Quinoline is one of the most widely studied scaffold due to its high biological activities like antimalarial, antitubercular, antitumor, anti-inflammatory, antifungal, antiprotozoal, etc. this compound also has corrosion resistant, fluorescent properties, which make it industrially also important. There are various conventional methods to synthesize this scaffold, but these have several drawbacks like harsh conditions, susceptible functional group get affected. These drawbacks can be overcome by the use of green methods. These methods include Tandem/domino methods, cascade synthesis, cyclization/annulation by C-C, C-N bond formation, use of microwave, ultrasonication, ionic liquids, recyclable nano-catalyst, solid phase synthesis, solvent free synthesis, water as solvent, ball milling, use of cheap, easily available metal catalyst etc. Nowadays various naturally occurring biomass as raw material are also utilized as one of the reactant. These green methods reduce hazards to human as well as environment. This review provides an overview of recent discoveries in green synthetic methods of quinoline scaffold, and various applications of quinoline scaffold in medicine and other industrial applications.
In the present work, a series of amino acid–indole ester conjugates were prepared by incorporating the pharmacologically significant indole scaffold with amino acid moieties. To achieve this, Z- or Boc-protected amino acids were first activated via either the benzotriazole approach or the DCC-mediated coupling procedure and then esterified with 2-hydroxymethylindole to generate the target indole-based amino acid esters. Structural characterization of the synthesized compounds was accomplished using a combination of spectroscopic and analytical methods, including IR, NMR, mass spectrometry, and elemental analysis. Evaluation of the antioxidant properties revealed that the tryptophan-containing derivative (4) and the methionine-containing derivative (2) displayed the most pronounced antioxidant activity relative to the reference compound BHA.
We report a metal-free and temperature-controlled strategy for the tandem deallylation and oxidation of allyl ethers using an iodine/dimethyl sulfoxide (I2/DMSO) system. This methodology enables the one-pot conversion of allyl-protected substrates into the corresponding aldehydes and ketones under mild reaction conditions, with product selectivity governed by temperature. At a moderate temperature (60°C), the reaction selectively affords the deallylated alcohol intermediate, whereas at an elevated temperature (100°C), further oxidation leads to the corresponding carbonyl compounds. Under optimized conditions employing iodine as catalyst and sulfuric acid as additive, the desired products are obtained in good to excellent yields (82–92%).
Dear scientists and readers,As the Organic Communications team, we proudly prepeare each new issue with the same excitement as with our very first issue for the last 19 years.The first issue of 2026 represents both the change of the calendar and a new symbol of maturity and renewed vision of building a culture for the future.Science Unites: A Shared HeritageWhen I look back to 2008-2009 A significant moment stands out in my memory. At the beginning of our journey, among the very first manuscripts submitted to Organic Communications, one was from Palestine and another from Israel.This coincidence demonstrates us the true mission of science: Science is universal; it has no country or homeland. Beyond the political borders, arguments and national concerns science is the most enduring bridge built for shared aspirations of humanity.Scientists, as they have throughout history, continue to act together to carry this great heritage into the future.We owe this to our past.A Numerical Portrait of a 19-Year JourneyIn line with this universal vision, our journal today reaches a global audience, featuring scientific contributions from 50 different countries spanning from Scandinavia to Australia. According to Web of Science data, the interest garnered by the 347 articles we have published to date is a clear indicator of our commitment to quality:Global Impact: From a journey that began with just 4 citations, we have become a point of reference, receiving over 260 citations annually in 2024 and 2025.Academic Trust: Web of Science data (as of 25.01.2026) shows that the vast majority of our 2,169 total citations (specifically 2,018) are not self-citations. A self-citation rate of only 6.7% proves how naturally and objectively our work is accepted worldwide. Articles published in Organic Communications have been cited in highly prestigious journals across various fields—primarily Chemistry, followed by Pharmacology, Pharmacy, Polymer Science, Biochemistry and Molecular Biology, Engineering, Infectious Diseases, Science and Technology, Material Science, Physics, and Environmental Sciences. This low self-citation rate is a refreshing data point in a publishing world often plagued by citation manipulation; it stands as a testament to the mutual trust between our authors, readers, and ourselves. We reaffirm our commitment to these principles and our role as a reliable pillar of the scientific community.Respect for Scientific Effort: We believe that every effort is worth sharing. We have advocated that not only successful outcomes but also honestly reported "negative results" contribute to scientific methodology and prevent other researchers from wasting time and effort. Despite this inclusive approach, we have never compromised on academic rigor. Over the past 19 years, we have maintained a high scientific standard by providing constructive criticism and declining many more studies than we published. Recognizing the Peer Review system as a tool for collective learning and growth, our principled, transparent, and accountable decision-making process remains the greatest sign of our respect for all scientific contributors.2026: A new modelAs we are getting closer to our 19th year, we are excited to share significant developments with our readers:i)New Layout: Our papers now will be more user friendly and professional; it will keep it easier for everyone to read in an efficient way.ii) Continuous Publication Model: To keep pace with the accelerating nature of scientific publishing, we are adopting a continuous publication model. Accepted manuscripts will be rapidly converted into HTML and PDF formats, assigned a DOI, and published online without waiting for the completion of an issue. XML files will also be generated for indexing databases. AcknowledgementsSince the beginning of this road, we have supported Open Access philosophy and with this same approach we will keep distributing the knowledge without institutional barriers.I would like to extend my sincere gratitude to the members of our Editorial Board, to the more than one thousand authors from 50 countries who have contributed to our journal, and to our dedicated reviewers whose rigorous peer-review efforts have ensured the quality of our publications.I wish you all a year driven by science, bringing peace and happiness to all humanity.
Rhodanine, also known as 2thioxo-4-thiazolidinone, is a five-membered cyclic compound containing sulfur, oxygen and nitrogen, and its compounds have found significant applications in photochemistry, medicinal chemistry, biochemistry, and various other industries. The -NH group in rhodanine compounds allows for hydrophobic interactions, hydrogen bonding, and complexation with metal ions. Analytical chemists have exploited these properties in order to use rhodanine derivatives as sensor materials, and developed sensors suitable for use in many areas. Rhodanine derivatives exhibit properties significantly superior to many organic compounds known as sensor materials, making them highly suitable as sensor materials. This review provides an overview of the uses and applications of rhodanine derivative molecules as sensor materials in various analytical techniques, including colorimetric, fluorescence, or electrochemical methods.
A process-optimized, one-pot multicomponent reaction catalyzed by DBUHI3 was developed, enabling the synthesis of diverse 1,4-dihydropyridines (1,4-DHPs), a class of bioactive nitrogen heterocycles from substituted benzaldehydes, ethyl acetoacetate, and ammonium acetate under mild conditions in DMSO. The methodology afforded good to excellent yields for a variety of aryl aldehyde substrates bearing both electron-donating and electronwithdrawing groups. Structural confirmation was achieved through IR, 1H NMR, 13C NMR, and HRMS analyses. This work not only summarizes key synthetic strategies but also provides a practical, sustainable route to the preparation of 1,4-DHPs, supporting further medicinal and synthetic exploration.
A series of new dispiropyrrolidine oxindole derivatives (8-10) were successfully synthesised with yield of 57 to 95% via one-pot 1,3-dipolar cycloaddition reaction of azomethine ylides and characterised by various spectroscopic techniques such as NMR, FT-IR, and HRMS. The compounds were evaluated for their activity against methicillin-resistance Staphylococcus aureus (MRSA). Among the compounds, compound 9f and 9g exhibit moderate activity against MRSA with minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of 250 µg/mL and 325 µg/mL, respectively. The binding energies and interactions of both compounds with S. aureus adhesion proteins such as sdrE, CIfA and FnBPA were further studied through molecular docking studies. Compound 9f (-8.5 ± 0.00 kcal/mol) showed a strong binding affinity than compound 9g (-7.5 ± 0.20 kcal/mol) particularly towards FnBPA adhesion protein. The molecular docking results revealed that the interactions between the compounds 9f and 9g with target proteins correlate with the observed MRSA inhibitory activity, highlighting their potential as promising lead candidates for anti-MRSA drug development.
In recent years, there has been a growing interest in developing green and sustainable synthetic strategies for chalcones, aiming to minimize waste, reduce the use of hazardous chemicals, and enhance the overall efficiency of the reactions. This review provides an overview of various green synthesis approaches for chalcones and their derivatives, emphasizing environmentally friendly techniques such as solvent-free reactions, microwave-assisted synthesis, ultrasound-assisted synthesis, and enzyme-catalytic methods. Additionally, the biological activities of chalcones synthesized via green methods are explored, underscoring their potential in drug development and therapeutic applications
This review focuses on the design, synthesis, and biological evaluation of novel heterocyclic compounds derived from β-diketones and cyanomethylene reagents through multicomponent and green synthetic methodologies. The study encompasses a wide range of heterocyclic scaffolds, including xanthene, chromene, chromenone, coumarin, acridine, quinoline, thiazole, thiophene, and spiro-heterocycles containing nitrogen, oxygen, and sulfur. A variety of catalysts were employed such as DBSA, P-TSA, NbCl₅, and nano-magnetic composites like CuFe₂O₄/chitosan to optimize reaction conditions for eco-friendly and high-yielding transformations. The developed synthetic strategies included one-pot, microwave-assisted, and solvent-free techniques, resulting in efficient routes to complex molecular architectures. The biological activity of the synthesized compounds was extensively screened, with several candidates exhibiting promising antimicrobial, antifungal, anticancer, and kinase-inhibitory properties. Structure-activity relationship (SAR) studies indicated that specific heteroatom substitutions enhanced biological potency, particularly in xanthene and chromenoquinoline derivatives. This work contributes to advancing heterocyclic chemistry by introducing new reaction pathways, novel molecular frameworks, and bioactive agents with potential pharmaceutical applications.
of the most common chronic illnesses and a major cause of death in recent years is diabetes mellitus (DM). As a result, strategies for identifying, stopping, or delaying this illness and its co-morbidities have long been debated. Patients with diabetes mellitus (DM), especially those with type 2 DM, are now recommended to modify their diet and exercise routines and to gradually go from monotherapy, dual therapy, and multi-agent therapy to insulin delivery as the disease progresses. While there have been advancements, the search for the "ideal" diabetes medication is currently ongoing. There is still much disagreement on the molecular pathways that regulate DM. Since each drug has different risks, drawbacks, side effects, and modes of action, selecting the best course of treatment requires careful consideration. In this article, many classes of anti-diabetic medications were reviewed that are on the market, their uses, and their modes of action. This study will focus especially on the more recent and/or commonly prescribed classes. Since these medications influence the pathways in various cellular systems and organs, encouraging metabolic modifications responsible for either favorable or detrimental consequences, special attention will be paid to how they affect cellular metabolism. It is imperative to thoroughly examine this essential attribute before recommending an antidiabetic. The most common kind of diabetes is type-2, and oral anti-diabetic medications are essential for managing it. Sulfonylureas, thiazolidinediones, meglitinides, sodium glucose co-transporter (SGLT2), a-glucosidase inhibitors, dipeptidyl peptidase-(IV) inhibitors, and biguanides are some of the classes of oral anti-diabetic medications that are marketed today. To avert a possible public emergency, the scientific community has been working hard to create better and more sustainable synthetic methodologies towards these anti-diabetics as the burden of type-2 diabetes continues to rise. The several documented synthetic approaches for anti-diabetic medications in the aforementioned classes are summarized in this article. We hope that this compilation will provide organic and medicinal chemists with an invaluable comprehensive basis and reference source for the continued development of DM medicines.
A series of new dispiropyrrolidine oxindole derivatives (8-10) were successfully synthesised with yield of 57 to 95% via one-pot 1,3-dipolar cycloaddition reaction of azomethine ylides and characterised by various spectroscopic techniques such as NMR, FT-IR, and HRMS. The compounds were evaluated for their activity against methicillin-resistance Staphylococcus aureus (MRSA). Among the compounds, compound 9f and 9g exhibit moderate activity against MRSA with minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of 250 mu g/mL and 325 mu g/mL, respectively. The binding energies and interactions of both compounds with S. aureus adhesion proteins such as sdrE, CIfA and FnBPA were further studied through molecular docking studies. Compound 9f (-8.5 +/- 0.00 kcal/mol) showed a strong binding affinity than compound 9g (-7.5 +/- 0.20 kcal/mol) particularly towards FnBPA adhesion protein. The molecular docking results revealed that the interactions between the compounds 9f and 9g with target proteins correlate with the observed MRSA inhibitory activity, highlighting their potential as promising lead candidates for anti-MRSA drug development.
Here, we outlined the synthesis of pyrroles, pyrazoles, imidazoles, pyridines, pyrimidines and pyrazines using nanocatalysts. For example, quinazolin-4(1H)-ones 49a-c were produced by the multicomponent reaction between isatoic anhydride (48), various amines 3, substituted aldehydes 7 in water using Fe3O4 nanoparticles. These N-heterocyclic compounds are essential in pharmaceutical fields. Using nanocatalysts in this synthesis is very important because these catalysts lie under the green synthesis or sustainable synthesis that most researchers headed in recent years, due to nanocatalysts have a large surface area compared with their volume making a larger chance of reaction between the reactants. In addition, they reduce side reactions, improve selectivity, enhance recycling rates, and enable cleaner, faster, and less expensive reactions. Furthermore, they show self-recovery and excellent product yield.
The use of deep eutectic solvents (DESs) not only promotes the reaction but also aligns with green chemistry principles due to their biodegradability, low toxicity, cost-effectiveness, and recyclability. A green and efficient one-pot, three-component synthesis of 2-amino-4-phenyl-1,8-naphthyridine-3-carbonitrile derivatives has been developed using lactic acid-based DESs. The reaction, involving 2-aminopyridine, aromatic aldehydes, and malononitrile, proceeds under mild conditions in a DES composed of lactic Acid, maltose, and amla (Indian gooseberry) Juice (3:1:3 molar ratio) without the need for any additional catalysts or additives. Among various DESs evaluated, this ternary mixture exhibited the highest catalytic activity, delivering products in good to excellent yields. The methodology offers notable advantages, including high atom economy, reduced reaction time, and elimination of hazardous solvents. The synthesized naphthyridine derivatives were structurally confirmed by FTIR, NMR, and HRMS analyses. This study highlights the potential of natural-product-based DESs as sustainable media for multicomponent heterocycle synthesis, with significant implications for the field of organic synthesis and green chemistry.
In search for novel antidiabetic agents, a new series of substituted 2-benzylidene-1-indanone derivatives were synthesized via crossed Adol condensation reaction. The structures of the synthesized compounds were determined using various spectroscopic techniques, including HREIMS, FTIR, and NMR. The enzyme inhibitory activities of the target analogues were assessed using in vitro assays. The tested compounds demonstrated inhibitory potential against alpha-amylase, as indicated by their IC50 values ranging from 17.7 to 28.2 mu M as compared to standard drug acarbose with IC(50 )value of 30.2 +/- 1.9 mu M. Furthermore, molecular docking study was conducted to elucidate the binding interactions of the compounds within the alpha-amylase enzyme binding pocket (PDB ID 2QV4). The results of molecular docking studies indicated that compounds 3m, 3c, 3d has the lowest binding energy (-9.8,-9.3 and-9.4, respectively). The structure-activity relationship (SAR) analysis revealed that alteration in the inhibitory activities of alpha-amylase enzymes was provided by distinct types of substituents attached to either ortho-or para positions of the phenyl group. The combined SAR and docking results highlight the importance of para-position substitution on ring A for optimal activity, particularly when introducing moderately electron-withdrawing groups such as chlorine, fluorine, and bromine. Thus, in the pursuit of developing newer antidiabetic agents, the in silico ADME prediction was carried out with promising physicochemical, drug likeness and ADME properties which indicated that some compounds were considered drug-like as they do not violate any of the rule-based filters of Lipinski.
A simple and efficient method has been developed for the synthesis of xanthene derivatives using various aromatic aldehydes and 2-naphthol under solvent-free conditions. In this procedure, ferric phosphate (FePO4) is used as an efficient and reusable heterogeneous Lewis acid catalyst for the synthesis of various derivatives of 14-aryl-14H-dibenzo[a,j]xanthene (3a-3m) in excellent yields (87-96%). The present method affords notable advantages such as short reaction time, simple workup procedure, reusability of the catalyst and high conversions of the products. All products have been confirmed by their melting points and spectroscopic techniques such as 1H NMR, 13C NMR, IR spectroscopy and mass spectrometry.
Cyclohexanecarboxamido hydrazones constitute a promising new class of therapeutic candidates exhibiting notable antioxidant, antibacterial, anticancer, and anti-inflammatory activities. In contrast to conventional hydrazones, these compounds combine the versatile hydrazone pharmacophore with a drug-like cyclohexyl amide moiety, a structural feature that may improve bioavailability, metabolic stability, and overall therapeutic performance. This study shows that, a series of sixteen novel derivatives. 2-(1-(4-chlorophenyl)cyclohexane-carboxamido)-N '-arylidenoacetohydrazides (8a-8p), were synthesized through a six-step pathway starting from 2-(4-chlorophenyl)acetic acid. The key hydrazide intermediate was condensed with various substituted aromatic aldehydes, affording the target hydrazones in good to excellent yields (72-86%). Structures of all compounds were confirmed by 1H NMR, 13C NMR, IR, LC-MS, and elemental analysis. The synthetic methodology demonstrated broad functional group tolerance, thus providing a reliable platform for generating structurally diverse analogues in consistently high yields.
A one-pot, ionic-liquid mediated synthesis has been developed for novel thiazolidine-4-ones containing a pyrazole and thiazole hybrid. This was achieved using a three-component reaction of 2-aminothiazole, pyrazole-3-aldehyde, and mercaptoacetic acid in [bmim][PF6]. The whole procedure is robust and straightforward. By employing this protocol, a series of novel thiazolidine-4-ones containing pyrazole and thiazole hybrids were prepared in good yield (56-88%) and their preliminary cyclooxygenase activities were also studied and reported. The compounds 3h and 3k show the top-tier selective index for cyclooxygenase enzyme, in comparable with celecoxib as a standard.
A series of nitrile derivatives of Petromurin C were synthesized and assessed for their cytotoxic effects on tumor cell lines and inhibitory activity against Mycobacterium tuberculosis (M.tb H37Ra). Bromoalkyl nitriles (Br(CH2)nCN; n=1-5) and (o-, m-, p-) bromomethyl benzonitriles were used as alkylating reagents. The majority of the syntheses consisted of O-alkylated derivatives in which the two NH group were not alkylated, as expected from the treatment of petromurin C with K2CO3 in DMF followed by treatment with alkylating reagents. Similarly, treatment of Petromurin C with NaH in DMF and the treatment with alkylating reagents yielded both OR and bis-NR alkylated structures. In the first method, 7 different O-alkyl Petromurin C derivatives were obtained. The second method yielded 7 different Petromurin-C derivatives containing both Oalkyl and bis-N-alkyl groups. Notably, compounds 1-4 and 7-10 demonstrated selective inhibitory activity against the acute myeloid leukemia cell line MV4-11, with IC50 values ranging from 12.96 to 20.00 mu M. Compound 15 exhibited a minimum inhibitory concentration (MIC) of 6.25 mu M against M.tb H37Ra. Importantly, all synthesized compounds showed negligible inhibition (below 50%) against human normal cell lines L-02 and 293T at a concentration of 100 mu M. These findings suggest that the compounds possess high efficacy and low toxicity, indicating their potential as novel therapeutic agents for the treatment of leukemia and tuberculosis.
A novel series of amide-based soluble epoxide hydrolase (sEH) inhibitors was rationally designed by incorporating 2,4-dichlorobenzyl and terminal heterocyclic moieties into a central amide scaffold. The target compounds were synthesized and structurally confirmed as new chemical entities using HRMS, H-1 NMR, and C-13 NMR spectroscopy. Molecular docking studies of the synthesized inhibitors with sEH revealed key hydrogen bonding interactions with Asp335, Tyr383, and Tyr466, along with pi-pi stacking interactions with His524 and Trp525, indicating their effective binding to the sEH active site. In vitro biological evaluation showed that all synthesized derivatives exhibit potent sEH inhibitory activity at both 10 and 100 nM, with compound 11 emerging as the most promising lead for further development of potent anti-inflammatory agents.
We have thoroughly investigated the C-benzylation of pyrrole (1) using different second and third generation ionic liquids (ILs). The pyrrole C-benzylation is achieved with benzyl halides, mesylate, and tosylate selectively at C2 position in good yield. Moreover, minimal byproducts under relatively mild conditions in hexaethylene glycol substituted imidazolium based ILs (hexaEGILs) have been observed. 2-Benzyl pyrrole (3) was synthesized in high yield from pyrrole (1) and benzyl bromide (2a) in the presence of [hexaEGmim][OMs] and [dihexaEGim][OMs] as two different tailor-made ILs as catalysts (10 mol%) in MeCN at 80 oC within an hour.
