Yousaf Khan, Anila Mukhtiar, Hina Sarfraz, Shoaib Khan, Rafaqat Hussain, Mujeeb Ul Naeem, Abdul Sattar, Tariq Aziz, Zia Ur Rehman Panezai, Thamer H Albekairi, Farwa Jabbir
{"title":"Unveiling of the novel benzothiazole derived thiazolidinone derivatives: in vitro and in silico insights to design a promising agent for anti-Alzheimer's disease.","authors":"Yousaf Khan, Anila Mukhtiar, Hina Sarfraz, Shoaib Khan, Rafaqat Hussain, Mujeeb Ul Naeem, Abdul Sattar, Tariq Aziz, Zia Ur Rehman Panezai, Thamer H Albekairi, Farwa Jabbir","doi":"10.1515/znc-2024-0244","DOIUrl":"https://doi.org/10.1515/znc-2024-0244","url":null,"abstract":"<p><p>The present investigation explained various heterocyclic moieties particularly the thiazolidinone scaffold (<b>1-16</b>) which were synthesized from benzothiazole as promising anti-Alzheimer agent. In this, we have unveiled the synthetic path for generation of thiazolidinone scaffolds which was initiated benzothiazole having 2-amine moiety. These synthesized scaffolds were then inveterate through several analytical techniques including high-resolution electron impact mass spectrometry (HREI-MS), proton nuclear magnetic resonance (<sup>1</sup>H NMR), and carbon-13 nuclear magnetic resonance (<sup>13</sup>C NMR). The anti-Alzheimer potential of these compounds was evaluated through molecular docking studies to examine their interactions with target proteins. Additionally, ADMET analysis was performed to assess drug-likeness and pharmacokinetic properties. Among the synthesized analogs, scaffold-<b>3</b> emerged as the most promising inhibitor compared to other derivatives in the series. This study highlights the potential of thiazolidinone derivatives in the development of novel anti-Alzheimer drugs and underscores the need for further optimization to enhance their therapeutic efficacy.</p>","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2025-06-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144477592","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Anila Mukhtiar, Yousaf Khan, Hina Sarfraz, Aisha Usman, Marouan Kouki, Umair Mukhtiar
{"title":"<i>Moringa oleifera</i>: a multifunctional botanical resource for sustainable agriculture, nutrition, and therapeutic applications, a review.","authors":"Anila Mukhtiar, Yousaf Khan, Hina Sarfraz, Aisha Usman, Marouan Kouki, Umair Mukhtiar","doi":"10.1515/znc-2024-0195","DOIUrl":"https://doi.org/10.1515/znc-2024-0195","url":null,"abstract":"<p><p><i>Moringa oleifera</i>, widely recognized as the \"miracle tree,\" has garnered significant scientific interest due to its exceptional nutritional, medicinal, and industrial properties. This study provides a comprehensive evaluation of its potential as a sustainable feed additive, antimicrobial agent, functional food ingredient, and a bioresource for agricultural and industrial advancements. Enriched with high-quality proteins, essential amino acids, vitamins, minerals, antioxidants, and bioactive compounds, <i>M. oleifera</i> exhibits remarkable benefits in aquaculture, livestock production, and human nutrition. Its potent immunomodulatory, antifungal, antidiabetic, and antimicrobial properties further underscore its therapeutic significance in disease prevention and health promotion. Additionally, its ecological advantages, including soil enrichment, natural pest control, and wastewater purification, highlight its pivotal role in fostering environmental sustainability. A comprehensive investigation over the past five years has consistently validated its effective insecticidal efficacy, further expanding its agricultural applications. The efficacy of <i>M. oleifera</i> bioactive compounds is profoundly influenced by extraction methodologies. Advanced techniques such as ultrasound-assisted extraction (UAE), microwave-assisted extraction (MAE), supercritical fluid extraction (SFE), and enzymatic-assisted extraction (EAE) significantly enhance the yield, purity, and bioavailability of phytochemicals, optimizing their pharmacological and industrial applications. The selection of an appropriate extraction strategy is crucial to preserving bioactivity and ensuring maximum efficacy in pharmaceutical, nutraceutical, and functional food formulations. Despite its vast potential, challenges such as the presence of anti-nutritional factors, variations in nutrient composition due to differing cultivation and processing methods, and the absence of standardized dosage guidelines require further investigation. Future research should focus on optimizing inclusion levels in animal and human diets, elucidating molecular mechanisms of action, and advancing green extraction technologies to enhance its efficacy and sustainability. This study highlights the multifaceted applications of <i>M. oleifera</i> across diverse sectors and its potential to revolutionize sustainable agriculture, healthcare, and environmental conservation. Addressing existing challenges through cutting-edge research and technological innovation will unlock its full potential as a key natural resource for enhancing global food security, promoting sustainable development, and pioneering pharmaceutical breakthroughs. By integrating information from recent five-year literature from 2019 to 2024, this work offers a roadmap for future study, addressing significant challenges and outlining prospective avenues for the development of novel therapeutic and pest control approaches exploiting <i>M. ole","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2025-06-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144267795","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Chemometric study of the effects of the geographical origin and the collection period on the chemical compositions and the antimicrobial activities of <i>Pituranthos tortuosus</i> essential oils.","authors":"Zina Benissa, Fatma Chtourou, Françoise Dumas, Sylvie Bouttier, Mohamed Bouaziz, Sami Zouari","doi":"10.1515/znc-2024-0302","DOIUrl":"https://doi.org/10.1515/znc-2024-0302","url":null,"abstract":"<p><p>The present study aims to analyze the chemometric variation of the chemical composition of the aerial part's essential oils of <i>Pituranthos tortuosus</i>, collected from different regions from Tunisia (Majoura and Sened (Gafsa), Sbeitla (Kasserine), and Eljem (Mahdia)) during the period from February to June and to assess their antimicrobial activity. The different samples of the aerial parts of <i>P. tortuosus</i> were hydrodistillated during 4 h. The obtained essential oils were analyzed by GC/FID and GC/MS techniques. The antimicrobial activity of these essential oils samples was evaluated <i>in vitro</i> using Petri dishes against <i>Staphylococcus aureus</i> subsp<i>. aureus</i>, <i>Pseudomonas aeruginosa</i>, <i>Escherichia coli</i>, and <i>Candida albicans</i>. The obtained results showed that the yields of all essential oils were ranging from 0.42 to 0.77 %. They differ significantly (<i>p</i> ≤ 0.01) with the regions of collection. The chromatographic analysis of these essential oils displayed different chemical compositions leading to the identification of eight chemotypes. The majority of their chemical compounds differ significantly with the collection regions (<i>p</i> ≤ 0.05). The studied antimicrobial effects of the essential oils revealed significant differences (<i>p</i> ≤ 0.02) with the collection region. All the essential oils displayed an important antimicrobial effect against <i>S. aureus</i> and <i>C. albicans</i>.</p>","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2025-06-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144235721","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Tolessa Duguma, Yadessa Melaku, Akalu Terfa, Kebede Shenkute, Taye B Demissie, Nayang Kgakatsi, Mo Hunsen
{"title":"<i>In vitro</i> antibacterial, DPPH radical scavenging activities, and <i>in silico</i> studies of isolated compounds from <i>Rubus apetalus</i> leaves extract.","authors":"Tolessa Duguma, Yadessa Melaku, Akalu Terfa, Kebede Shenkute, Taye B Demissie, Nayang Kgakatsi, Mo Hunsen","doi":"10.1515/znc-2025-0003","DOIUrl":"https://doi.org/10.1515/znc-2025-0003","url":null,"abstract":"<p><p><i>Rubus apetalus</i> Poir. is a medicinal plant used in Ethiopia to treat different diseases. This study aimed to isolate phytochemicals from the leave<i>s</i> and evaluate their antibacterial and DPPH scavenging activities using <i>in vitro</i> and <i>in silico</i> studies. The GC-MS study resulted in the identification of 16 compounds. Palmitic acid (<b>9</b>), palmityl alcohol (<b>17</b>), <i>β</i>-sitosterol (<b>18</b>), tiliroside (<b>19</b>), and astragalin (<b>20</b>) were isolated using chromatographic techniques and characterized using NMR data. The inhibition zones (IZs) of 100 mg/mL extracts and 5 mg/mL isolated compounds ranged from 9.33 ± 0.47 to 15.07 ± 0.74 mm against all bacteria. Compound <b>18</b> showed better activity against <i>Staphylococcus aureus</i> and <i>Streptococcus pyogenes</i>. Compound <b>19</b> exhibited better activity against <i>Escherichia coli</i> and <i>Pseudomonas aeruginosa</i>. The activity of compound <b>19</b> was supported by molecular docking studies against <i>E</i>. <i>coli</i> DNA gyrase B (-8.0 kcal/mol) and <i>Pseudomonas</i> quinolone signal A (PqsA, -9.5 kcal/mol) for <i>E</i>. <i>coli</i> and <i>P</i>. <i>aeruginosa</i>, respectively. At 62.5 mg/mL, combined fractions 16-21 and compound <b>19</b> showed the lowest (54.5 %) and the highest (89.8 %) DPPH scavenging activity, respectively. The <i>in silico</i> studies indicated that none of the isolated compounds is fatal if swallowed. Therefore, these findings support the traditional use of the plant to treat various bacterial diseases.</p>","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2025-06-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144235720","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Kashvy R Morakhia, Aayushi C Shah, Mannat P Patel, Jainam K Shah, Rajanikant Patel, Mehul R Chorawala
{"title":"From current landscape to future horizon in stem cell therapy for tissue regeneration and wound healing: bridging the gap.","authors":"Kashvy R Morakhia, Aayushi C Shah, Mannat P Patel, Jainam K Shah, Rajanikant Patel, Mehul R Chorawala","doi":"10.1515/znc-2025-0020","DOIUrl":"https://doi.org/10.1515/znc-2025-0020","url":null,"abstract":"<p><p>Stem cell therapy has emerged as a groundbreaking approach in regenerative medicine, offering immense potential for tissue regeneration and wound healing. Stem cells, with their ability to self-renew and differentiate into specialized cell types, provide innovative therapeutic strategies for variety of medical conditions. Key stem cell types, including embryonic, induced pluripotent, and adult stem cells such as mesenchymal and hematopoietic stem cells, play pivotal roles in regenerative processes and wound repair. In tissue regeneration, stem cells replenish damaged or necrotic cells by differentiating into specialized cell types like bone, muscle, or nerve cells, thus restoring the structural and functional integrity of tissues. In wound healing, stem cells stimulate angiogenesis, generate new skin cells, and modulate immune responses to enhance repair. This multifaceted therapeutic potential has paved the way for clinical applications in cardiovascular, neurological, musculoskeletal, and autoimmune disorders, as well as skin and burn injuries. This review highlights recent advancements in stem cell therapy, exploring its clinical applications and addressing challenges such as immune rejection, ethical concerns, scalability, and the need for long-term clinical trials. The article underscores the importance of continued research to fully realize the transformative potential of stem cell therapy in modern medicine.</p>","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2025-05-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144152705","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Sphingolipids in medicinal mushrooms: structural insights, biological activities, and therapeutic potential.","authors":"Yhiya Amen, Ahmed Othman, Kuniyoshi Shimizu","doi":"10.1515/znc-2024-0206","DOIUrl":"https://doi.org/10.1515/znc-2024-0206","url":null,"abstract":"<p><p>Edible mushrooms are well-known for their nutritional value, serving as rich sources of bioactive nutrients, mainly proteins, carbohydrates, lipids, vitamins, and minerals that are vital for human health. Lipids, integral to biological functions such as cellular structure and energy storage, play crucial roles in mushrooms' bioactivity. Sphingolipids, an important class of lipids, serve not only as structural elements in cell membranes but also act as bioactive molecules, playing key roles in cancer prevention, skin health, and infection control. Recent studies highlight their unique presence in mushrooms. Despite their relatively low abundance, sphingolipids in mushrooms are pivotal in cellular processes and offer therapeutic potential. Advances in analytical techniques have facilitated the characterization of these compounds. This review explores the structural profiles, biological activities, and therapeutic applications of sphingolipids in medicinal mushrooms, highlighting their potential in the development of functional foods and novel therapeutic agents.</p>","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2025-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144024126","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Abubakar Siddiq Salihu, Wan Mohd Nuzul Hakimi Wan Salleh, Nurunajah Ab Ghani, Arwa R Althaher, Salam Ahmed Abed
{"title":"Chemical composition, anticholinesterase activity and cytotoxicity of the essential oil of <i>Luvunga scandens</i> (Roxb.) Wight from Malaysia.","authors":"Abubakar Siddiq Salihu, Wan Mohd Nuzul Hakimi Wan Salleh, Nurunajah Ab Ghani, Arwa R Althaher, Salam Ahmed Abed","doi":"10.1515/znc-2025-0053","DOIUrl":"https://doi.org/10.1515/znc-2025-0053","url":null,"abstract":"<p><p><i>Luvunga scandens</i> (Roxb.) Wight is identified as one of the vital folk medicinal plants in Malaysia. Despite its traditional use, the essential oil composition and bioactivities of <i>L. scandens</i> remain largely unexplored. This study investigates the essential oil composition, anticholinesterase activity, and cytotoxicity of <i>L. scandens</i> leaves. After the essential oil was extracted using hydrodistillation, GC-FID and GC-MS were used for analysis, identifying 35 components, representing 93.8 % of the total oil. The major components included germacrene D (17.8 %), <i>γ</i>-elemene (15.6 %), <i>β</i>-gurjunene (10.8 %), <i>α</i>-cadinol (5.3 %), <i>α</i>-humulene (4.9 %), and alloaromadendrene (4.5 %). With IC<sub>50</sub> values of 78.5 and 95.2 μg/mL, the essential oil showed moderate inhibition of butyrylcholinesterase (BChE) and acetylcholinesterase (AChE). The cytotoxicity was evaluated using an MTT assay. The essential oil exhibited cytotoxicity against three cancer cell lines; HepG2, MCF7, and A549 with IC<sub>50</sub> values of 70.2, 52.8, and 65.5 μg/mL, respectively. These findings provide new insights into the potential therapeutic applications of <i>L. scandens</i> essential oil, particularly in neurodegenerative diseases and cancer therapy.</p>","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2025-04-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143994998","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Native/modified dextran-based nanogel in delivering drug and management of ocular complications: a review.","authors":"Biswajit Basu, Suraj Mallick, Suman Dhauria, Pooja V Nagime, Sudarshan Singh","doi":"10.1515/znc-2025-0014","DOIUrl":"https://doi.org/10.1515/znc-2025-0014","url":null,"abstract":"<p><p>Ocular nanogels have emerged as a promising therapeutic approach, and nanotechnology has speed up the growth of the pharmaceutical and medical technology sectors. The physiological and anatomical barriers of the eye limit the use of traditional ocular preparations, which leads to low drug bioavailability and a brief retention period. This presents a serious problem for patients, doctors, and chemists. Nevertheless, nanogels can encapsulate medications within three-dimensional crosslinked polymeric networks and provide controlled and prolonged drug delivery by using particular structural layouts and unique preparation techniques, improving therapeutic efficacy and patient compliance. Dextran and its variants, a naturally occurring polysaccharide, have drawn a lot of interest in developing delivery systems for use in pharmaceutical and medical applications. Many dextran-based delivery systems with customized geometries and features have been fabricated recently, such as hydrogels, nanogels, magnetic nanoparticles, nanoemulsions, self-assembled micelles and nanoparticles, and microparticles. The review presents advancement and therapeutic potential of dextran-based nanogels for the treatment of various eye conditions, such as cataract, conjunctivitis, glaucoma, dry eye syndrome, age-related macular degeneration, and corneal ulcers. Moreover, the process for development and assessing these nanomedicines, emphasizing their safety and effectiveness as established by preclinical, toxicological, clinical assessments, and patent updates, has been elaborated.</p>","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2025-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144053641","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Biotransformation of vinblastine into vincristine using a fungal endophyte <i>Fusarium equiseti</i> along with the assessment of its antiangiogenic properties.","authors":"Gauri Srivastava, Ruchika Mittal, Nidhi Srivastava, Sarita Srivastava, Deepak Ganjewala","doi":"10.1515/znc-2024-0263","DOIUrl":"https://doi.org/10.1515/znc-2024-0263","url":null,"abstract":"<p><p>This study focuses on the microbial biotransformation of vinblastine to vincristine, a compound with enhanced anticancer efficacy compared to vinblastine utilizing a fungal endophyte <i>Fusarium equiseti</i>, isolated from <i>Catharanthus roseus</i>. Additionally, the antiangiogenic properties of the resulting vincristine were evaluated <i>in vivo</i> using the chick chorioallantoic membrane assay. The biotransformation was conducted in liquid medium containing vinblastine (0.6-2.4 mM), and <i>F. equiseti</i> spore suspension (50-150 µL) by incubating at 30 °C, pH 5.6, and 200 rpm for eight days. After the reaction was over, products were extracted using methanol and analyzed by LC-MS/MS. The results confirmed the production of vincristine from vinblastine in different sets of biotransformation reactions. In biotransformation reaction-1, which comprised of vinblastine (0.6 mM) and fungal inoculum 150 µL (82 × 10<sup>4</sup> spores/mL), 92 % of vinblastine was converted into vincristine on 8th day of incubation. The vincristine produced demonstrated significant antiangiogenetic properties in the chick chorioallantoic membrane assay in a dose-dependent manner. The antiangiogenic properties of vincristine produced was comparable to standard vincristine. Hence, the study revealed that <i>F. equiseti</i> present a viable alternative to produce vincristine from vinblastine. To our knowledge, this is the first report on <i>F. equiseti</i> highlighting its vinblastine biotransformation potential.</p>","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2025-03-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143677324","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Shoaib Khan, Tayyiaba Iqbal, Tayyaba Zahoor, Rafaqat Hussain, Mohammad Shahidul Islam, Kholood A Dahlous
{"title":"Insight the confirmation of benzothiazolidinone-derived thiadiazole scaffolds as promising antiurease and anti-Alzheimer agents: synthesis, <i>in vitro</i>, and <i>in silico</i> investigations.","authors":"Shoaib Khan, Tayyiaba Iqbal, Tayyaba Zahoor, Rafaqat Hussain, Mohammad Shahidul Islam, Kholood A Dahlous","doi":"10.1515/znc-2024-0243","DOIUrl":"https://doi.org/10.1515/znc-2024-0243","url":null,"abstract":"<p><p>Alzheimer's disease is a serious neurological disorder, and traditional therapies for Alzheimer's, like radiation and surgical procedures, as well as chemotherapeutics, are usually linked with multiple negative consequences. Finding a novel therapeutic anti-Alzheimer agent with high efficacy and minimal side effects, we have designed and synthesized benzothiazolidinone-derived thiadiazole-based Schiff base derivatives (<b>1-15</b>). Biological assessment of these compounds was carried out against acetylcholinesterase and butyrylcholinesterase, and all the derivatives showed varying degrees of inhibitory activity. Analog <b>8</b> (IC<sub>50</sub> = <b>3.60 ± 0.20</b> and <b>4.10 ± 0.20 μM</b> for acetylcholinesterase and butyrylcholinesterase, respectively) demonstrated spellbinding efficacy in contrast to standard donepezil (IC<sub>50</sub> = <b>50 ± 0.10</b> and <b>8.10 ± 0.20 μM</b>). The surpassing inhibition of analog <b>8</b> is due to highly reactive CF<sub>3</sub> moiety at the <i>para</i>-position, inhibiting the enzymes via strong hydrogen bond. Analog <b>7</b> with IC<sub>50</sub> value of <b>5.70 ± 0.10</b> and <b>6.20 ± 0.40 μM</b> was also found with strong therapeutic potential than standard drug. The strong inhibition potential of lead compounds was also evaluated under enzyme kinetics and spellbinding potential was observed. Biological effectiveness of potent compounds was validated by visualizing the binding interactions via <i>in silico</i> molecular docking study and prediction of drug-likeness via ADME analysis. All the synthesized compounds were analyzed for their structural confirmation via <sup>1</sup>HNMR, <sup>13</sup>CNMR, and HREI-MS.</p>","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2025-03-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143671504","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}