Article
Chemistry, Medicinal
Niccolo Chiaramonte, Andrea Angeli, Silvia Sgambellone, Alessandro Bonardi, Alessio Nocentini, Gianluca Bartolucci, Laura Braconi, Silvia Dei, Laura Lucarini, Elisabetta Teodori, Paola Gratteri, Bernhard Wuensch, Claudiu T. Supuran, Maria Novella Romanelli
Summary: Targeting carbonic anhydrases is a strategy for treating various diseases. In this study, a new series of chiral piperazine compounds was synthesized to widen the structure-activity relationships of potent human carbonic anhydrase inhibitors. Some of the synthesized compounds showed high inhibitory activity.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Physical
Serdar Burmaoglu, Elif Akin Kazancioglu, Mustafa Z. Kazancioglu, Ruya Saglamtas, Gozde Yalcin, Ilhami Gulcin, Oztekin Algul
Summary: This study synthesized new biphenyl-substituted chalcone derivatives and evaluated their inhibitory activity against various enzymes. The results showed that these derivatives exhibited effective inhibition against the enzymes and have potential for the development of new drugs for the treatment of diverse diseases.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Chemistry, Medicinal
Busra O. Aydin, Derya Anil, Yeliz Demir
Summary: In this study, new derivatives of pyrazolo[3,4-d]pyrimidine were synthesized by alkylating the N1 nitrogen atom. These compounds showed a broad spectrum of biological activity. The synthesis involved a series of steps to generate N-alkylated pyrazolo[3,4-d]pyrimidine derivatives, which were then tested for their ability to inhibit AChE and hCA isoforms. Among them, compound 10 exhibited the highest selectivity and potency as a CA I inhibitor.
ARCHIV DER PHARMAZIE
(2021)
Review
Chemistry, Medicinal
Shubham Kumar, Sandeep Rulhania, Shalini Jaswal, Vikramdeep Monga
Summary: Carbonic anhydrase is an important enzyme involved in various physiological and pathological processes, with 16 different isoforms in humans. Inhibitors targeting different isoforms of carbonic anhydrase have clinical applications in treating various diseases, but current drugs lack selectivity leading to undesired side effects. Efforts are being made to develop novel isoform-selective inhibitors of carbonic anhydrase for therapeutic implications.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Physical
Samira Zareei, Maryam Mohammadi-Khanaposhtani, Mehdi Adib, Mohammad Mahdavi, Parham Taslimi
Summary: In this study, a series of new sulfonamide-phosphonate hybrids were synthesized and evaluated for their inhibitory effects on carbonic anhydrase enzymes. The results demonstrated that these compounds exhibited potent inhibitory activity against human carbonic anhydrase, with certain compounds showing even greater potential. Molecular docking studies further revealed significant interactions between these compounds and the active site of the enzymes.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Biochemistry & Molecular Biology
Xiaojing Huang, Daniel Winter, Dominic. J. J. Glover, Claudiu. T. T. Supuran, William. A. A. Donald
Summary: Carbonic anhydrases (CAs) are metalloenzymes that play important roles in cellular processes and have been implicated in various diseases. Phosphorylation, a common post-translational modification of CAs, can significantly impact their catalytic activity and drug-binding capabilities. This study highlights the potential regulatory role of phosphorylation in CA activity and its effect on small molecule drug binding.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Cuneyt Turkes, Yeliz Demir, Sukru Beydemir
Summary: The study found that some calcium channel blockers may act as potential inhibitors of hCA I and hCA II, with nimodipine showing the best performance. These compounds could be useful in developing new CA inhibitors.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2021)
Article
Chemistry, Multidisciplinary
Marta Meneghello, Ana Rita Oliveira, Aurore Jacq-Bailly, Ines A. C. Pereira, Christophe Leger, Vincent Fourmond
Summary: Mo/W formate dehydrogenases catalyze the reversible reduction of CO2 to formate, and it has been definitively demonstrated through an electrochemical method that the substrate is indeed CO2, not a hydrated species like HCO3-.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2021)
Article
Biochemistry & Molecular Biology
Alessandro Bonardi, Seppo Parkkila, Claudiu T. Supuran
Summary: This study investigated the inhibition of the alpha-class carbonic anhydrase from Trypanosoma cruzi with phenols, which have a different mechanism of inhibition compared to previously studied compounds. The results showed that certain phenols were effective inhibitors of the enzyme, suggesting their potential as antiprotozoal agents.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Fevzi Topal, Kadir Aksu, Ilhami Gulcin, Ferhan Tumer, Suleyman Goksu
Summary: This study identified a series of symmetric sulfamide compounds that exhibited good inhibitory effects against human carbonic anhydrase I and II isoenzymes, with compound 11 showing the best performance. Acetazolamide, used as the standard, displayed higher IC50 values. Additionally, in silico ADME-Tox study showed good oral bioavailability for all synthesized compounds according to Jorgensen's rule of three and Lipinski's rule of five.
CHEMISTRY & BIODIVERSITY
(2021)
Article
Biochemistry & Molecular Biology
Furkan Orhan, Murat Senturk, Mucip Genisel
Summary: This study documented the characterization and inhibition characteristic of alpha-class carbonic anhydrase from Chromohalobacter (ChCA) for the first time. The enzyme had a high yield and purity, with a specific activity of 318.52 U/mg proteins. Alternative substrates were tested for the enzyme, and the inhibitory activities of various anions were also evaluated. The results showed that the tested anions inhibited the ChCA enzyme, but the susceptibility differed significantly from other organisms' carbonic anhydrases.
COMPARATIVE BIOCHEMISTRY AND PHYSIOLOGY C-TOXICOLOGY & PHARMACOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Davide Moi, Serena Vittorio, Andrea Angeli, Gianfranco Balboni, Claudiu T. Supuran, Valentina Onnis
Summary: A series of hydrazonobenzenesulfonamides were designed, synthesized and evaluated for their inhibitory activity against human carbonic anhydrase (hCA) isoforms. The synthesized compounds showed inhibitory activity at low nanomolar levels against hCA I, II, IX and XII, with selectivity against hCA II isoform, as well as hCA IX and XII isoforms. Docking studies were conducted to understand the activity and selectivity of the most potent and selective hydrazones towards different CA isoforms.
Article
Biology
Derya Aktas Anil, M. Fatih Polat, Ruya Saglamtas, Ayse H. Tarikogullari, M. Abdullah Alagoz, Ilhami Gulcin, Oztekin Algul, Serdar Burmaoglu
Summary: Enzyme inhibition is an active area of research in drug design and development. Chalcone derivatives have potential as new drugs with broad enzyme inhibitory activity. In this study, halogenated chalcones were synthesized and evaluated for their inhibitory activity against acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and human erythrocyte carbonic anhydrase I (hCA I) and II (hCA II). The results showed potent inhibition against AChE and BChE, indicating their potential in the development of new drugs to treat global disorders such as Alzheimer's disease, glaucoma, and diabetes.
COMPUTATIONAL BIOLOGY AND CHEMISTRY
(2022)
Article
Microbiology
Gayatri Shankar Chilambi, Yu-Hao Wang, Nathan R. Wallace, Chetachukwu Obiwuma, Kirsten M. Evans, Yanhong Li, Menna-Allah W. Shalaby, Daniel P. Flaherty, Ryan K. Shields, Yohei Doi, Daria Van Tyne
Summary: This study identified a mutant strain of Enterococcus faecalis that is hypersusceptible to aminoglycoside antibiotics due to disruption of alpha-carbonic anhydrase (alpha-CA). Disruption of alpha-CA increased proton motive force and membrane permeability, leading to increased gentamicin uptake in E. faecalis. Additionally, an FDA-approved alpha-CA inhibitor sensitized various E. faecalis strains to gentamicin.
MICROBIOLOGY SPECTRUM
(2023)
Article
Plant Sciences
Naveen Sharma, John E. Froehlich, Rees Rillema, Daniel A. Raba, Taylor Chambers, Cheryl A. Kerfeld, David M. Kramer, Berkley Walker, Federica Brandizzi
Summary: This study characterized two plastidial beta carbonic anhydrases, beta CA1 and beta CA5, in Arabidopsis plants. The results showed that both proteins are localized in the chloroplast stroma and that the loss of beta CA5 induces the expression of beta CA1. The study also revealed that the two enzymes have different enzymatic kinetics and physiological relevance. Rating: 8 out of 10
Article
Chemistry, Multidisciplinary
Zubeyda Israfilova, Parham Taslimi, Ilhami Gulcin, Yusif Abdullayev, Vagif Farzaliyev, Muhammet Karaman, Afsun Sujayev, Saleh H. Alwasel
Summary: This study focuses on the synthesis of thiocyanate-containing heterocyclic compounds and determines their inhibitory abilities against various enzymes. Theoretical calculations reveal the mechanism of substituting chloride with thiocyanate in aziridine derivatives. The synthesized compounds show potent inhibitory abilities and specifically inhibit hCA I and hCA II enzymes.
Article
Biology
Muzaffer Mutlu, Zeynebe Bingol, Eda Mehtap Uc, Ekrem Koksal, Ahmet C. Goren, Saleh H. Alwasel, Ilhami Gulcin
Summary: This study evaluated the antioxidant and antidiabetic properties of cinnamon leaf essential oil and determined its inhibitory effects on enzymes associated with metabolic diseases. Phenolic contents and essential oil profiles were analyzed. Cinnamon oil showed strong radical scavenging abilities and effectively inhibited carbonic anhydrase II, acetylcholinesterase, and alpha-amylase. This multidisciplinary study is valuable for further research on antioxidant properties and enzyme inhibition profiles of important plants and their oils.
Article
Chemistry, Inorganic & Nuclear
Ramazan Zengin, Yetkin Gok, Yeliz Demir, Betul Sen, Tugba Taskin-Tok, Aydin Aktas, Ozlem Demirci, Ilhami Gulcin, Muhittin Aygun
Summary: In this study, a series of symmetric and unsymmetric N-heterocyclic carbene (NHC) precursors based on benzimidazol-2-ylidene were synthesized and their structures were characterized. The enzyme inhibition activities of these compounds against acetylcholinesterase (AChE) and carbonic anhydrases (hCAs) were investigated, showing potent inhibitory effects. These results have potential implications for the development of new drug candidates for the treatment of Alzheimer's disease and glaucoma.
JOURNAL OF FLUORINE CHEMISTRY
(2023)
Article
Chemistry, Physical
Zafer Bulut, Nurgul Abul, Ayse Halic Poslu, Ilhami Gulcin, Abdulilah Ece, Erol Ercag, Omer Koz, Gamze Koz
Summary: A series of novel uracil-appended benzylic amines were synthesized through reductive amination with moderate to good yields (30-84% yields). The compounds were characterized using FT-IR, H-1 NMR, C-13 NMR spectroscopy and elemental analysis. The inhibition abilities of the compounds were evaluated against acetylcholinesterase (AChE) and human carbonic anhydrase I and II (hCA I and II) isoenzymes.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Chemistry, Physical
Nawrooz Ali Zahedi, Maryam Mohammadi-Khanaposhtani, Parisa Rezaei, Mohammad Askarzadeh, Majid Alikhani, Mehdi Adib, Mohammad Mahdavi, Bagher Larijani, Somayeh Niakan, Maliheh Barazandeh Tehrani, Parham Taslimi, Ilhami Gulcin
Summary: Alzheimer's disease (AD) is a complex and progressive cognitive disorder. Cholinesterase (ChE) inhibitors have been proven to be effective in treating AD, and recent studies have shown that inhibiting human carbonic anhydrases (hCAs) can also aid in AD treatment. New coumarindihydropyridine derivatives (6a-m) were designed to combine potent ChE and hCA inhibitory effects. These compounds were evaluated and showed promising results against AChE, BChE, and hCAs. In silico screening using Autodock software and preADMET online software further confirmed their potential therapeutic properties.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Chemistry, Multidisciplinary
Mehmet Koca, Ilhami Gulcin, Eda Mehtap Uc, Sinan Bilginer, Amine Sena Aydin
Summary: In this study, a hybrid molecule consisting of salicylic acid and salicyl amide structures was synthesized and five new amide derivatives were synthesized for the first time. Their antioxidant potentials were evaluated through various assays, and their potential as drug candidates for Alzheimer's disease was investigated through AChE inhibition studies.
JOURNAL OF THE IRANIAN CHEMICAL SOCIETY
(2023)
Article
Chemistry, Medicinal
Halil Senol, Gurbet Celik Turgut, Alaattin Sen, Rueya Saglamtas, Salih Tuncay, Ilhami Gulcin, Guelacti Topcu
Summary: In this study, a series of compounds were synthesized from oleanolic acid (OA), including five new compounds (10, 11, 12, 15 and 17) as oxime, imine and hydrazone derivatives. NMR and HRMS analyses were conducted to determine their structures. The inhibitory effects of these compounds on acetylcholinesterase (AChE), human carbonic anhydrase I (hCA I) and II (hCA II) were evaluated. Compounds 13 and 15 exhibited significant inhibitory activity against both hCA I and hCA II, with compound 15 also showing the strongest AChE inhibitory activity.
MEDICINAL CHEMISTRY RESEARCH
(2023)
Article
Biochemistry & Molecular Biology
Hasan Karagecili, Mustafa Abdullah Yilmaz, Adem Erturk, Hatice Kiziltas, Leyla Guven, Saleh H. Alwasel, Ilhami Gulcin
Summary: This study investigated the chemical composition and antioxidant activities of propolis, finding that it is rich in phenolic and flavonoid compounds with antioxidant, antimicrobial, and anticancer properties. Propolis extract also exhibited inhibitory activities against enzymes associated with diabetes, Alzheimer's disease, and glaucoma. Additionally, twenty-eight phenolic compounds were determined to be major organic compounds in propolis, making it a potential natural product for the treatment of various diseases.
Article
Chemistry, Medicinal
Leyla Guven, Adem Erturk, Fatma Demirkaya Miloglu, Saleh Alwasel, Ilhami Gulcin
Summary: In this study, we evaluated the in vitro antiglaucoma, antidiabetic, anti-Alzheimer's disease, and antioxidant activities of the methanolic and water extracts of Astragalus alopecurus. The extracts showed inhibition ability on various enzymes and exhibited antioxidant properties. These findings provide a foundation for further exploring the therapeutic potential of Astragalus species.
Article
Biology
Hasan Karagecili, Ebubekir Izol, Ekrem Kirecci, Ilhami Gulcin
Summary: Zivzik pomegranate (Punica granatum) has gained interest recently for its nutritional and antioxidant properties. The antioxidant capacities of different extracts from peel and seed were evaluated using several methods, and compared with commonly used synthetic antioxidants. The extracts showed lower IC50 values for scavenging activities and exhibited inhibitory effects on various enzymes. LC-MS/MS analysis identified multiple phenolic compounds. Additionally, the bacteria E. coli and S. aureus showed resistance to standard antibiotics.
Article
Biochemistry & Molecular Biology
Cetin Bayrak, Parham Taslimi, Namik Kilinc, Ilhami Gulcin, Abdullah Menzek
Summary: In this study, the natural bromophenol butyl 2-(3,5-dibromo-4-hydroxyphenyl)acetate (1) and indene derivatives 34 and 35 were successfully synthesized. Several known natural bromophenols and their derivatives were also synthesized. The synthesized compounds exhibited strong inhibition effects against acetylcholinesterase, butyrylcholinesterase, and α-glycosidase enzymes.
CHEMISTRY & BIODIVERSITY
(2023)
Article
Biochemistry & Molecular Biology
Songul Cakmakci, Ilhami Gulcin, Engin Gundogdu, Hatice Ertem Oztekin, Parham Taslimi
Summary: Oxidation is a significant factor impacting the shelf life and quality of food. Plant-derived antioxidants, such as green tea powder, have been studied for their health benefits and use in food. This study compares the antioxidant effects of green tea powder with commercial antioxidants in butter and evaluates their impact on various properties.
Article
Biology
Eda Mehtap Ozden, Zeynebe Bingol, Muzaffer Mutlu, Hasan Karagecili, Ekrem Koksal, Ahmet C. Goren, Saleh H. Alwasel, Ilhami Gulcin
Summary: This research comprehensively examined and researched the kiwifruit oil using various bioanalytical methods, determining its antioxidant, antiglaucoma, antidiabetic, and anti-Alzheimer's capabilities. The inhibitory effects on several enzymes linked to metabolic illnesses were also established. The chemical composition and quantity of essential oils contained in kiwifruit oil were studied. The results demonstrated the potent radical scavenging properties and inhibition effects on enzymes of kiwifruit oil, suggesting its significant potential in pharmaceutical procedures.
Article
Biochemistry & Molecular Biology
Alper Yildirim, Ufuk Atmaca, Ertan Sahin, Parham Taslimi, Tugba Taskin-Tok, Murat Celik, Ilhami Gulcin
Summary: This article examines the use of oxazolidinones in various applications such as antibiotics and protein synthesis inhibition. The synthesized compounds were found to have potent inhibitory effects on enzymes such as acetylcholinesterase and carbonic anhydrase. Molecular docking and ADMET analysis were conducted to correlate the experimental data.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Biochemistry & Molecular Biology
Erkan Oner, Yetkin Gok, Yeliz Demir, Tugba Taskin-Tok, Aydin Aktas, Ilhami Gulcin, Serap Yalin
Summary: This study presents the synthesis and characterization of a series of benzimidazolium salts, and investigates their enzyme inhibition abilities against acetylcholinesterase and carbonic anhydrase. The results show that these salts have potent inhibition effects. The pharmacokinetic properties of the compounds were also predicted.
CHEMISTRY & BIODIVERSITY
(2023)
