-i values in the range of 37 +/- 2.04 to 88640 +/- 1990nM for AChE, 120.94 +/- 37.06 to 1150.95 +/- 304.48nM for hCA I, 267.58 +/- 98.05 to 1568.16 +/- 438.67nM for hCA II, and 84 +/- 3.86 to 144120 +/- 2910nM for BChE. As a result, monophenyl indenoquinolines 16-18 may have promising anti-Alzheimer drug potential and 3,8-dibromoindenoquinoline amine (15f) can be novel hCA I and hCA II enzyme inhibitors.
