Artificial intelligence and clinical guidance in male reproductive health: ChatGPT4.0's AUA/ASRM guideline compliance evaluation.

BACKGROUND: Male infertility is defined as the inability of a male to achieve a pregnancy in a fertile female by the American Urological Association (AUA) and the American Society for Reproductive Medicine (ASRM). Artificial intelligence, particularly in language processing models like ChatGPT4.0, offers new possibilities for supporting clinical decision-making. This study aims to assess the effectiveness of ChatGPT4.0 in responding to clinical queries regarding male infertility, which is aligned with AUA/ASRM guidelines. METHODS: This observational study employed a design to evaluate the performance of ChatGPT4.0 across 1073 structured clinical queries categorized into true/false, multiple-choice, and open-ended. Two independent reviewers specializing in reproductive medicine assessed the responses using a six-point Likert scale to evaluate accuracy, relevance, and guideline adherence. RESULTS: In the true/false category, the initial accuracy was 92%, which increased to 94% by the end of the study period. For multiple-choice questions, accuracy improved from 85% to 89%. The most significant gains were seen in open-ended questions, where accuracy rose from 78% to 86%. Initially, some responses did not fully align with the AUA/ASRM guidelines. However, by the end of the 60 days, these responses had become more comprehensive and clinically relevant, indicating an improvement in the model's ability to generate guideline-conformant answers (p < 0.05). The depth and accuracy of responses for higher difficulty questions also showed enhancement (p < 0.01). CONCLUSION: ChatGPT4.0 can serve as a valuable support tool in managing male infertility, providing reliable, guideline-based information that enhances the accuracy of clinical decision-making tools and supports patient education.

A pioneer Turkish urologist-medical historian (Saim Erkun 1901-1949) and his one-century-old review about prostate.

Saim Erkun (1901-1949) was born in Manisa at Aegean region of Anatolia as an Ottoman citizen. While his early life was spent in late Ottoman times at military actions including military prison camp in British colony; India, his active professional productive period was in early Turkish republic period (Est. 1923, centenary). He had a good education period for medicine with the help of his good level of all main World scientific languages such as French, German, and English. Besides his main profession, he was also interested in Ottoman urological medicine around the conquer of Istanbul and allocated them a space in his books in 1930s. He was one of the earliest urology resident (1929-1933, Istanbul) of modern medicine in Turkey. He performed many urological procedures and published the outcomes following modern scientific algorithms, furthermore, there have been urological books including "history" partly referring to antique Ottoman literature among his publications. In this manuscript we focused on the magic word of Urology forever; "Prostate," among his essays. Turkish medicine, particularly urology, renewed itself by some intelligent hard working young clinicians such as Saim Erkun, immediately after the short struggling by means of establishment process of modern Turkiye after World War I by the collapsing of old Ottoman Empire. Furthermore, we think that the stunning special word of urology, "prostate," should especially be mentioned to emphasize the importance of this beginning.

Rigicon disposable Furlow insertion tool has the potential to decrease infection rates after inflatable penile prosthesis implantation.

Furlow insertion tool is frequently used during the insertion of the inflatable penile prosthesis cylinders inside the corporal bodies. Although these devices are completely disassembled and separately sterilized after each operation, the residual blood clots and tissues after inadequate cleaning may become the primary sources of penile prosthesis infection. In order to minimize the risk of infection, Rigicon, Inc. (NY, USA) has developed the first disposable Furlow insertion tool. Head-to-head comparison studies with conventional and disposable Furlow insertion tools are necessary to confirm if there is a significant difference in post-implant infection rates.

The Evaluation of the First Bahname Written in Turkish in the Ottoman Era Concerning Current Urology.

OBJECTIVE: Our study investigated the oldest known Turkish bahname, translated by Musa b. Mes'ud, in comparison with the current literature. MATERIAL AND METHODS: First, the original manuscript of the translation was transcribed in Latin. The final version of the text was analyzed in the results. In discussion, findings were examined and interpreted within the framework of current knowledge of sexology, urology, and andrology. RESULTS: Although the work mostly mentions supportive and therapeutic practices in sexual health, it also provides advice on sexuality and sexual life, discussing several topics regarding sexual intercourse types, explaining which ones are good or harmful, and their timing or frequency. The author recommends many foods and compounds or specific drugs and ointments to enhance sexual stamina and avoid erectile dysfunc tion. In addition, he also tries to find solutions to some other sexual health problems related to men and women. These issues are generally evaluated in the context of health; a religious perspective is also provided when needed. CONCLUSION: Interestingly, the author's recommendations on sexual health and herbal or animal drugs are consistent with the current literature. Nevertheless, some information and suggestions in works are entirely irrational and unscientific. Consequently, this study is an original investigation of the first translated bahname into Turkish. There is no other study examining the bahnames with this method. Thus, we believe that our work will be a significant contribution to the research literature.

Molecular docking and inhibition profiles of some antibiotics on lactoperoxidase enzyme purified from bovine milk.

Antibiotics are generally used for human and veterinary applications to preserve and to control microbial diseases. Milk has a biologically significant enzyme known as lactoperoxidase (LPO) that is a member of peroxidase family. In metabolism, LPO has ability to catalyze the transformation of thiocyanate (SCN-) to hypothiocyanite (OSCN-) that is an antibacterial agent and the reaction occurs with hydrogen peroxide. In this work, LPO inhibition effects of some antibiotics including cefazolin, oxytetracycline, flunixin meglumine, cefuroxime, tylosin, vancomycin, chloramphenicol and lincomycin were tested. Among the antibiotics cefazolin was indicated the strongest inhibitory efficacy. The half maximal inhibitory concentration (IC50) and the inhibition constant (Ki) values of cefazolin were found as 8.19 and 34.66 µM, respectively. It was shown competitive inhibition. 5-Methyl-1,3,4-thiadiazol-2-yl moiety activity plays a key role in the inhibition mechanism of cefazolin.Communicated by Ramaswamy H. Sarma.

Possible inhibition mechanism of dobutamine hydrochloride as potent inhibitor for human glucose-6-phosphate dehydrogenase enzyme.

Glucose-6-phosphate dehydrogenase (G6PD) is the first rate-limiting enzyme in the pentose phosphate pathway. One of the enzyme's most important functions is the production of a reducing agent that is essential for preserving the level of reduced glutathione (GSH). However, some chemicals, such as industrial waste and the active ingredients of several drugs, can cause reduction or blockage in this enzyme's activity. This case causes the occurrence of anemia by damaging erythrocytes. In this study, the G6PD enzyme was purified 21,981 fold with affinity chromatography and the effects of the active ingredients of some antiarrhythmic drugs on enzyme activity were investigated with in vitro and in silico methods. We found that dobutamine hydrochloride significantly decreased enzyme activity and its inhibitory constant (Ki) value was calculated as 19.02 ± 4.83 mM. The in vitro study results also show that dobutamine hydrochloride is a potent inhibitor of enzyme activity. We also found that dobutamine hydrochloride inhibits the hG6PD enzyme's activity by causing structural alterations in substrate and coenzyme binding sites.Communicated by Ramaswamy H. Sarma.

Design, synthesis, molecular docking, and some metabolic enzyme inhibition properties of novel quinazolinone derivatives.

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) derivatives were synthesized. The structures of the novel molecules were characterized using infrared spectroscopy, nuclear magnetic resonance spectroscopy (1 H-NMR and 13 C-NMR), and high-resolution mass spectroscopy. The novel compounds were tested against some metabolic enzymes, including α-glucosidase (α-Glu), acetylcholinesterase (AChE), and human carbonic anhydrases I and II (hCA I and II). The novel compounds showed Ki values in the range of 244-988 nM for hCA I, 194-900 nM for hCA II, 30-156 nM for AChE, and 215-625 nM for α-Glu. The binding affinities of the most active compounds were calculated as -7.636, -6.972, -10.080, and -8.486 kcal/mol for hCA I, hCA II, AChE, and α-Glu enzymes, respectively. The aromatic ring of the quinazoline moiety plays a critical role in the inhibition of the enzymes.

A study on the effects of inhibition mechanism of curcumin, quercetin, and resveratrol on human glutathione reductase through in vitro and in silico approaches.

Glutathione reductase (GR) is a major antioxidant enzyme essential to maintain GSH/GSSG ratio by catalyzing recovery of reduced glutathione (GSH) from oxidized glutathione (GSSG). Because of this vital task, the inhibition of GR is an important target in the treatment of many diseases, so we aimed to identify natural and new GR inhibitors to be guide for drug design.For this purpose, two different approaches were used. The first one is in vitro inhibition, the first phase of which was the purification of the enzyme from human erythrocyte by 2', 5'-ADP Sepharose 4B affinity chromatography, and then the in vitro inhibition effects of curcumin, quercetin, and resveratrol were examined. The second one is in silico study, which was performed to elucidate the drug-likeness, active site identification and inhibition mechanisms of these compounds.hGR was isolated from human erythrocytes with 7.036 EU/mg protein specific activity and 48.97% yield. Then, IC50 values were as 17.25 ± 3.8 µM, 57.8 ± 14.2 µM, and 520 ± 96.7 µM for curcumin, quercetin, and resveratrol respectively. Docking studies of compounds were performed against hGR receptors with induced-fit docking method. The compound showed Glide score as 10.519 kcal/mol, -9.789, and -8.133 respectively.In conclusion, it was seen that curcumin is the much better inhibitor than quercetin and resveratrol for hGR according to both in vitro and in silico studies. Curcumin, a potential inhibitor of hGR, can be used in drug design to target the glutathione system in cellular injury.Communicated by Ramaswamy H. Sarma.

Inhibition effects of isoproterenol, chlorpromazine, carbamazepine, tamoxifen drugs on glutathione S-transferase, cholinesterases enzymes and molecular docking studies.

Nowadays, inhibition of acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and glutathione S-transferases (GSTs) have been a very crucial issue for pharmacological treatments of several disasters. Herein, we investigated inhibition effects of Tamoxifen (TAM), Isoprenaline (ISO), Chlorpromazines (CPZ) and Carbamazepine (CBZ) on GST, AChE, BChE and then molecular structures and active sides of the tested drugs by molecular docking process. The enzyme activity results showed that nearly the whole tested drugs inhibited GST, BChE, AChE efficiently. Chlorpromazine was found to be the best inhibitor for the GST enzyme and the Ki value of this drug was found to be 42.83 ± 8.52 nM. Besides, Isoproterenol drug with the Ki value of 51.80 ± 9.44 nM was found to be the most effective inhibitor on the AChE enzyme. Molecular docking studies showed that the receptor-binding sites of GST, AChE, and BChE were found to 1.069, 1.090, and 1.15 of Sitecore and 0.992, 1.113, and 1.217 of Dscore, respectively. The method was validated by doing validation studies and these validations revealed that re-docked ligands located a very closed position with co-crystallized ligand into the active site for all receptors. Calculation studies for determining the possible enzyme inhibition mechanism with the used drugs revealed that amino and aromatic ring in the structure of the drugs used are effective in inhibition reactions.Communicated by Ramaswamy H. Sarma.

Neuroprotective effect of chrysin on isoniazid-induced neurotoxicity via suppression of oxidative stress, inflammation and apoptosis in rats.

Isoniazid (INH) is among the most important anti-tuberculosis agents widely prescribed. However, its clinical use is restricted due to its severe side effects associated with neurotoxicity. The aim of the present study was to investigate the neuroprotective effects of chrysin (CR), a natural antioxidant, against INH-induced neurotoxicity in rats. The rats were treated orally with INH (400 mg/kg body weight) alone or with CR (25 and 50 mg/kg body weight) for 7 consecutive days. INH administration significantly increased brain lipid peroxidation and resulted in a significant decrease in antioxidant biomarkers including superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GPx) and glutathione (GSH). INH treatment also increased levels of nuclear factor kappa B (NF-κB), tumor necrosis factor-α (TNF-α), glial fibrillary acidic protein (GFAP) and activities of p38α mitogen-activated protein kinase (p38α MAPK) while decreasing levels of neural cell adhesion molecule (NCAM). Double immunofluorescence expressions of c-Jun N-terminal kinase (JNK) and Bcl-2 associated X protein (Bax) in brain tissues were increased after INH administration. Furthermore, INH increased mRNA expression levels of nuclear factor erythroid 2-related factor 2 (Nrf-2), heme oxygenase-1 (HO-1), NAD(P)H: quinone oxidoreductase 1 (NQO1), glutamate-cysteine ligase modifier subunit (Gclm), glutamate cysteine ligase catalytic subunit (Gclc), NF-κB, TNF-α, interleukin-1ß (IL-1ß), interleukin-6 (IL-6) and GFAP in rat brain tissues. Co-treatment with CR increased anti-oxidant capacity as well as regulated inflammation and apoptosis in brain. Additionally, molecular docking results showed that CR had the potential to interact with the active sites of TNF-α and NFκ-B. In conclusion, CR improved INH-induced brain oxidative damage, inflammation and apoptosis, possibly through their antioxidant properties.

Novel cyclic thiourea derivatives of aminoalcohols at the presence of AlCl3 catalyst as potent α-glycosidase and α-amylase inhibitors: Synthesis, characterization, bioactivity investigation and molecular docking studies.

The article is devoted to the targeted synthesis and study of cyclic thiourea and their various new derivatives as new organic compounds containing polyfunctional group in the molecule. First time the reaction of the corresponding synthesized pyrimidinethione with 1,2-epoxy-3-chlorpropane at the presence of AlCl3 catalyst in 75-80% yield alkyl-1-(3-chloro-2-hydroxypropyl)-4-alkyl-6-phenyl-2-thioxo-1,2,5,6- tetrahydropyrimidine-5-carboxylates. In the next stage, new cyclic thiourea derivatives of aminoalcohols were synthesised from the reaction of chlorinated derivatives of pyrimidinethiones with single amines and their structures were investigated by spectroscopic methods. In this study, a series of novel compounds were tested towards some metabolic enzymes including α-glycosidase (α-Gly) and α-amylase (α-Amy) enzymes. Novel compounds showed Kis in ranging of 10.43 ± 0.94-111.37 ± 13.25 µM on α-glycosidase and IC50 values in ranging of 14.38-106.51 µM on α-amylase. The novel cyclic thiourea derivatives of aminoalcohols had effective inhibition profiles against all tested metabolic enzymes. Binding affinity and inhibition mechanism of the most active compounds were detected with in silico studies and have shown that 2-Hydroxypropyl and butan-1-aminium moieties play a key role for inhibition of the enzymes.

Evaluation of some thiophene-based sulfonamides as potent inhibitors of carbonic anhydrase I and II isoenzymes isolated from human erythrocytes by kinetic and molecular modelling studies.

BACKGROUND: Thiophene(s) are an important group in therapeutic applications, and sulfonamides are the most important class of carbonic anhydrase (CA) inhibitors. In this study, inhibition effects of some thiophene-based sulfonamides on human erythrocytes carbonic anhydrase I and II isoenzymes (hCA-I and hCA-II) were investigated. Thiophene-based sulfonamides used in this study showed potent inhibition effect on both isoenzymes at very small concentrations. MATERIALS AND METHODS: We report on the purification of the carbonic anhydrase I and II isoenzymes (hCA-I and hCA-II) using affinity chromatography method. The inhibition effect of the thiophene-based sulfonamides was determined by IC50 and Ki parameters. A molecular docking study was performed for each molecule. RESULTS: Thiophene-based sulfonamides showed IC50 values of in the range of 69 nM to 70 µM against hCA-I, 23.4 nM to 1.405 µM against hCA-II. Ki values were in the range of 66.49 ± 17.15 nM to 234.99 ± 15.44 µM against hCA-I, 74.88 ± 20.65 nM to 38.04 ± 12.97 µM against hCA-II. Thiophene-based sulfonamides studied in this research showed noncompetitive inhibitory properties on both isoenzymes. To elucidate the mechanism of inhibition, a molecular docking study was performed for molecules 1 and 4 exhibiting a strong inhibitory effect on hCA-I and hCA-II. The compounds inhibit the enzymes by interacting out of catalytic active site. The sulfonamide and thiophene moiety played a significant role in the inhibition of the enzymes. CONCLUSION: We hope that this study will contribute to the design of novel thiophene-based sulfonamide derived therapeutic agents that may be carbonic anhydrase inhibitors in inhibitor design studies.

Protective Effect of Udenafil Against Ischemia Reperfusion Injury Due to Testicular Torsion/Detorsion in Rat Model.

OBJECTIVE: Testicular torsion causes migration of neutrophils to the ischemic region and formation of free oxygen radicals that have a critical effect on ischemic reperfusion (I/R) injury. Udenafil is a selective, strong, and reversible inhibitor of phosphodiesterase type enzyme. In our study, we evaluate the protective effect of udenafil against reperfusion injury due to I/R. MATERIALS AND METHODS: Twenty-one male, adult, Wistar-Albino rats aged 8 months were randomly divided into three groups; sham, I/R, and I/R+udenafil. One hour before the detorsion operation, the sham and I/R groupssaline, and I/R+udenafil groups were administered 2 mg/kg udenafil intraperitoneally. Blood samples were collected to evaluate the inflammatory mediators. Spermatogenic factors were evaluated according to Johnsen criteria. RESULTS: Histopathological and molecular parameters from all groups were compared. Mean values of TNF-α and IL-1ß in venous blood samples were calculated. We observed that TNF-a values were statistically significantly increased in the I/R group than those in sham groups, and these values were decreased with udenafil treatment Furthermore, the glutathione peroxidase (GPx) level was statistically significantly decreased in the I/R group, and treatment with udenafil prevented this decrease. Evaluation of spermatogenesis using the Johnsen scoring system showed no statistically significant difference in mean scores between the groups. CONCLUSION: We concluded that deterioration of biochemical and histopathological parameters are reversed, and injury due to I/R in testicle tissue may be decreased with udenafil treatment. Results of this experimental study show that efficacy of the udenafil treatment in testis torsion should be investigated.

N-Substituted pyrimidinethione and acetophenone derivatives as a new therapeutic approach in diabetes.

In this study, compounds with 4-hydroxybutyl, 4-phenyl, 5-carboxylate, and pyrimidine moieties were determined as α-glycosidase inhibitors. N-Substituted pyrimidinethione and acetophenone derivatives (A1-A5, B1-B11, and C1-C11) were good inhibitors of the α-glycosidase enzyme, with Ki values in the range of 104.27 ± 15.75 to 1,004.25 ± 100.43 nM. Among them, compound B7 was recorded as the best inhibitor, with a Ki of 104.27 ± 15.75 nM against α-glycosidase. In silico studies were carried out to clarify the binding affinity and interaction mode of the compounds with the best inhibition score against α-glycosidase from Saccharomyces cerevisiae. Compounds B7 (S) and B11 (R) exhibited a good binding affinity with docking scores of -8.608 and 8.582 kcal/mol, respectively. The docking results also showed that the 4-hydroxybutyl and pyrimidinethione moieties play a key role in S. cerevisiae and human α-glycosidase inhibition.

Lactoperoxidase inhibition of some natural phenolic compounds: Kinetics and molecular docking studies.

The inhibition effects of some phenolic compounds from natural products such as taxifolin, resveratrol, olivetol, cynarine, and phloretin on bovine milk lactoperoxidase (LPO) enzyme were examined. For this aim, LPO was purified by the affinity chromatography technique with a yield of 77.68% in 421.32 times. The kinetic value, Ki , was calculated from the equations obtained from drawn graphs. In order to discover inhibition mechanism of phenolic compounds, induced fit docking process was performed on the LPO receptors. The binding affinity of the compounds was calculated and at the best-scored ligand-receptor complex, residues responsible for enzyme inhibition were detected. As a result, this molecule demonstrated the potential inhibitory effect on LPO. According to the results of kinetic study. It has shown a noncompetitive inhibition effect, Phloretin's Ki value was determined by 48.89 ± 14.22 nM. PRACTICAL APPLICATIONS: There are natural antimicrobial systems, such as the lactoperoxidase (E.C.1.11.1.7; LPO) system, which eliminates the harmful effects of microorganisms in milk. The chemical reactions in this system are catalyzed by the LPO. In the dairy industry, the LPO system is considered critical for the preservation of pasteurized milk, yogurt, raw milk, and cheese. The system is used for improvement the protection condition of milk at high temperatures.

Novel 2-methylimidazolium salts: Synthesis, characterization, molecular docking, and carbonic anhydrase and acetylcholinesterase inhibitory properties.

In this work, structures of different imidazolium compounds were designed and synthesized. These compounds were synthesized from 2-methylimidazole and alkyl/aryl halides. Their structures were characterized by using 1H NMR, 13C NMR, FTIR spectroscopic techniques. All the synthesized compounds were tested for their inhibition activities on different enzymes. Inhibition experiments gave good and moderate results, proving their activities of these compounds as anticholinergics potential. These obtained novel 2-methylimidazolium salts (1a-e and 2a-e) molecules were effective inhibitors of the carbonic anhydrase I and II isozymes (hCA I and II) and acetylcholinesterase (AChE) enzymes with Ki values in the range of 26.45 ± 6.49-77.60 ± 9.53 nM for hCA I, 27.87 ± 5.00-86.61 ± 5.71 nM for hCA II, and 1.15 ± 0.19-8.89 ± 0.49 nM for AChE, respectively. AChE enzyme inhibitors are the most common drugs applied in the therapy of diseases such as senile dementia, Alzheimer's disease, ataxia, Parkinson's disease, and among others.

In vitro effects of standard antioxidants on lactoperoxidase enzyme-A molecular docking approach.

Lactoperoxidase (LPO), an antioxidant enzyme, is a natural antimicrobial system that eliminates the harmful effects of microorganisms in milk. It has a wide range of applications and is also preferred in cosmetic and clinical applications, as well as used in foods. The use of antioxidants is well recognized in the food and feed industries to improve the shelf life of products. This study aimed to determine the in vitro inhibition effects of Trolox, α-tocopherol, butylated hydroxyanisole, butylated hydroxytoluene, and propyl gallate, which are commonly used as antioxidants in food and pharmaceutical products. For this purpose, LPO was first purified in a single step using sepharose-4B-l-tyrosine-sulfanilamide affinity gel chromatography. Also, some inhibition parameters, including half-maximal inhibitory concentration (IC50 ), Ki values, and inhibition types, were calculated for each antioxidant molecule. The IC50 values of these molecules, which exhibited competitive inhibition, varied between 377.7 and 3397.8 nM. Molecular docking studies were also performed for all compounds. According to the binding scores, α-tocopherol was shown to exhibit the most effective inhibitor property (IC50 : 377.7 nM and Ki : 635.8 ± 16.8 nM) among the standard antioxidants used in this study. Inhibiting the LPO activity by standard antioxidants results in the weakening of the immune system during lactation, which is important for metabolism.

Pyrazole[3,4-d]pyridazine derivatives: Molecular docking and explore of acetylcholinesterase and carbonic anhydrase enzymes inhibitors as anticholinergics potentials.

Recently, the pyridazine nucleus has been widely studied in the field of particular and new medicinal factors as drugs acting on the cardiovascular system. Additionally, a number of thienopyridazines have been claimed to possess interacting biological macromolecules and pharmacological activities such as NAD(P)H oxidase inhibitor, anticancer, and identified as a novel allosteric modulator of the adenosine A1 receptor. The literature survey demonstrates that coumarin, 1,2-pyrazole benzothiazole, and 1,3- thiazole scaffolds are the most versatile class of molecules. In this study, a series of substituted pyrazole[3,4-d]pyridazine derivatives (2a-n) were prepared, and their structures were characterized by Mass analysis, NMR, and FT-IR. These obtained pyrazole[3,4-d]pyridazine compounds were very good inhibitors of the carbonic anhydrase (hCA I and II) isoenzymes and acetylcholinesterase (AChE) with Ki values in the range of 9.03 ±â€¯3.81-55.42 ±â€¯14.77 nM for hCA I, 18.04 ±â€¯4.55-66.24 ±â€¯19.21 nM for hCA II, and 394.77 ±â€¯68.13-952.93 ±â€¯182.72 nM for AChE, respectively. The possible inhibition mechanism of the best-posed pyrazole[3,4-d]pyridazine and pyrazole-3-carboxylic acid derivatives and their interaction with catalytic active pocket residues were determined based on the calculations.

The green synthesis and molecular docking of novel N-substituted rhodanines as effective inhibitors for carbonic anhydrase and acetylcholinesterase enzymes.

Recently, inhibition effects of enzymes such as acetylcholinesterase (AChE) and carbonic anhydrase (CA) has appeared as a promising approach for pharmacological intervention in a variety of disorders such as epilepsy, Alzheimer's disease and obesity. For this purpose, novel N-substituted rhodanine derivatives (RhAs) were synthesized by a green synthetic approach over one-pot reaction. Following synthesis the novel compounds, RhAs derivatives were tested against AChE and cytosolic carbonic anhydrase I, and II (hCAs I, and II) isoforms. As a result of this study, inhibition constant (Ki) were found in the range of 66.35 ±â€¯8.35 to 141.92 ±â€¯12.63 nM for AChE, 43.55 ±â€¯14.20 to 89.44 ±â€¯24.77 nM for hCA I, and 16.97 ±â€¯1.42 to 64.57 ±â€¯13.27 nM for hCA II, respectively. Binding energies were calculated with docking studies as -5.969, -5.981, and -9.121 kcal/mol for hCA I, hCA II, and AChE, respectively.