Anti-inflammatory & anti-allergy agents in medicinal chemistry最新文献

{"title":"<i>In-silico</i> based Designing of benzo<i>[d]</i>thiazol-2-amine Derivatives as Analgesic and Anti-inflammatory Agents.","authors":"Arun K Mishra, Kamal Y Thajudeen, Mhaveer Singh, Gulam Rasool, Arvind Kumar, Harpreet Singh, Kalicharan Sharma, Amrita Mishra","doi":"10.2174/0118715230296273240725065839","DOIUrl":"10.2174/0118715230296273240725065839","url":null,"abstract":"<p><strong>Background: </strong>Benzo[d]thiazoles represent a significant class of heterocyclic compounds renowned for their diverse pharmacological activities, including analgesic and antiinflammatory properties. This molecular scaffold holds substantial interest among medicinal chemists owing to its structural versatility and therapeutic potential. Incorporating the benzo[d]thiazole moiety into drug molecules has been extensively investigated as a strategy to craft novel therapeutics with heightened efficacy and minimized adverse effects.</p><p><strong>Aims: </strong>The aim of the present research work was to design, synthesize and characterize the new benzo[d]thiazol-2-amine derivatives as potent analgesic and anti-inflammatory agents.</p><p><strong>Materials and methods: </strong>The synthesis of the presented benzo[d]thiazol-2-amine derivatives was performed by condensing-(4-chlorobenzylidene) benzo[d]thiazol-2-amine with a number of substituted phenols in the presence of potassium iodide and anhydrous potassium carbonate in dry acetone. IR spectroscopy, 1HNMR spectroscopy, 13CNMR spectroscopy and Mass spectroscopy methods were used to characterize the structural properties of all 13 newly synthesized derivatives. The molecular properties of these newly synthesized derivatives were estimated to study the attributes of drug-like candidates. Benzo[d]thiazol-2-amine derivatives were molecularly docked with selective enzymes COX-1 and COX-2. Analgesic and anti-inflammatory activities of synthesized compounds were evaluated by using albino rats.</p><p><strong>Results: </strong>Findings of the research suggested that compounds G3, G4, G6, G8 and G11 possess higher binding affinity than diclofenac sodium, when docking was performed with enzyme COX-1. Compounds G1, G3, G6, G8 and G10 showed lower binding affinity than Indomethacin when docking was performed with enzyme COX-2. <i>In vitro</i> evaluation of the COX-1 and COX-2 enzyme inhibitory activities was performed for synthesized compounds.</p><p><strong>Discussion: </strong>Compounds G10 and G11 exhibited significant COX-1 and COX-2 enzyme inhibitory action with an IC₅₀ value of 5.0 and 10 μM, respectively. Using the hot plate method and the carrageenan-induced rat paw edema model, the synthesized compounds were screened for their biological activities, including analgesic and anti-inflammatory activities. Highest analgesic action was exhibited by derivative G11 and the compound G10 showed the highest anti-inflammatory response. Inhibition of COX may be considered as a mechanism of action of these compounds.</p><p><strong>Conclusion: </strong>It was concluded that synthesized derivatives G10 and G11 exhibited significant analgesic and anti-inflammatory effect; therefore, the said compounds may be subjected to further clinical investigation for establishing these as future compounds for the treatment of pain and inflammation.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"230-260"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142006215","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Corrigendum to: Anti- SARS-CoV-2 IgG and IgM Levels in Iraqi General Population.","authors":"Amina Hamed Alobaidi, Hussein Inam Mustafa, Ahmed Mutar Salih, Abdulghani Mohamed Alsamarai","doi":"10.2174/1871523023999240522153411","DOIUrl":"https://doi.org/10.2174/1871523023999240522153411","url":null,"abstract":"<p><p>A typographical error in the Reference No. 175 appeared erroneously in the References List of the article titled \"Anti- SARSCoV- 2 IgG and IgM Levels in Iraqi General Population\", 2023; 22(2) [1]. Original: Barassi, A.; Pezzilli, R.; Mondoni, M.; Rinaldo, R.F.; Dav, I.M.; Cozzolino, M. Vitamin D in severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) patients with non-invasive ventilation support. Panminerva Med., 2021, ••• Corrected: Barassi, A.; Pezzilli, R.; Mondoni, M.; Rinaldo, R.F.; Davì, M.; Cozzolino, M. Vitamin D in severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) patients with non-invasive ventilation support. Panminerva Med., 2023, 65(1), 23-29. We apologize to the readers for the inconvenience caused due to this error. The original article can be found online at: https://www.eurekaselect.com/article/135111.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":"23 2","pages":"148"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142006216","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Exploration of Antileishmanial Compounds Derived from Natural Sources.","authors":"Gajala Deethamvali Ghouse Peer, Anjali Priyadarshini, Archana Gupta, Arpana Vibhuti, Vethakkani Samuel Raj, Chung-Ming Chang, Ramendra Pati Pandey","doi":"10.2174/0118715230270724231214112636","DOIUrl":"10.2174/0118715230270724231214112636","url":null,"abstract":"<p><strong>Aims: </strong>Leishmaniasis is a deadly tropical disease that is neglected in many countries. World Health Organization, along with a few other countries, has been working together to protect against these parasites. Many novel drugs from the past few years have been discovered and subjected against leishmaniasis, which have been effective but they are quite expensive for lower-class people. Some drugs showed no effect on the patients, and the longer use of these medicines has made resistance against these deadly parasites. Researchers have been working for better medication by using natural products from medicinal plants (oils, secondary metabolites, plant extracts) and other alternatives to find active compounds as an alternative to the current synthetic drugs.</p><p><strong>Materials and methods: </strong>To find more potential natural products to treat Leishmania spp, a study has been conducted and reported many plant metabolites and other natural alternatives from plants and their extracts. Selected research papers with few term words such as natural products, plant metabolites, Leishmaniasis, <i>in vivo</i>, <i>in vitro</i>, and treatment against leishmaniasis; in the Google Scholar, PubMed, and Science Direct databases with selected research papers published between 2015 and 2021 have been chosen for further analysis has been included in this report which has examined either <i>in vivo</i> or <i>in vitro</i> analysis.</p><p><strong>Results: </strong>This paper reported more than 20 novel natural compounds in 20 research papers that have been identified which report a leishmanicidal activity and shows an action against promastigote, axenic, and intracellular amastigote forms.</p><p><strong>Conclusion: </strong>Medicinal plants, along with a few plant parts and extracts, have been reported as a possible novel anti-leishmanial medication. These medicinal plants are considered nontoxic to Host cells. Leishmaniasis treatments will draw on the isolated compounds as a source further and these compounds compete with those already offered in clinics.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"1-13"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139567424","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Standardization and Pharmacological Evaluation of <i>Ziziphus mauritiana</i> Extract for Sedative and Anticonvulsant Activity in Mice and Rat.","authors":"Nadim Siddique, Akash Ved, Karuna Shanker Shukla, Amit Kumar Nigam","doi":"10.2174/0118715230276586231215045816","DOIUrl":"10.2174/0118715230276586231215045816","url":null,"abstract":"<p><strong>Introduction: </strong><i>Ziziphus mauritiana</i>, sometimes called Indian jujube or Ber, belongs to the Rhamnaceae group of plants. The aqueous and ethanolic Ziziphus mauritiana formulations were shown to have analgesic, antipyretic, potent analgesic, anti-inflammatory, and anti-emetic properties.</p><p><strong>Aims & objectives: </strong>The aim of this study is to investigate the sedative and anticonvulsant activities of <i>Ziziphus mauritiana</i> extract by governing 200 and 400 mg/kg body weight orally.</p><p><strong>Materials and methods: </strong>The leaves are extracted with ethanol and lukewarm water with a soxhlet apparatus for 72 hours. After that acute extract toxicity study was performed and then locomotor activity, pentobarbital induced sleeping time and anticonvulsant activity were performed with the extract.</p><p><strong>Results: </strong>Oral administration of extract at dosages of 200 & 400 mg/kg was employed after an immediate toxicity test. At a dosage of 400 mg/kg, the number of locomotions was reduced significantly lengthened the period of time spent sleeping and there was showed a dosage-dependent reduction in all phases of an epileptic episode.</p><p><strong>Conclusion: </strong>In this study, the extract reduced locomotor activity, however, it had a superior profile for an antiepileptic action than phenytoin since it decreased locomotor activity to a lesser level. The considerable increase in pentobarbitone sleep hours with the extracts at a higher dose supported the sedative action of <i>Z. mauritiana</i>.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"31-38"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139567426","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Decades Long Involvement of THP-1 Cells as a Model for Macrophage Research: A Comprehensive Review.","authors":"Prakhar Sharma, Kaliyamurthi Venkatachalam, Ambika Binesh","doi":"10.2174/0118715230294413240415054610","DOIUrl":"10.2174/0118715230294413240415054610","url":null,"abstract":"<p><p>Over the years, researchers have endeavored to identify dependable and reproducible <i>in vitro</i> models for examining macrophage behavior under controlled conditions. The THP-1 cell line has become a significant and widely employed tool in macrophage research within these models. Originating from the peripheral blood of individuals with acute monocytic leukemia, this human monocytic cell line can undergo transformation into macrophage-like cells, closely mirroring primary human macrophages when exposed to stimulants. Macrophages play a vital role in the innate immune system, actively regulating inflammation, responding to infections, and maintaining tissue homeostasis. A comprehensive understanding of macrophage biology and function is crucial for gaining insights into immunological responses, tissue healing, and the pathogenesis of diseases such as viral infections, autoimmune disorders, and neoplastic conditions. This review aims to thoroughly evaluate and emphasize the extensive history of THP-1 cells as a model for macrophage research. Additionally, it will delve into the significance of THP-1 cells in advancing our comprehension of macrophage biology and their invaluable contributions to diverse scientific domains.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"85-104"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140858191","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Potential of Natural Products as Therapeutic Agents for Inflammatory Diseases.","authors":"Chintan Aundhia, Ghanshyam Parmar, Chitrali Talele, Piyushkumar Sadhu, Ashim Kumar Sen, Pramojeeta Rana","doi":"10.2174/0118715230307969240614102321","DOIUrl":"10.2174/0118715230307969240614102321","url":null,"abstract":"<p><p>Inflammation is a complex biological response that plays a pivotal role in various pathological conditions, including inflammatory diseases. The search for effective therapeutic agents has led researchers to explore natural products due to their diverse chemical composition and potential therapeutic benefits. This review comprehensively examines the current state of research on natural products as potential therapeutic agents for inflammatory diseases. The article discusses the antiinflammatory properties of various natural compounds, their mechanisms of action, and their potential applications in managing inflammatory disorders. Additionally, formulation and delivery systems, challenges and future prospects in this field are also highlighted.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"149-163"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141565527","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"<i>In-vitro</i> and <i>In Silico</i> Assessment of Anti-inflammation Properties of Saponarin Extracted from Hordeum Vulgare.","authors":"Revathi Boyina, Sreya Kosanam, Sasidhar Bhimana, Raveendra Babu Gudimitla, Dhachinamoorthi Duraiswamy","doi":"10.2174/0118715230284334240101100450","DOIUrl":"10.2174/0118715230284334240101100450","url":null,"abstract":"<p><strong>Background: </strong>Hordeum vulgare, commonly known as Barley grass, is a historically significant cultivated plant with profound implications for societies, agricultural sciences, and human nutrition. It has been valued for both sustenance and its potential medicinal properties.</p><p><strong>Objectives: </strong>This study aims to comprehensively investigate the medicinal properties of Hordeum vulgare, focusing on its potential therapeutic benefits and anti-inflammatory properties. Additionally, we seek to quantify and compare the phytochemical content of two distinct extracts: Barley Grass Hexane Extract (BGHE) and Barley grass aqueous extract (BGAQ).</p><p><strong>Methods: </strong>We quantified the phytochemical contents of BGHE and BGAQ and evaluated their anti-inflammatory effects using UV spectroscopy at 560 nm, coupled with the RBC membrane stabilization technique. Subsequently, we conducted <i>in silico</i> studies to assess the <i>in vitro</i> anti-inflammatory potential of Barley grass leaf extracts.</p><p><strong>Results: </strong>Both BGHE and BGAQ demonstrated significant inhibitory effects on inflammation compared to the control group. However, BGHE exhibited superior anti-inflammatory efficacy when compared to BGAQ, suggesting its role as a potential anti-inflammatory agent. <i>In silico</i> studies further supported the anti-inflammatory potential of Barley grass leaf extracts.</p><p><strong>Conclusion: </strong>Hordeum vulgare, or Barley grass, offers a wealth of health benefits, including anti-inflammatory, anti-diabetic, anti-cancer, antioxidant, anti-acne, and anti-depressant properties. These properties contribute to improved immunity, reduced cardiovascular disorders, and alleviation of fatigue. The distinct extracts, BGHE and BGAQ, both exhibit promising anti-inflammatory capabilities, but BGHE shows better anti-inflammatory activity. This research sheds light on the therapeutic potential of Barley grass, making it a valuable candidate for further exploration in the field of natural medicine.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"14-20"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139521906","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"The Influence of Phytoconstituents for the Management of Antipsoriatic Activity in Various Animal Models.","authors":"Ravina Yadav, Tejpal Yadav, Ashutosh Upadhayay, Md Sabir Alam, Gaurav Dubey, Vikram Kumar, Adarsh Sahu","doi":"10.2174/0118715230320581240711063558","DOIUrl":"10.2174/0118715230320581240711063558","url":null,"abstract":"<p><p>It is possible for psoriasis to manifest at any point in a person's life, regardless of their age, gender, or geographic location. It is a chronic immune-linked inflammatory skin illness that affects individuals of various racial and ethnic origins. It is recognized to be a longlasting condition. Because of the significant contribution that natural products have made, there has been a significant advancement in the treatment of skin illnesses such as psoriasis. The biggest number of phytochemicals derived from a wide range of plants and herbs are now being used in a variety of applications throughout the whole world. Additionally, a number of phytochemicals, including aloe-emodin, psoralen, curcumin, and others, have been effectively extracted in pure or clear form, and they have shown a great deal of efficacy in the treatment of psoriasis illness. There is evidence that few herbal remedies are effective, and the occurrence of these phytochemicals provides more proof. When synthetic medications are used for chronic therapy, they may cause a variety of adverse consequences; hence, the exploration of natural pharmaceuticals can give a successful natural treatment with a minimal amount of adverse effects. Within the scope of this concise review, a number of plant sources that possess anti-psoriatic activity are investigated, and the antipsoriatic effects of these plant sources are shown on a number of animal models using particular pathways.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"215-229"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141857544","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Formulation and Characterization of Emulgel Lornoxicam Containing Lemon Grass Oil as Penetration Enhancer.","authors":"Vibha Kumari, Meenakshi Bajpai","doi":"10.2174/0118715230289163240703075629","DOIUrl":"10.2174/0118715230289163240703075629","url":null,"abstract":"<p><strong>Introduction: </strong>Emulgel dosage form is an advanced form of transdermal drug delivery. It is a combination of emulsion and gel in a definite ratio. Emulsions are incorporated into the gel with proper mixing. The emulsion present in emulgel can be either oil/water or water/oil, which is thickened by mixing it with a gelling agent.</p><p><strong>Materials and methods: </strong>On the basis of the solubility of lornoxicam in various oils, a surfactant and a co-surfactant were selected for further research. For the preparation of emulgel, the emulsion was prepared with Smix (surfactant and co-surfactant) in a ratio of 1:2. The prepared emulsion was incorporated into different concentrations of carbapol 934 in a 1:1 ratio to make a homogenous emulgel.</p><p><strong>Results: </strong>The emulgel was inspected visually to see if it had any phase behaviour, spreadability, or grittiness by applying it to a slide. All formulations were evaluated for pH, physical properties, drug content, spreadability, extrudability, swelling index, viscosity, and centrifugation. Franz diffusion cell was used to perform <i>in-vitro</i> release of formulation with the help of egg membrane. Among all formulations, F3 showed 83% release after 6 hours and showed acceptable physical properties like homogeneity, colour, consistency, pH value, spreadability, extrudability, and drug content.</p><p><strong>Discussion: </strong>Thus, emulgel can be regarded as a more feasible drug delivery system for hydrophobic drugs (lornoxicam) than the currently marketed formulation. Optimized emulgel formulation consists of a microemulsion of lornoxicam, 1% of carbopol 934, propylene glycol, sodium benzoate, lemon grass oil, glycerin, and distilled water. In the <i>in-vitro</i> release studies, pH 7.4 phosphate buffer emulgel formulation (F3) showed 83% after 6 hours. Emulgel was found to be stable under stable conditions.</p><p><strong>Conclusion: </strong>The emulgel of the poorly water-soluble drug (lornoxicam) was formulated. The components and their optimum ratio for the formulation of microemulsion were obtained by solubility studies and droplet size analysis. Thus, microemulsion can be regarded as a more feasible dose delivery system for lornoxicam than the currently marketed tablet, capsule, and injection formulations. Optimized microemulsion of lornoxicam was incorporated into the gel base. Therefore, it may be concluded that emulgel of lornoxicam can be used as a controlledrelease dosage form of the drug for local application in rheumatoid arthritis.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"164-173"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141790763","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Pyrazoles as Anti-inflammatory and Analgesic Agents: <i>In-vivo</i> and <i>In-silico</i> Studies.","authors":"Geeta Chahal, Jyoti Monga, Isha Rani, Shubham Saini, Manish Devgun, Asif Husain, Sukhbir Lal Khokra","doi":"10.2174/0118715230275741231207115011","DOIUrl":"https://doi.org/10.2174/0118715230275741231207115011","url":null,"abstract":"<p><strong>Background: </strong>Pyrazole is a well-known nucleus in the pharmacy field with a wide range of other activities in addition to anti-inflammatory and analgesic, i.e., anticonvulsant, antiviral, and anticancer activities. There are well-known marketed drugs having pyrazole moiety as celecoxib, and lonazolac as COX-II inhibitors.</p><p><strong>Aims: </strong>We aim to synthesize better anti-inflammatory than existing ones. Thiophene is also known for its analgesic and anti-inflammatory action. Thus, the fusion of both gives better anti-inflammatory agents. In the present studies, derivatives from two series of pyrazole were prepared by reacting substituted chalcone (3a-3f) derivatives prepared from 2-acetyl thiophene. They substituted aromatic aldehydes with phenyl hydrazine to form (5a-5f) and with 2, 4-dinitro phenyl hydrazine giving compounds (6a-6f) separately.</p><p><strong>Methods: </strong>Purified and characterized pyrazoles have been analyzed for <i>in-vivo</i> analgesic and anti-inflammatory activities by using standard methods. Compounds 5e, 5f, and 6d were proved to be potent analgesics and series (5a-5f) was found to have anti-inflammatory action, which was further validated using docking and ADME studies.</p><p><strong>Results: </strong>The ADME profile of synthesized compounds was found to be satisfactory.</p><p><strong>Conclusion: </strong>The synthesized compounds can serve as lead for further drug designing.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":"23 1","pages":"39-51"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141200815","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}