Feyzi Sinan Tokalı

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• Professor (Associate) at Kafkas University

The rising incidence of type 2 diabetes mellitus (T2DM) and its related complications has created an urgent need for new therapeutic approaches. We herein describe the synthesis as well as biological investigation of a series of sixteen new phenolic Mannich base derivatives of thiazolidine-2,4-dione as α-glucosidase (α-Glu) and aldose reductase (AL...

In this study, 16 novel quinazolin-4(3H)-one derivatives were synthesized and evaluated for their antileishmanial activity against Leishmania major and Leishmania donovani. Among them, compounds 2 (4-hydroxy substituted) and 9 (4-morpholino substituted) exhibited the highest efficacy, with compound 2 showing IC50 values of 23.94 μM for L. major and...

Quinazolinones, a prominent class of heterocyclic compounds, have garnered significant attention due to their diverse biological activities and synthetic versatility. Over the past thirty years, extensive research has been conducted to explore their pharmacological potential, making them an essential scaffold in modern medicinal chemistry. This re...

Discovery of novel and effective molecules is of vital importance in solving global health problems such as cancer, neurodegenerative diseases and antibiotic resistance. In this study, a series of isoniazid-based hydrazone derivatives were synthesized for the first time via the condensation of isoniazid with structurally diverse aldehydes, includin...

Aldose reductase (ALR2) inhibition is a promising therapeutic strategy for managing diabetes-related complications, including neuropathy, retinopathy, and nephropathy. This study reports the design, synthesis, and biological evaluation of eighteen novel quinazolin-4(3H)-one derivatives incorporating a 4-bromo-2-fluorobenzylidene moiety as ALR2 inhi...

The inhibition of aldose reductase (ALR2) presents a promising strategy for mitigating diabetes-related complications. In this study, eighteen novel thiazolidin-2,4-dione derivatives were synthesized and evaluated for their ALR2 inhibitory activity, with several exhibiting superior inhibition compared to the standard inhibitor epalrestat (EPR). Amo...

In this study, eleven novel quinazolin-4(3H)-one-thiazolidine-4-one hybrid compounds (1-11) were synthesized and evaluated for their in vitro aldose reductase (AR) inhibitory activity as potential therapeutics for diabetic complications. Structural characterization was performed using FT-IR, NMR, and HRMS techniques. The biological activity evaluat...

In this study, four compounds (1-4) belonging to the quinazolin-4(3H)-one class, which represents a significant part of nitrogen-containing six-membered heterocyclic compounds, were synthesized, and their structures were characterized using FTIR, NMR (1H and 13C), and HRMS spectroscopy techniques. As an application, the antioxidant activities of th...

In this study, ten new rhodanine and thiazolidine-2,4-dione derivatives based on Mannich-modified vanillin were synthesized, characterized, and evaluated for their anticancer potential against A549 lung cancer and BEAS-2B normal cells. Among them, compound 5c exhibited the most potent anticancer activity, with an IC50 of 2.43 µM and a selectivity i...

In this study, a series of 16 arylidene hydrazide derivatives (7a–7p), hybridized with the natural product carvacrol, were successfully synthesized starting from anthranilic acid methyl ester. The cytotoxic effects of these compounds were examined against two different cell lines, A549 and BEAS‐2B. Additionally, in silico studies were conducted to...

This study synthesized a total of 18 new anthranilic acid hydrazones and quinazolin‐4(3H)‐one derivatives, evaluating their cytotoxicity against the MCF7 and HUVEC cell lines. The anticancer effects of these compounds and their interactions with estrogen receptor alpha (ERα) and HER2 through molecular docking and molecular dynamics simulations. Cyt...

In this study, twelve novel polyphenols containing the quinazolin-4(3H)-one ring were synthesized and characterized using ¹H and ¹³C NMR, as well as HRMS, yielding compounds (1–12) with excellent yields (88–96%). Biological evaluation revealed significant cytotoxic activity against PC3 prostate cancer and 3T3 fibroblast cell lines, with compounds 2...

Several novel quinazoline derivatives bearing phenolic hydroxyl moiety (2–7) have been produced with good yields and screened for biological activities. All the title compounds were characterized using spectroscopic techniques such as 1H NMR, 13C NMR, FTIR, and HRMS. Then, the anti-browning effects of synthesized quinazoline derivatives were invest...

In this study, we synthesized and characterized sixteen new polymethoxy-substituted hydrazone derivatives. These compounds were evaluated for their in vitro cytotoxic activity against human prostate cancer (PC3) and human umbilical vein endothelial (HUVEC) cell lines. Compounds 5, 6, 7, and 11 exhibited significant cytotoxic effects with high selec...

In this study, we synthesized 15 novel quinazoline‐morpholinobenzylideneamino hybrid compounds from methyl anthranilate and we assessed their cytotoxicity via in vitro assays against A549 and BEAS‐2B cell lines. Molecular docking studies were conducted to evaluate the protein‐ligand interactions and inhibition mechanisms on nine different molecular...

In this study, we synthesized a new derivative molecule ( 5 ) that exhibits sensor properties. The characterization of the synthesized molecule was performed using spectroscopic methods such as ¹ H−, ¹³ C–NMR, FT–IR and Q–TOF. PVC‐membrane ion‐selective sensors were prepared in which the synthesized molecule was used as an ionophore. Surface images...

In this study, a new sulfonyl hydrazone derivative molecule was synthesized, and its characterization was performed using several spectroscopic methods (1H–, 13C NMR, FT–IR and Q-TOF). New potentiometric sensors were developed using this molecule, and subsequently, their potentiometric performance properties were investigated. Based on the data obt...

The secondary sulfonamide derivatives containing benzothiazole scaffold (1–10) were synthesized to determine their inhibition properties on two physiologically essential human carbonic anhydrases isoforms (hCAs, EC, 4.2.1.1), hCA I, and hCA II. The inhibitory effects of the compounds on hCA I and hCA II isoenzymes were investigated by comparing the...

Quinazolinones, which represent an important part of nitrogen‐containing six‐membered heterocyclic compounds, are frequently used in drug design due to their wide biological activity properties. Therefore, the novel quinazolinones were synthesized from the reaction of acylated derivatives of 4‐hydroxy benzaldehyde with 3‐amino‐2‐alkylquinazolin‐4(3...

In this study, new quinazoline–chromene hybrid compounds were synthesized. The cytotoxic effects on cell viability of the hybrid compounds were tested against A549 human lung adenocarcinoma and BEAS‐2B healthy bronchial epithelial cell lines in vitro. In addition, the ability of the active compounds to inhibit cell migration was tested. Molecular d...

N-substitued anthranilic acid derivatives are commonly found in the structure of many biologically active molecules. In this study, new members of hydrazones derived from anthranilic acid (1−15) were synthesized and investigated their effect on some metabolic enzymes such as acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and α-glycosida...

A series of thizaolidin-4-one derivatives (3a-o) was synthesized with excellent yield (94-97%) and the structures of the compounds were characterized with Fourier-transform Infrared (FTIR), Nuclear Magnetic Resonance (1H NMR - 13C NMR), and High-resolution Mass Spectroscopy (HRMS). Novel compounds were tested towards some metabolic enzymes includin...

In this study, twenty new anthranilic acid hydrazones 6–9 (a–e) were synthesized and their structures were characterized by Fourier‐transform Infrared (FT‐IR), Nuclear Magnetic Resonance (¹H‐NMR – ¹³C‐NMR), and High‐resolution Mass Spectroscopy (HR‐MS). The inhibitory effects of the compounds against COX‐II were evaluated. IC50 values of the compou...

In this study, acetovanillone derivative compounds (1–7) were synthesized, and their structures were analyzed using nuclear magnetic resonance (¹H NMR—¹³C NMR)and Fourier-transform infrared (FTIR) methods. The xylanase gene within the scope of the study was cloned using recombinant DNA techniques. The purified recombinant protein was subjected to c...

In this study, imines bearing quinazolin‐4(3H)‐one were synthesized and their inhibitory properties were investigated against some metabolic enzymes including Acetylcholinesterase (AChE), Butyrylcholinesterase (BChE), α‐Glycosidase (α‐Gly), and human Carbonic Anhydrase I–II (hCA I–II). All compounds had inhibitory strength with Ki values in the ran...

The design and synthesis of hydrazone derivatives are increasing in popularity day by day due to the significant biological activities of this scaffold. In the present study, twelve novel isonicotinic hydrazide-hydrazone analogues were synthesized by the condensation reaction of isonicotinic hydrazide with benzaldehyde possessing sulfonate moiety....

In this study, it was planned to synthesize new members of fenamate isosteres and investigate its effect on some metabolic enzymes such as Acetylcholinesterase, Butyrylcholinesterase, α‐Glucosidase, Carbonic andyhrase I–II. The target compounds were obtained from the reaction of N‐subtituted anthranilic hydrazides with sulfonylated aldehyde derivat...

In this study, a new series of quinazolin‐4(3H)‐ones, which constitute an important part of biologically active heterocyclic compounds, were synthesized with excellent yields (99‐94 %). The structures of the synthesized compounds (1–14) were characterized with Fourier‐transform infrared (FTIR), nuclear magnetic resonance (¹H NMR – ¹³C NMR), and hig...

Quinazolines are a group of bioactive heterocyclic compounds with a wide range of biological activities and have gained an important place in the design of active drugs with various targets due to their pharmacological properties. Carbonic anhydrase (CA) and acetylcholinesterase (AChE) inhibitors are very important pharmacologically. In this study,...

Cancer is one of the most common and lethal disease in the world therefore, patients need to new and potent anti-cancer agents to treatment. In this study, starting from vanillin, 24 new compounds, which are 12 thiosemicarbazone (4a-h, 5i-j, 6k) and 12 thiazolidin-4-one (7a-h, 8i-j and 9k) derivatives, were synthesized and characterized by NMR, HRM...

Aldose reductase (AR) is a crucial enzyme of the polyol pathway through which glucose is metabolized under conditions of hyperglycemia related to diabetes. A series of novel acetic acid derivatives containing quinazolin‐4(3H)‐one ring (1–22) was synthesized and tested for in vitro AR inhibitory effect. All the target compounds exhibited nanomolar a...

Triazoles are bioactive heterocyclic compounds with a wide range of biological activities and have an important place in drug design due to their pharmacological properties. In this study, six new 1,2,4-triazol-5-one derivatives (1-6) were synthesized, inspired by the pharmacological properties of triazoles. The structures of the new molecules were...

In this study, four new molecules belonging to the sulfonamide class, which are found in the structure of many biologically important molecules, were synthesized. Sulfadiazine (4-amino-N-(pyrimidin-2-yl)benzenesulfonamide), an important member of the sulfa drugs family, has been used as an amine reactant. The target compounds (1-4) were obtained fr...

In this study, new benzoic acid derivatives of the quinazolinone ring, which is one of the biologically active members of nitrogen‐containing heterocyclic compounds, were synthesized with excellent yields (98–90 %). The structures of the novel compounds (1–12) were characterized with Fourier‐transform Infrared (FTIR), Nuclear Magnetic Resonance (¹H...

İki ya da daha fazla bileşik sınıfından molekülün kimyasal reaksiyonlar kullanılarak tek bir molekülde birleştirilmesi moleküler hibridizasyon olarak bilinmektedir. Moleküler hibridizasyon ilaç tasarımı için iyi bir stratejidir. Biyolojik aktif iki ya da daha fazla molekülü bünyesinde bulunduran tek bir molekül biyolojik olarak daha etkili, seçici...

Quinazoline and quinazolinone derivatives display an extensive application in organic and pharmaceutical chemistry, and they have been used as natural and synthetic materials for medicinal chemistry purposes. Here I reported an investigation of a new series of quinazolin-4(3H)-one ring derivatives. In this context, starting from the methyl anthrani...

In the polyol pathway, aldose reductase (AR) catalyzes the formation of sorbitol from glucose. In order to detoxify some dangerous aldehydes, AR is essential. However, due to the effects of the active polyol pathway, AR overexpression in the hyperglycemic state leads to microvascular and macrovascular diabetic problems. As a result, AR inhibition h...

In this study, a simple and highly selective potentiometric sensor has been developed for the determination of cobalt(II) ions based on a poly(vinly chloride) (PVC) membrane. As an ionophore, a hydrazone derivative molecule (3) was synthesized for the first time, and its characterization was completed using NMR, FT‐IR and Q‐TOF spectroscopic techni...

Nitrogen-containing heterocyclic compounds are found in the structure of many drug molecules and many pharmacologically active molecules. Quinazolines and quinazolinones represent an important group of six-membered nitrogen-containing heterocycles. On the other hand, phenolic Mannich Bases are an important class of compounds that are frequently use...

In this study, 9 3-alkyl(aryl)-4-amino-4,5-dihydro-1H-1,2,4-triazol-5-one compounds were synthesized and their reactions with 4-formylphenyl 4-bromobenzenesulfonate were investigated and 9 new 4,5-dihydro-1H-1,2,4-triazol-5-one derivatives were obtained. Some of these synthesized compounds were reacted with formaldehyde and morpholine to yield 6 ne...

A series of novel sulfonates containing quinazolin‐4(3H)‐one ring derivatives was designed to inhibit aldose reductase (ALR2, EC 1.1.1.21). Novel quinazolinone derivatives (1–21) were synthesized from the reaction of sulfonated aldehydes with 3‐amino‐2‐alkylquinazolin‐4(3H)‐ones in glacial acetic acid with good yields (85%–94%). The structures of t...

In this study, it was aimed to synthesize novel molecules containing potential biological active phenolic Mannich base moiety and evaluate the inhibition properties against α-glycosidase (α-Gly) and acetylcholinesterase (AChE). For this purpose, phenolic aldehydes (1–3) were synthesized from 4-hydroxy-3-methoxy benzaldehyde (vanillin) according to...

3‐Amino‐2‐ethylquinazolin‐4(3H)‐one (3) was synthesized in two steps from the reaction of amide (2), which was obtained from the treatment of methyl anthranilate (1) with propionyl chloride, with hydrazine. From the reaction of 3‐amino‐2‐ethylquinazolin‐4(3H)‐one (3) with various aromatic aldehydes, novel benzylidenaminoquinazolin‐4(3H)‐one (3a–n)...

In this study, it was investigated how the Lipase enzyme will be affected by phenolic Mannich bases and some derivatives of them heterocyclic Schiff base.

In this study, its planned to synthesis of O-acyl, O-sulfonyl and C-Mannich base derivatives of acetovanillon (4-hydroxy-3-methoxy acetophenone) and investigate their effects on Endo-1,4-β xylanase enzyme obtained recombinantly from Bacillus subtilis (BTX6).

In this study, eight new Schiff base derivatives (2a-h) were synthesized and their inhibition activities against Acetylcholinesterase (AChE), Butyrylcholinesterase (BChE), α-Glucosidase and Lactoperoxidase (LPO) were investigated. Structures of the synthesized compounds were characterized using 1 H and 13 C nuclear magnetic resonance (NMR), infrare...

In this paper, eight novel 1-(morpholine-4-yl-methyl)-3-alkyl(aryl)-4-[4-(dimethylamino)-benzylidenamino]-4,5-dihydro-1H-1,2,4-triazol-5-ones (2) were obtained by the reactions of 3-alkyl(aryl)-4-[4-(dimethylamino)-benzylidenamino]-4,5-dihydro-1H-1,2,4-triazol-5-ones (1) with formaldehyde and morpholine. The novel synthesized compounds were identif...

We aimed a novel electrochemical sensor based on iron nanoparticles (FeNPs) and 2-aminoethanethiol (2-AET) functionalized graphene oxide (2-AETGO). The methods such as transmission electron microscope (TEM), scanning electron microscope (SEM), x-ray photoelectron spectroscopy (XPS), reflection-absorption infrared spectroscopy (RAIRS), electrochemic...