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AbstractDeposition of hydroxyapatite (HA) or alkaline phosphate crystals on soft tissues causes the pathological calcification diseases comprising of end-stage osteoarthritis (OA), ankylosing spondylitis (AS), medial artery calcification and tumour calcification. The pathological calcification is symbolised by increased concentration of tissue non-specific alkaline phosphatase (TNAP). An efficient therapeutic strategy to eradicate these diseases is required, and for this the alkaline phosphatase inhibitors can play a potential role. In this context a series of novel quinolinyl iminothiazolines was synthesised and evaluated for alkaline phosphatase inhibition potential. All the compounds were subjected to DFT studies where N-benzamide quinolinyl iminothiazoline (6g), N-dichlorobenzamide quinolinyl iminothiazoline (6i) and N-nitrobenzamide quinolinyl iminothiazoline (6j) were found as the most reactive compounds. Then during the in-vitro testing, the compound N-benzamide quinolinyl iminothiazoline (6g) exhibited the maximum alkaline phosphatase inhibitory effect (IC50 = 0.337 ± 0.015 µM) as compared to other analogues and standard KH2PO4 (IC50 = 5.245 ± 0.477 µM). The results were supported by the molecular docking studies, molecular dynamics simulations and kinetic analysis which also revealed the inhibitory potential of compound N-benzamide quinolinyl iminothiazoline (6g) against alkaline phosphatase. This compound can be act as lead molecule for the synthesis of more effective inhibitors and can be suggested to test at the molecular level.

Background: It is emphasized in medical education that assessment drives learning. In 2020, during the first COVID-19 lockdown, University College of Medicine and Dentistry made a shift towards Computer Based Assessments (CBAs) in order to facilitate learning. Objective: To determine undergraduate medical student’s perception for computer based assessment environment in medical school Methods: The cross-sectional descriptive study was conducted at the University of Lahore, Pakistan, from May 2022 to September 2022, and included undergraduate medical students who were requested to complete the Assessment Environment Questionnaire. Students' individual perception scores were calculated and the means of individual domains and global scores were compared in different academic years. SPSS version 23 was used for statistical analysis. Results: Of 574 participants, 20% of the participants were from 1st year, 20.7% were from second year, 20% from 3rd year, 19.9% from 4thyear and 19.3% from final year. Generally, the students perceived their assessment environment positive resulting in a global mean score of 67.6±13.7 out of the maximum 80. First year students scored significantly higher (P

Background and Objective: The essential goal of any medical school is to train medical graduates to work as independent clinicians. Inadequately prepared doctors put the well-being of patients at a great risk. The objective of the study was to evaluate the preparedness for independent clinical practice of house officers who graduated from medical schools with the traditional discipline-based curriculum, from both public and private sectors, and with high and low merit.Methods: A quantitative correlational study was conducted by using an already validated questionnaire. A total of 241 house officers who graduated from public and private sector medical schools from Lahore, Pakistan, with high and relatively low merit, were selected. The data from the filled responses were analyzed by using Statistical Package for the Social Sciences version 25.0Results: Of the 241 respondents, 152 (55.3%) were females and 89 (32.4%) were males. The mean age of the respondents was 24.19 ± 0.91 years. The difference in mean score between the public and private sectors was significant in the subscales of clinical skills, procedural skills, and patient management. Analysis of free-text responses showed a deficiency in procedural skills, communication skills, time management, and management of acutely ill patients in the emergency department in both classes of medical schools. Many graduates suggested early clinical exposure with hands-on training and the addition of modules of ethics and medical laws in the curriculum.Conclusion: The medical graduates lack pertinent training in professionalism, ethics, medical laws, and communication skills which may hamper their appropriate preparedness before dealing directly with the high turnover of patients during house jobs.

Introduction: In COVID-19 pandemic, whole of the medical education faced a paradigm shift. Majority of the medical schools shifted their academics online but fair conduction of assessments was still in question. Around the world, many techniques were applied and one was followed at University Medical and Dental College, Lahore (UCMD). Aims & Objectives: To assess the perception of students about modified version of OSPE (displayed on multimedia) so that to implement the same protocol in future by meeting the SOPs without affecting the academics. Place and duration of study: The study was carried out at UCMD, Lahore in year 2021 and was of 6 months duration. Material & Methods:150 students each from first and second year MBBS classes participated in this study. After following the strict SOPs of COVID-19, the students were settled in an auditorium and OSPE was displayed on multimedia screen instead of moving from one station to another as done previously. Feedback was taken from the students after the exam. Results: Response from the students was recorded and percentages were calculated which showed that majority of the students appreciated this modified version of OSPE. Conclusion: This study proved that modified Anatomy OSPE was an effective tool to grade the students without academic disturbance which was imminent in global pandemic and this method can be adapted henceforward.

Methylene blue (MB) is a most commonly used synthetic dye in the textile industry. It is an extremely carcinogenic phenothiazine derivative and therefore needs to be removed from the water bodies. In the present study, a single-step hydrothermal novel synthesis of carbon quantum dots (CQDs) extracted from biomass of chicken feathers has been performed, and the synthesized CQDs were applied to remove MB present in the aqueous samples. A number of techniques such as ultraviolet-visible (UV-Vis) spectroscopy, Fourier-transform infrared (FTIR) spectroscopy, scanning electron microscopy (SEM), energy-dispersive spectroscopy (EDS), and X-ray diffraction (XRD) were used to characterize the samples for the conformity purposes. SEM and XRD analysis showed that CQDs are highly crystalline and have spherical structures with an average particle diameter of 35 nm. In the presence of 0.2 g of synthesized CQDs, MB dye degraded drastically under the sunlight. The rate of degradation was studied by determining the absorbance of the degraded sample with time relevant to untreated sample. The % degradation achieved during first 60 min of time was approximately 92% which increased minimally to a value of only 95% after 100 min of time. The ease of synthesis of carbon dots at low cost contributes hugely to their utilizations as an efficient photocatalyst for the degradation of aqueous pollutants. The opted approach to synthesize CQDs is cost-effective and eco-friendly and demonstrates excellent potential to remove MB from the aqueous samples.

Introduction: The COVID-19 pandemic influenced education system worldwide. This change was unusual for both students and anatomists. The present study is conducted to perceive online learning experience of 1st& 2nd year MBBS students in a modular system comparing online SGD & lectures with face to face. Objectives: To assess how medical students of 1st and 2nd year MBBS perceive the experience of learning Anatomy online in an integrated modular system, their attitude towards online small group discussions (SGD) and online Interactive lectures by comparing with face-to-face learning anatomy. Place and duration of study: The study was conducted in the Department of Anatomy at University College of Medicine, University of Lahore during academic year of 2021 over a period of six months from March 2021. Material & Methods: This descriptive cross-sectional study was conducted by using a Questionnaire validated by five medical educationists. The sampling was done by nonprobability convenience technique. For a confidence level of 97%, sample size was 197. A total of 202 students from 1st & 2nd year MBBS, were asked to fill in a Questionnaire with Likert scale of 5, anonymously after taking informed consent, regarding online learning Anatomy through Zoom by comparing online SGD and Interactive lectures with face-to-face learning during COVID-19 pandemic. Data was analyzed using SPSS (version 28) software, p value ?0.05 was considered significant. Results: A total of 202 responses were received of which 197 responses were complete. Of which 56 were from 1styear while 141 were from 2nd Year MBBS. Some students did not answer some questions. Percentages were calculated against student responses, for missing data the percentages were calculated from total number of responses to each question answered. p values calculated were not significant but overall students did not prefer online learning over face to face learning. Conclusion: Our present study concludes that learning anatomy online is challenging. Overall students did not value online learning more than face-to-face learning in terms of flexibility, freedom, interaction with teachers, lack of hands-on practice and concepts, although they enjoyed the leisure of self-study with whole study material available to them at any time.

Using a big data set of venture capital financing and related startup firms from Crunchbase, this paper develops a machine-learning model called CapitalVX (for “Capital Venture eXchange”) to predict the outcomes for startups, i.e., whether they will exit successfully through an IPO or acquisition, fail, or remain private. Using a large feature set, the out-of-sample accuracy of predictions on startup outcomes and follow-on funding is 80–89%. This research suggests that VC/PE firms may be able to benefit from using machine learning to screen potential investments using publicly available information, diverting this time instead into mentoring and monitoring the investments they make.

The designed bi-heterocyclic sulfonamides were synthesized through a two-step protocol and their structures were ascertained by spectral techniques including IR, 1H NMR and 13C NMR along with CHN analysis. The in vitro inhibitory effects of these sulfonamides were evaluated against tyrosinase and kinetics mechanism was analyzed by Lineweaver–Burk plots. The binding modes of these molecules were ascribed through molecular docking studies. These synthesized bi-heterocyclic molecules were identified as potent inhibitors relative to the standard (kojic acid) and compound 5 inhibited the tyrosinase non-competitively by forming an enzyme-inhibitor complex. The inhibition constant Ki (0.09 µM) for compound 5 was calculated from Dixon plots. Computational results also displayed that all compounds possessed good binding profile against tyrosinase and interacted with core residues of target protein.

The present study describes the anti‐melanogenesis effect of Acemetacin (ACE). Essential protein (melanin) that is vital for the skin for defense from UV rays. In the present research, emerging drug ACE was examined for its melanin inhibition using three different (in vitro, in vivo and computational) methods. ACE showed remarkable potency (IC50 = 0.353 ± 0.003 µM) against tyrosinase in the comparison of standard, kojic acid (IC50 = 16.841 ± 1.161 µM) and ACE exhibited competitive inhibition. In the in vivo study zebrafish embryos were exposed with 5, 10, 15 and 20 µM of ACE and same doses for positive control (Kojic Acid). At 72 h treatment, ACE expressively (P

Carbonic anhydrases (CA), having Zn2+ metal atoms, are responsible for the catalysis of CO2 and water to bicarbonate and protons. Any abnormality in the functioning of these enzymes may lead to morbidities such as glaucoma and different types of cancers including brain, renal and pancreatic carcinomas. To cope with the lack of presence of a promising therapeutic agent against these cancers, searching for an efficient and suitable carbonic anhydrase inhibitor is crucial. In the current study, ten novel 3-ethylaniline hybrid imino-thiazolidinones were synthesized and characterized by FTIR, NMR (1H, 13C), and mass spectrometry. Synthesis was carried out by diethyl but-2-ynedioate cyclization and different acyl thiourea substitutions of 3-ethyl amine. The CA (II) enzyme inhibition profile for all synthesized derivatives was determined. It was observed that compound 6e demonstrated highest inhibition of CA-II with an IC50 value of 1.545 ± 0.016 µM. In order to explore the pharmacophoric properties and develop structure activity relationship, in silico screening was performed. In silico investigations included density functional theory (DFT) studies, pharmacophore-guided model development, molecular docking, molecular dynamic (MD) simulations, and prediction of drug likeness scores. DFT investigations provided insight into the electronic characteristics of compounds, while molecular docking determined the binding orientation of derivatives within the CA-II active site. Compounds 6a, 6e, and 6g had a reactive profile and generated stable protein-ligand interactions with respective docking scores of −6.12, −6.99, and −6.76 kcal/mol. MD simulations were used to evaluate the stability of the top-ranked complex. In addition, pharmacophore-guided modeling demonstrated that compound 6e produced the best pharmacophore model (HHAAARR) compared to standard brinzolamide. In vitro and in silico investigations anticipated that compound 6e would be an inhibitor of carbonic anhydrase II with high efficacy. Compound 6e may serve as a potential lead for future synthesis that can be investigated at the molecular level, and additional in vivo studies are strongly encouraged.

To develop new alkaline phosphatase inhibitors (ALP), a series of pyrazolo-oxothiazolidine derivatives were synthesized and biologically assessed, and the results showed that all of the synthesized compounds significantly inhibited ALP. Specifically, compound 7g displayed the strongest inhibitory activity (IC50 = 0.045 ± 0.004 μM), which is 116-fold more active than monopotassium phosphate (IC50 = 5.242 ± 0.472 μM) as a standard reference. The most potent compound among the series (7g) was checked for its mode of binding with the enzyme and shown as non-competitively binding with the target enzyme. The antioxidant activity of these compounds was examined to investigate the radical scavenging effect. Moreover, the MTT assay method was performed to evaluate their toxic effects on the viability of MG-63 human osteosarcoma cells, and all compounds have no toxic effect on the cells at 4 μM. Computational research was also conducted to examine the binding affinity of the ligands with alkaline phosphatase, and the results revealed that all compounds showed good binding energy values within the active site of the target. Therefore, these novel pyrazolo-oxothiazolidine derivatives might be employed as promising pharmacophores for potent and selective alkaline phosphatase inhibitors.

Urease is an amidohydrolase enzyme that is responsible for fatal morbidities in the human body, such as catheter encrustation, encephalopathy, peptic ulcers, hepatic coma, kidney stone formation, and many others. In recent years, scientists have devoted considerable efforts to the quest for efficient urease inhibitors. In the pharmaceutical chemistry, the thiourea skeleton plays a vital role. Thus, the present work focused on the development and discovery of novel urease inhibitors and reported the synthesis of a set of 1-aroyl-3-[3-chloro-2-methylphenyl] thiourea hybrids with aliphatic and aromatic side chains 4a–j. The compounds were characterized by different analytical techniques including FT-IR, 1H-NMR, and 13C-NMR, and were evaluated for in-vitro enzyme inhibitory activity against jack bean urease (JBU), where they were found to be potent anti-urease inhibitors and the inhibitory activity IC50 was found in the range of 0.0019 ± 0.0011 to 0.0532 ± 0.9951 μM as compared to the standard thiourea (IC50 = 4.7455 ± 0.0545 μM). Other studies included density functional theory (DFT), antioxidant radical scavenging assay, physicochemical properties (ADMET properties), molecular docking and molecular dynamics simulations. All compounds were found to be more active than the standard, with compound 4i exhibiting the greatest JBU enzyme inhibition (IC50 value of 0.0019 ± 0.0011 µM). The kinetics of enzyme inhibition revealed that compound 4i exhibited non-competitive inhibition with a Ki value of 0.0003 µM. The correlation between DFT experiments with a modest HOMO-LUMO energy gap and biological data was optimal. These recently identified urease enzyme inhibitors may serve as a starting point for future research and development.

Novel drug development is onerous, time consuming and overpriced process with particularly low success and relatively high enfeebling rates. To overcome this burden, drug repositioning approach is being used to predict the possible therapeutic effects of FDA approved drugs in different diseases. Herein, we designed a computational and enzyme inhibitory mechanistic approach to fetch the promising drugs from the pool of FDA approved drugs against AD. The binding interaction patterns and conformations of screened drugs within active region of AChE were confirmed through molecular docking profiles. The possible associations of selected drugs with AD genes were predicted by pharmacogenomics analysis and confirmed through data mining. The stability behaviour of docked complexes (Drugs-AChE) were checked by MD simulations. The possible therapeutic potential of repositioned drugs against AChE were checked by in vitro analysis. Taken together, Cinitapride displayed a comparable results with standard and can be used as possible therapeutic agent in the treatment of AD.

In the study presented here, a novel chlorobenzylated bi-heterocyclic hybrid molecule (7) was synthesized and its structural confirmation was carried out by IR, 1H-NMR, 13C-NMR and CHN analysis data. This compound 7 was subjected to biological study with B16F10 mouse melanoma cells. The anti-proliferative results showed that 7 showed no significant toxicity at concentrations ranging of 0–44 μM. The treatment of B16F10 cells with 7 at aforementioned concentration range indicated that migration of cells was significantly lower than that of the control cells in a dose dependent manner. The possible migration inhibitory effect of these melanoma cells was further evaluated through gelatinolytic activity of MMP-2 and MMP-9 secreted from B16F10 cells. It was inferred from our results that 7 was not affecting the expression and activity of these enzymes. Some other zinc-dependent matrix metalloproteinases (MMPs) were involved in the inhibitory progression. Taken together, compound 7 inhibited migrations of B16F10 mouse melanoma cells. Therefore, it may deserve consideration as a potential agent for the treatment of cancer. Keywords: 2-Aminothiazole, Triazole, Anti-proliferation, Matrix metalloproteinase, Zymography

While the recent technological advancements have enabled instructors to deliver mathematical concepts and theories beyond the physical boundaries innovatively and interactively, poor performance and low success rate in mathematic courses have always been a major concern of educators. More specifically, in an online learning environment, where students are not physically present in the classroom and access course materials over the network, it is toilsome for course coordinators to track and monitor every student’s academic learning and experiences. Thus, automated student performance monitoring is indispensable since it is easy for online students, especially those underperforming, to be “out of sight,” hence getting derailed and off-track. Since student learning and performance are evolving over time, it is reasonable to consider student performance monitoring as a time-series problem and implement a time-series predictive model to forecast students’ educational progress and achievement. This research paper presents a case study from a higher education institute where interaction data and course achievement of a previously offered online course are used to develop a time-series predictive model using a Long Short-Term Memory network, a special kind of Recurrent Neural Network architecture. The proposed model makes predictions of student status at any given time of the semester by examining the trend or pattern learned in the previous events. The model reported an average classification accuracy of 86 and 84% with the training dataset and testing dataset, respectively. The proposed model is trialed on selected online math courses with exciting yet dissimilar trends recorded.

Mathematics is the engine, vehicle, driver, and language of today’s initiatives, innovations, and human endeavors. In this mathematical-driven world, the ability to perform mathematical tasks and logical reasoning is also essential in solving quotidian tasks and problems. Therefore, mathematical competency and problem-solving skills are kept as an integral component in almost every educational curriculum around the globe. However, there are numerous stumbling blocks along the way to successful teaching, conducive learning environment, and good student performances in almost all disciplines, but more prevalent and visible in mathematics. The major concerns of educators responsible for teaching mathematics and mathematics-related courses are to find effective and innovative ways to deliver mathematical content, to extend the concepts and theories beyond the classrooms, to integrate mathematics with important concepts such as gamification, data mining, learning analytics, deep learning, and effective tools such as mobile devices, learning management systems, and digital technology, and to maintain a good record of students’ performance. In online deliveries, these concerns are further escalated due to no or limited one-to-one interactions and lack of face time, to mention a few. This article investigates the efficacy and effectiveness of traditional and innovative pedagogical practices used in online mathematic courses at the University of the South Pacific (USP). It examines the interdependence of embedded activities and students’ achievement. The results indicate that these online mathematics courses were highly dominated by conventional approaches and were less interactive and engaging, resulting in lower success rates when compared to the courses from other disciplines. To recommend possible ways to enhance the quality of learning and teaching in online mathematics courses, selected online courses from the information system discipline were explored. The reasons for the high online presence in the course were investigated and activities that could lead to collaborative and active learning beyond the passive materials were data mined. The evidence drawn from the statistical analysis highlights the importance of including selected interactive and engaging activities in online learning space of mathematics courses to promote student engagement and help create a sense of community among geographically dispersed students. Overall, based on the observations and theoretical foundation from literature, it can be said that including regular and frequent active assessment strategies, such as weekly quizzes and discussion forums, could extend and promote interactive and engaging learning in online learning space.

A series of nine novel 1,2,4-triazole based compounds were synthesized through a multistep reaction pathway and their structures were scrutinized by using spectral methods such as FTIR, LC-MS, 1H NMR, and 13C NMR. The synthesized derivatives were screened for inhibitory activity against the mushroom tyrosinase and we found that all the synthesized compounds demonstrated decent inhibitory activity against tyrosinase. However, among the series of compounds, N-(4-fluorophenyl)-2-(5-(2-fluorophenyl)-4-(4-fluorophenyl)-4H-1,2,4-triazol-3-ylthio) acetamide exhibited more prominent activity when accompanied with the standard drug kojic acid. Furthermore, the molecular docking studies identified the interaction profile of all synthesized derivatives at the active site of tyrosinase. Based on these results, N-(4-fluorophenyl)-2-(5-(2-fluorophenyl)-4-(4-fluorophenyl)-4H-1,2,4-triazol-3-ylthio) acetamide could be used as a novel scaffold to design some new drugs against melanogenesis.

This article describes the design and synthesis of a series of novel amantadine-thiourea conjugates (3a–j) as Jack bean urease inhibitors. The synthesized hybrids were assayed for their in vitro urease inhibition. Accordingly, N-(adamantan-1-ylcarbamothioyl)octanamide (3j) possessing a 7-carbon alkyl chain showed excellent activity with IC50 value 0.0085 ± 0.0011 µM indicating that the long alkyl chain plays a vital role in enzyme inhibition. Whilst N-(adamantan-1-ylcarbamothioyl)-2-chlorobenzamide (3g) possessing a 2-chlorophenyl substitution was the next most efficient compound belonging to the aryl series with IC50 value of 0.0087 ± 0.001 µM. The kinetic mechanism analyzed by Lineweaver–Burk plots revealed the non-competitive mode of inhibition for compound 3j. Moreover, in silico molecular docking against target protein (PDBID 4H9M) indicated that most of the synthesized compounds exhibit good binding affinity with protein. The compound 3j forms two hydrogen bonds with amino acid residue VAL391 having a binding distance of 1.858 Å and 2.240 Å. The interaction of 3j with amino acid residue located outside the catalytic site showed its non-competitive mode of inhibition. Based upon these results, it is anticipated that compound 3j may serve as a lead structure for the design of more potent urease inhibitors.

Context: Ostericum koreanum (Maxim.) Kitagawa (Apiaceae) roots are traditionally used as an analgesic and antiulcer agent. However, the antiulcer potential of isoimperatorin isolated from O. koreanum has not yet been explored. Aim: To evaluate the antiulcer activity of isoimperatorin isolated from the roots of O. koreanum. Materials and methods: Isoimperatorin was isolated as cubic crystals by repeated column chromatography of the ethyl acetate fraction and structure was verified with 1H NMR, 13C NMR and high-resolution mass spectrometry (HRMS-FAB). The crystals obtained were analyzed with the single crystal X-ray method. The MTT assay was used to determine its cytotoxicity against chondrocytes at different concentrations (0.0–737.74 μM, 24 h). The in vivo antiulcer activity of isoimperatorin (40 mg/kg) was determined against ethanol-, indomethacin- and pyloric ligation-induced ulcers in Sprague-Dawley rats. Furthermore, the effect of isoimperatorin (0.0–737.74 μM, 24 h) on the expression of type II collagen in chondrocytes was determined using western blot method. The in vitro urease inhibitory activity of isoimperatorin (0–80 μM) and molecular docking was also performed against urease. Results and discussion: Isoimperatorin demonstrated significant inhibitory activity (IC50 36.43 μM) against urease as compared to the standard drug thiourea (IC50 33.57 μM) without cytotoxic effects. It provided 70.9%, 67.65% and 54.25% protection in ulcer models induced by ethanol, indomethacin and pyloric ligation, respectively. Isoimperatorin showed the highest expression level of type II collagen at 368.87 μM. The docking results confirmed strong binding affinity with the target protein. Conclusion: Isoimperatorin may be used to develop antiulcer drugs with decreased side effects.

Background: The methods like bio-green are advantageous over chemical and physical methods due to ecofriendly and cost-effective synthesis of nanoparticles. Current study was designed for green synthesis of silver nanoparticles (AgNPs) and their biological evaluation. Methods: Methanolic extract of Bergenia ciliata (BC) rhizomes prepared by maceration was used for the synthesis of AgNPs and confirmed by UV–visible and Fourier Transform Infra-Red (FTIR) spectroscopy. Further field emission scanning electron microscope (SEM) was used for the shape and size determination. In vitro Antioxidant, antimicrobial and cytotoxic potential was determined by using standard protocols. Results: The nanoparticles were spherical in shape having average particle size of 35 nm. FTIR analysis revealed the possible involvement of phyto-constituents in silver nanoparticles of crude extract. Green synthesized nanoparticles (BCAgNPs) showed the enhanced antioxidant properties compared to the crude extract. These nanoparticles showed the cytotoxic effects against brine shrimp (Artemia salina) nauplii with a value of 33.92 μg/ml LD50. BCAgNPs were found effective against the pathogenic fungal and bacterial strains in comparison to the Bergenia ciliata extract. Conclusion: Green synthesized BCAgNPs showed enhanced biological activities. Present results also support the advantages of using bio-green method for the production of nanoparticles having the potential of antimicrobial and cytotoxic activities.

The present study comprises the synthesis of a new series of sulfonamides derived from 4-methoxyphenethylamine (1). The synthesis was initiated by the reaction of 1 with 4-methylbenzenesulfonyl chloride (2) in aqueous sodium carbonate solution at pH 9 to yield N-(4-methoxyphenethyl)-4-methylbenzensulfonamide (3).This parent molecule 3 was subsequently treated with various alkyl/aralkyl halides, (4a–j), using N,N-dimethylformamide (DMF) as solvent and LiH as activator to produce a series of new N-(4-methoxyphenethyl)-N-(substituted)-4-methylbenzenesulfonamides (5a–j). The structural characterization of these derivatives was carried out by spectroscopic techniques like IR, 1H-NMR, and 13C-NMR. The elemental analysis data was also coherent with spectral data of these molecules. The inhibitory effects on acetylcholinesterase and DPPH were evaluated and it was observed that N-(4-Methoxyphenethyl)-4-methyl-N-(2-propyl)benzensulfonamide (5c) showed acetylcholinesterase inhibitory activity 0.075 ± 0.001 (IC50 0.075 ± 0.001 µM) comparable to Neostigmine methylsulfate (IC50 2.038 ± 0.039 µM).The docking studies of synthesized ligands 5a–j were also carried out against acetylcholinesterase (PDBID 4PQE) to compare the binding affinities with IC50 values. The kinetic mechanism analyzed by Lineweaver-Burk plots demonstrated that compound (5c) inhibits the acetylcholinesterase competitively to form an enzyme inhibitor complex. The inhibition constants Ki calculated from Dixon plots for compound (5c) is 2.5 µM. It was also found from kinetic analysis that derivative 5c irreversible enzyme inhibitor complex. It is proposed on the basis of our investigation that title compound 5c may serve as lead structure for the design of more potent acetylcholinesterase inhibitors.