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YILMAZ, ANIL

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ANIL
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YILMAZ
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Now showing 1 - 6 of 6
  • PublicationMetadata only
    Semisynthesis and Kappa-Opioid Receptor Activity of Derivatives of Columbin, a Furanolactone Diterpene
    (2017-07-01) Yilmaz, ANIL; Crowley, Rachel Saylor; Sherwood, Alexander M.; Prisinzano, Thomas E.; YILMAZ, ANIL
    Columbin (1) is a furanolactone diterpene isolated from the roots of Jateorhiza and Tinospora species. These species generally grow in Asia and Africa and have been used in folk medicine for their apparent analgesic and antipyretic activities. Columbin (1) is of particular interest due to its structural similarity to the known kappa-opioid receptor (KOR) agonist salvinorin A. Given that the KOR is of interest in the study of many serious diseases, such as anxiety, depression, and drug addiction, obtaining natural or semisynthetic molecules with KOR activity recently has gained much interest. For this reason, in the present study, derivatives of 1 were designed and synthesized using known structure-activity relationships of salvinorin A at KORs. The structures of the columbin analogues prepared were elucidated by NMR spectroscopy and mass spectroscopy, and their KOR activity was investigated in vitro by inhibition of forskolin-induced CAMP accumulation. Slight improvements in KOR activity were observed in columbin derivatives over their parent compound. However, despite the structural similarities to salvinorin A, neither columbin (1) nor its derivatives were potent KOR ligands. This work represents not only the first evaluation of columbin (1) at the KOR but also one of the first works to explore synthetic strategies that are tolerated on the columbin core.
  • PublicationMetadata only
    A promising novel antidiabetic compound: Alysine-A
    (2016-09-01) Sen, A.; Ayar, B.; Topcu, GÜLAÇTI; Yilmaz, ANIL; TOPÇU, GÜLAÇTI; YILMAZ, ANIL
  • PublicationMetadata only
    Novel Terpenoids with Potential Anti-Alzheimer Activity from Nepeta obtusicrena
    (2016-01-01) Yilmaz, ANIL; Boga, Mehmet; Topcu, GÜLAÇTI; YILMAZ, ANIL; TOPÇU, GÜLAÇTI
    Dichloromethane extract of Nepeta obtusicrena Boiss. Et Kotschy Ex Hedge afforded two novel terpenoids, a diterpenoid and a triterpenoid in addition to two known triterpenoids, oleanolic acid and ursolic acid. Purification of the diterpenoid was carried out by HPLC, and its structure was elucidated as 14a-acetoxy-6-oxo-abieta-7-ene, and structure of the triterpenoid was elucidated as 2 alpha, 3 beta, 19 alpha, 24-tetrahydroxy-11-oxo-olean-12-ene. Both of the novel terpenes were obtained from nature for the first time and named as obtusicrenone and nemrutolone, respectively. Anticholinesterase (anti-Alzheimer) and antioxidant activities [DPPH free radical scavenging activity, ABTS cation radical scavenging activity, lipid peroxidation inhibitory activity, CUPRAC (Cupric Reducing Antioxidant Capacity)] of the dichloromethane and methanol extracts and the isolated four terpenoids were investigated. Both of the extracts and the isolated four terpenoids exhibited high anticholinesterase activity, particularly against acetylcholinesterase (AChE) enzyme. None of the samples tested showed high antioxidant activity.
  • PublicationMetadata only
    Therapeutic effects of Licorice (Glycyrrhiza glabra) on colitis through its antioxidant properties and biochemical analyses
    (2015-08-01) Uckaya, FATİH; Bektay, Yunus; Yilmaz, ANIL; Bayindir, NİHAN; Selek, ŞAHBETTİN; Topcu, GÜLAÇTI; Esrefoglu, MUKADDES; UÇKAYA, FATİH; BEKTAY, MUHAMMED YUNUS; YILMAZ, ANIL; BAYINDIR, NİHAN; SELEK, ŞAHABETTİN; TOPÇU, GÜLAÇTI; EŞREFOĞLU, MUKADDES
  • PublicationMetadata only
    Evaluation of anti-diabetic potential of circiliol and circilineol using CACO2 cell line
    (2016-09-01) Ayar, B.; Sen, A.; Topcu, GÜLAÇTI; Yilmaz, ANIL; TOPÇU, GÜLAÇTI; YILMAZ, ANIL
  • PublicationMetadata only
    Scalable Regioselective and Stereoselective Synthesis of Functionalized (E)-4-lodobut-3-en-1-ols: Gram-Scale Total Synthesis of Fungal DeCanolides and Derivatives
    (2018-01-19) Sherwood, Alexander M.; Williamson, Samuel E.; Johnson, Stephanie N.; Yilmaz, ANIL; Day, Victor W.; Prisinzano, Thomas E.; YILMAZ, ANIL
    A reliable protocol to synthesize both racemic and chiral (E)-4-iodobut-3-en-1-ols from aldehydes or epoxides, respectively, containing various aromatic and aliphatic substitutions has been established. The utility of these compounds was then demonstrated by providing access to known fungal decanolides as well as novel aromatic macrocycles. The protocol provided a gram-scale route to (-)-aspinolide A and (-)-5-epi-aspinolide A utilizing a catalytic Nozaki-Hiyama-Kishi reaction to close the macrolide in the final step in 65-84% yields.