Mini-Reviews in Organic Chemistry - Online First
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Pyrazole and its Derivatives: Chemistry and Biological Importance
Authors: Pooja S. Meshram, Kalyani R. Thombre, Krishna R. Gupta and Milind J. UmekarAvailable online: 04 August 2025More LessCurrently, the main focus of research is to develop disease treatment strategies that are both more safe and more effective. Nitrogen-containing 5-membered heterocyclic pyrazole is a unique scaffold in pharmaceutical development. Because of its remarkable diversity in biological activities, pyrazole and its derivatives have become a prominent scaffold that has attracted the interest of medicinal chemistry researchers. Researchers have developed pyrazole as a multipurpose lead compound for effective pharmacological activities. They have demonstrated a wide range of biological and pharmacological activities, including antidiabetic, antiparkinsonian, antitumor, analgesic, anti-inflammatory, antimicrobial, antitubercular, antileishmanial activity, and neuroprotective properties. Many scientists have improved and developed new structural alternatives as a result of this logical variation in the physiological reaction pattern and much more effective pharmacological interventions. This review presents a detailed overview of the literature work reported by researchers on pyrazoles and reports recent efforts made on this moiety. This has been followed by an in-depth analysis of the pyrazole concerning its medicinal significance. This follow-up may help medicinal chemists generate new leads possessing pyrazole nuclei with high efficacy. It is crucial for earlier research and projects that aim to investigate the diverse activities of compounds linked to pyrazole and its derivatives in the near future. This overview summarizes the introduction, design, and biological activity of pyrazole derivatives as antimicrobial, anticancer, antiviral, antitubercular and antimalarial agents.
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Phytochemical and Pharmacological Investigations of Genus Ranunculus (Ranunculaceae)
Available online: 17 July 2025More LessThe genus Ranunculus, a member of the family Ranunculaceae, is widely distributed across regions such as India, China, Nepal, Pakistan, and Russia. These plants hold significant value in traditional medicine and folklore, having been used to treat a variety of ailments, including malaria, rheumatism, asthma, cardiovascular conditions, liver and gallbladder disorders, snake bites, and even cancer. Notably, numerous bioactive compounds such as flavonoids, triterpenes, saponins, alkaloids, and fatty acids have been isolated from this genus and investigated for their diverse pharmacological properties, including antioxidant, antitubercular, antimalarial, and immunomodulatory effects. This review aims to provide a comprehensive overview of the phytochemistry and pharmacological potential of Ranunculus species, highlighting their traditional medicinal uses. A distinctive feature of this work is its thorough compilation of phytochemical investigations across various Ranunculus species, along with a detailed account of the biological activities exhibited by their extracts and phytoconstituents.
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Advances in the Determination of Chemical Composition and Pharmacological Properties of Ainsliaea spp.
Authors: Sumimu Ruzemimti, Yuchen Liu, Haoran Xue, Abodubasiti Tuersunbake, Panpan Wang, and and Jinjie LiAvailable online: 07 July 2025More LessPlants of the Ainsliaea genus, belonging to the Compositae family, contain various compounds such as terpenoids, flavonoids, steroids, phenylpropanoids, phenolic acids, and fatty acids, among others. The main components are sesquiterpenes. In addition, several species within this genus exhibit excellent pharmacological properties, including anti-inflammatory, anti-tumor, antibacterial, antiviral, antioxidant, and hepatoprotective effects. This paper offers a comprehensive review and summary of the chemical compositions and pharmacological properties of Ainsliaea genus, aiming to enhance research, development, and utilization of these plants.
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An Expository Review on the Multifaceted Applications of Sodium Alginate as a Scaffold in Metal-Organic Frameworks
Authors: Pankaj Bhandari, Shefali Arora, Parteek Prasher, Versha Parcha, Sukanya Chhetri and Deepak KumarAvailable online: 07 July 2025More LessPolysaccharides like sodium alginate manifest numerous applications due to the characteristics of biocompatibility, low toxicity, adsorption benefits, nature of regenerating tissues, response to pH stimuli, and exemplary binding property with metal ions. Metal-Organic Frameworks (MOFs) absorb and trap toxins/drugs/biosensors to speed mass transfer rates. Sodium alginate features accessible -COOH and -OH functional groups that allow for easy modification with various functional groups. Sodium alginate incorporated Metal-Organic Frameworks (MOFs) significantly enhance its potential, unlocking numerous opportunities for diverse applications across fields such as drug delivery, sensors, and environmental remediation. This modification not only improves the material's functional properties but also reduces systemic toxicity. The film-forming nature with great biodegradability and biocompatibility of the SA@MOF system proves it an appropriate food packaging material with exceptional mechanical and antimicrobial properties, lessening toxicity by avoiding direct contact with food material, amplified water barrier property, and preservation longevity. The SA@MOF outperforms drug delivery, toxic adsorption, antibiotic sensing, food freshness, etc. The SA-MOF-based products like to depict itself as a research-based industry, as the source of innovative drugs, composite films, and toxin absorbents.
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The Synthesis of Amide and its Bioisosteres
Authors: Zechun Yang, Yuanyuan Liu, Minghui Liang, Mei Wang, Xiaoyuan Bi, Maoyuan Qu, Peng Zhan and Haiyong JiaAvailable online: 26 June 2025More LessAmide bonds represent crucial functional groups in numerous biomolecules and pharmaceuticals, characterized by distinct structures and properties, and are essential for drug synthesis. By employing a bioisosteric replacement strategy, innovative drug architectures can be devised that circumvent existing patent protections, thereby offering an effective avenue for the discovery of new drug candidates. This review primarily introduces the current synthetic methodologies for amides and their bioisosteres. Additionally, it discusses the advantages and disadvantages associated with various functional groups. A comparative analysis of the differing properties of amides and their bioisosteres within compounds is also presented.
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Recent Advances in the Chemistry of Tetrazole Derivatives-A Quinquennial Update (Mid-2019 to date)
Available online: 12 June 2025More LessDue to their advantageous physicochemical properties, metabolic stability, and bioisosterism with carboxylic acid and amide groups, tetrazole derivatives represent a valuable class of heterocycles that play a crucial role in medicinal chemistry and drug development. Advances in chemistry have enabled the versatile synthesis of tetrazole-based compounds. Therefore, optimizing the potential of tetrazoles to produce lead compounds requires effective synthetic access to a wide range of derivatives. According to the published papers, there are several methods for preparing tetrazole and its mono- and disubstituted derivatives, including 5-substituted 1H-tetrazoles, 2-substituted 1H-tetrazoles, 2,5- and 1,5-disubstituted, fused heterocycles, tetrazole derived hybrid azaheterocycles, etc. The use of tetrazoles as ligands, in bridging roles, in multiple tetrazole syntheses, and in other heterocyclic ring forms is also demonstrated. Alkylation, nucleophilic and electrophilic substitution in the side chain, electrophilic substitution at the ring carbon atom, and the effect of the reagents used are among the chemical characteristics of tetrazoles that are investigated. This mini-review also examines synthetic processes and discusses their benefits and drawbacks in this field of study.
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A Short Review on the Synthesis of 3,9-Disubstituted β-Carbolines: Unveiling Potent Anticancer and Antibacterial Properties
Authors: Siti Zafirah Zulkifli, Puteri Hana Megat Izzwan and Noor Hidayah PungotAvailable online: 02 June 2025More LessThe relentless rise in cancer incidence has sparked an urgent quest for a treatment. For centuries, natural product resources have been the bedrock of medicinal and pharmaceutical industries, capturing the interests of researchers to explore more on the potential of natural products to treat illnesses. Above all, β-carbolines derived from alkaloids are well-known for their various biological and pharmacological properties. In this work, we review the methodologies to synthesize 3,9-disubstituted β-carbolines framework through Pictet–Spengler, metal-catalysed cross-coupling, and multicomponent reactions. In addition, this study aims to investigate how the structural modifications affect their biological activities, with an emphasis on anticancer and antibacterial properties. Besides, the modifications at the C-3 and N-9 positions were evaluated for efficiency and selectivity towards 3,9-disubstituted β-carbolines. This article also highlighted the adaptability of 3,9-disubstituted β-carbolines scaffolds for further use in drug development.
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Domino Reactions through Metallaphotoredox Catalysis
Available online: 23 May 2025More LessThe exploitation of visible light as a cheap and natural source of energy has enabled a renaissance of classical radical chemistry with the development of photoredox catalysis. This resurgence is driven by the emergence of versatile photoredox catalysts, including organocatalysts and transition metal catalysts. Especially, the merger of transition metal catalysis with photoredox catalysis, called metallaphotoredox catalysis by MacMillan, has received considerable attention in both photochemistry and organometallic chemistry in the past decade, impressively expanding the synthetic utility of visible-light photocatalysis. Along with many simple reactions, such as cross-couplings or C-H activations, metallaphotoredox catalysis is particularly suitable to the development of more complex domino processes. Indeed, this green and powerful strategy, evolving through the generation of radical species under especially mild conditions, has led to the discovery of many novel green domino reactions not achievable by using single-catalyst systems. This review collects for the first time the recent developments in the field of dual photoredox and metal-catalyzed domino reactions since 2015, illustrating the diversity of green radical domino reactions that can be performed under mild conditions using this emerging methodology. It demonstrates that these visible-light-driven photoreactions are blooming to become a cheaper, safer, and greener alternative in organic synthesis. These findings pave the way for more sustainable and versatile synthetic methodologies in both academic and industrial settings. Along with precedent reports dealing with metallaphotoredox catalysis, this review is the first to focus specifically on domino reactions. It is divided into five sections, treating successively nickel metallaphotocatalysis, copper metallaphotocatalysis, gold metallaphotocatalysis, cobalt metallaphotocatalysis, and palladium metallaphotocatalysis.
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Oligostilbene’s Synthesis: Recent Advances in Metal-mediated and Enzymatic Conversion of Resveratrol Analogues
Authors: Nurain Syazwani Zaki, Andrey A. Mikhaylov and Mohamad Nurul AzmiAvailable online: 09 May 2025More LessOligostilbenes are a class of plant polyphenols derived in nature by enzymatic oxidative oligomerization of resveratrol. This subject has attracted the interest of synthetic chemists due to their structural complexity and wide range of biological activity. The formation of dimeric stilbene oligomers by metallic oxidants and enzymatically catalyzed conversion of resveratrol is covered in this study. A major part of this review is centered on the use of single-electron oxidants to dimerize the stilbenoid monomers. Formation of the coupling products resulting from different coupling modes, regioisomeric outcome with plausible formation mechanism are scrutinized. Great attention is paid to recent (2015-2022) approaches, employing modern synthetic methods.
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A Comprehensive Review on Thiazolidinones and their 5-ene Derivatives: Synthetic Methodologies and Pharmacological Profiles
Available online: 23 April 2025More LessThiazolidinones and their 5-ene derivatives have become pivotal in organic and medicinal chemistry due to their diverse pharmacological potential. These compounds have been widely explored for their therapeutic applications, with thiazolidine-based frameworks yielding numerous biologically active molecules. This review consolidates various synthetic approaches to thiazolidinone and 5-ene derivatives, including core modifications, one-pot or multistage syntheses, and transformations of related heterocycles. The manuscript highlights key pharmacological targets of thiazolidinones, ranging from initial hit compounds to fully developed drugs. Specifically, thiazolidinone-rhodanines often appear as frequent hitters or pan-assay interference compounds in high-throughput screens. Studies have shown that modifications at the C5 carbon, particularly through the addition of a 5-ene fraction, enhance the pharmacological profile of these compounds. Additionally, the review addresses substitutions at the C5 and N3 positions, including 5-ene and carboxyl groups, and discusses the biological utility of these modifications. Integrating pharmacologically active groups within a heterocyclic system often results in enhanced bioactivity. The review highlights innovative synthetic strategies for thiazolidinone derivatives, emphasizing the potential of these compounds to explore a broad spectrum of biological activities through structural diversity and targeted modifications.
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Isolation, Pharmacological Properties, Chemical Syntheses, and Biosynthesis of Isobavachalcone (IBC): A Historical Perspective for the Future Direction
Authors: Puneet Kumar, Kanhaiya Kumar and Jasha Momo H. AnalAvailable online: 22 April 2025More LessIsobavachalcone (IBC) is a prenylated flavonoid, originally isolated from Psoralea corylifolia, a legume used for centuries in traditional Chinese and Indian medicine to treat various health issues. Known for its diverse biological activities-including antibacterial, anti-inflammatory, anti-tumor, antiviral, neuroprotective, and bone-protective effects-IBC has become a focus of scientific study. This mini-review encompasses key studies of IBC, covering its isolation, pharmacological properties, chemical synthesis, and biosynthesis to benefit both chemists and biologists. The unique chalcone structure and prenyl group on the aromatic ring make IBC particularly intriguing for its wide-ranging bioactivities, synthetic approaches, structural variations, and biosynthetic insights that could aid future drug development and clinical applications.
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An In-depth Analysis of India's API Import Trends in Year 2022-23: Focus on the Top 10 Non-Chinese Sources
Authors: Bhupesh Samant, Ghouse Modin N. Mamdapur and Vishal MenonAvailable online: 03 April 2025More LessBackgroundIndia and China are pivotal players in the global Active Pharmaceutical Ingredient (API) market, and their interdependence is evident through intricate import-export dynamics within the sector. However, this symbiotic relationship faces stiff competition from counterparts in Europe, the USA, and LATAM. Specific factors drive India's procurement of certain APIs from nations beyond China, significantly impacting the economic landscape of Southern Asia. Interpreting these factors that influence import trends in the API market is necessary to strategize the future API demand-supply.
ObjectiveThis review focuses on the top 10 API imports into India in the year 2022-23 from countries other than China. The aim is to provide a comprehensive understanding of these crucial pharmaceutical components, including their applications, mode of action, and industrial synthesis processes. The review also seeks to illuminate diversification initiatives within India's API sector and unravel the reasons behind substantial import trends for each specific API.
MethodsThe process of data collection and its subsequent utilization in analyzing the specific surge in API imports in India during the period of 2020-2022 has been done by five distinct sub-processes: (a) data repossession and preprocessing; (b) development analysis of article publications; (c) distribution analysis of articles by subject, country, application, mode of action and synthesis; (d) scientific teamwork analysis among authors; and (e) development and discovery analysis of research topics. In the review, for each API, a framework has been provided that includes application information, synthesis with reaction scheme, price structure, and the reasons for the high import demand.
ResultsThe escalation of import volumes of specific Active Pharmaceutical Ingredients (APIs) into India from sources outside of China can be attributed to several key factors. Among these are the implementation of revised Indian internal policies, approval for drug formulation by authorized agencies, a heightened reliance on bio-enzymatic API synthesis processes within Europe in contrast to China, the establishment of new research centers in India, and a notable surge in the incidence of certain diseases within the country. Additionally, India's burgeoning population, coupled with increased consumption of animal-derived food products, has contributed to heightened demand for APIs sourced from alternative markets than the Chinese market. These factors collectively underscore the complexity of the pharmaceutical supply chain and the various influences driving import dynamics within the Indian market.
ConclusionA thorough examination of API imports into India during the fiscal year 2022-23 has unveiled significant trends, applications, and underlying rationales driving import patterns. The consolidation of manufacturing processes has provided invaluable insights into the synthetic research pathways associated with each API listed. The data serves as a critical resource for stakeholders within the pharmaceutical sector, facilitating informed strategic decision-making and fostering advancements in India's API industry.
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A Comprehensive Review on Plant-based Fluorophores and their Diverse Applications
Available online: 27 March 2025More LessFluorescence, a phenomenon where substances emit light upon excitation, has been largely explored in synthetic materials. However, plants have been harnessing this property for millions of years, with various extracts exhibiting fascinating fluorescent properties. This review delves into the realm of plant extracts displaying fluorescence, highlighting their diverse applications, mechanisms, and potential uses. This study summarizes various classes of fluorescent phytochemicals, including alkaloids, phenolics, and terpenoids, coumarins, anthocyanins, and discusses their excitation and emission spectra. The review also examines the structural dependent functional diversity of plant secondary metabolites influencing fluorescence. Furthermore, the applications of fluorescent plant extracts in fields like biomedicine, food technology, and environmental monitoring in combination with bioimaging, biosensing, and optoelectronics are also highlighted. This comprehensive review aims to spark further research into the untapped potential of fluorescent plant extracts, unlocking new avenues for scientific discovery and innovation.
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Advances in the Application of Mass Spectrometry in the Study of Alkaloid Structure
Available online: 18 March 2025More LessAs an efficient analytical method, mass spectrometry can identify the structure of alkaloid compounds, providing important support for drug development and clinical applications. In this manuscript, the basic principles and rules of alkaloid mass spectrometry analysis are reviewed, and the breakage modes and characteristic ions of different types of alkaloids in mass spectrometry are emphatically introduced. By discussing the fragmentation behavior of various alkaloids in negative ion mode and positive ion mode in detail, the mass spectrometry cleavage laws of various alkaloids are revealed, and the application of these laws in practical detection is summarized.
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Exploring Lichen-Fungi Biosynthetic Pathways: Evaluating the Pharmacological Activity of Olivetoric Acid and Biosynthetically Similar Metabolites
Available online: 26 February 2025More LessLichens, symbiotic organisms, produce a diverse array of bioactive compounds, including depsides and depsidones. These compounds exhibit potent biological activities, such as antioxidant, antimicrobial, anti-inflammatory, and anticancer properties. This review explores the biosynthesis of specific compounds, focusing on the role of polyketide synthases and cytochrome P450 enzymes. The majority of the review will focus on the pharmacological potential of olive-toric acid and biosynthetically similar compounds, highlighting their potential as future drug leads. Further research is needed to exploit the therapeutic potential of these natural products fully.
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Recent Advances in the Chemistry of Thienopyranone Heterocycles: Synthesis, Reactivity, and Application
Available online: 13 January 2025More LessThiophene and pyranone are valuable heterocyclic compounds that play a crucial role in the development of new drug molecules. The combination of thiophene and pyranone moieties in hybrid structures has opened exciting possibilities for various applications, leading to the discovery of thienopyranones (Thpyns), such as 5H-thieno[3,2-b]pyran-5-one, 2H-thieno[2,3-b]pyran-2-one, 4H-thieno[3,2-c]pyran-4-one, 7H-thieno[2,3-c]pyran-7-one, all of which exhibit intriguing properties. This review offers an in-depth analysis of the preparation methods and chemical reactivity of thienopyranones
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