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Item Recent advancement on peptide-based fluorescent/colorimetric sensors for metal ion detection(Wiley, 2025-10) Khungar, Bharti; Sakhuja, RajeevModernization and technology development lead to an increase in the contamination of toxic metal ions into the direct environment. Unlike the other pollutants, metal ions cannot be degraded by chemical or biological ways, and are hard to abolish. To check and regulate metal ion contamination, numerous advancements have been wittnessed to develop the materials that can sense particular metal ion selectively with synchronized variation in their optical behavior. In this realm, peptide serves as a toolbox with exceptional advantages over other chemical-based metal sensors owing to specific properties, such as biocompatibility, low toxicity, high selectivity, and environment friendly nature. In addition, short peptides affixed with fluorophores have been rationally designed to exhibit high specificity for metal ions by providing multiple coordination sites in their side chains with functionalities, including thiols, amines, carboxyls, and imidazoles, exhibiting promising applications in environmental monitoring, medical diagnostics, and biochemical research. Under this realm, fluorescence-based peptide sensors have been studied for rapid and on-site detection of metal ions, including Fe3+, Ni2+, Ag1+, Cu2+, Zn2+, Cd2+, Pb2+, Hg2+, As3+, and Al3+ following various photophysical pathways. This review showcases the recent advancements on the development of peptide-fabricated metal sensing agents and their mechanism of metal binding accompanied with photophysical changes.Item Steroid-triazole conjugates: A brief overview of synthesis and their application as anticancer agents(Elsevier, 2023-09) Sakhuja, RajeevSteroids are biomolecules that play pivotal roles in various physiological and drug discovery processes. Abundant research has been fuelled towards steroid-heterocycles conjugates over the last few decades as potential therapeutic agents against various diseases especially as anticancer agents. In this context various steroid-triazole conjugates have been synthesized and studied for their anticancer potential against various cancer cell lines. A thorough search of the literatures revealed that a concise review pertaining the present topic is not compiled. Therefore, in thus review we summarize the synthesis, anticancer activity against various cancer cell lines and structure activity relationship (SAR) of various steroid-triazole conjugates. This review can lay down the path towards the development of various steroid-heterocycles conjugates with lesser side effects and profound efficacy.Item Rhodium-catalyzed regioselective C3ar functionalization of tyrosines with maleimides and its late-stage peptide exemplification(ACS, 2023-10) Sakhuja, RajeevPyridyloxy-directed Rh(III)-catalyzed regioselective C3Ar–H alkenylation of protected tyrosines was achieved with N-aryl and N-alkyl maleimides, furnishing a series of maleimide-appended tyrosine-based unnatural amino acids in good yields. Further, the late-stage exemplification of the strategy was successfully accomplished on tyrosine-containing dipeptides, tripeptides, and tetrapeptides in moderate reactivity. Also, the chemical applications of the strategy were successfully executed toward nailing tyrosine with other amino acids via a maleimide linker and intramolecular hydroarylation to produce tyrosine-centered stapled products and succinimide-glued macrocyclized products, respectively.Item Palladium-catalyzed regioselective C-arylation and C, N-diarylation of N-Aryl-2, 3-dihydrophthalazine-1, 4-diones using diaryliodonium salts(Thieme, 2023) Sakhuja, RajeevRegioselective C-arylation and C,N-diarylation in 2-aryl-2,3-dihydrophthalazine-1,4-diones has been successfully accomplished with diaryliodonium salts under base-mediated slightly modified Pd-catalyzed conditions. These ligand-driven transformations provided a variety of diversely decorated bi(hetero)aryls in good-to-excellent yields, while N-arylated product could be obtained under similar Pd-catalyzed conditions in the absence of a ligand.Item Rhodium-catalyzed regioselective c7ar-functionalization of tryptophan with quinones and its late stage peptide exemplification(Wiley, 2023-11) Sakhuja, RajeevPivaloyl-directed Rh(III)-catalyzed regioselective C7Ar-H functionalization of protected tryptophans were accomplished with 1,4-benzoquinones, furnishing a series of quinone-appended tryptophan-based unnatural amino acids in high yields. Further, the late stage functionalization on tryptophan-containing dipeptides was achieved with 1,4-benzoquinones in moderate reactivity.Item Iridium-catalyzed diacylmethylation of tyrosine and its peptides with sulfoxonium ylides(RSC, 2024-06) Sakhuja, RajeevPyridyloxy-directed Ir(III)-catalyzed diacylmethylation of protected tyrosines was achieved with alkyl and (hetero)aryl sulfoxonium ylides, furnishing tyrosine-based unnatural amino acids in good yields. Furthermore, the late stage exemplification of the strategy was successfully accomplished in tyrosine-containing dipeptides, tripeptides and tetrapeptides in moderate yields. This methodology is distinguished by its site-selectivity, tolerance of sensitive functional groups, scalability, and retention of the chiral configuration for tyrosine motifs.Item Novel isatin conjugates endowed with analgesic and anti-inflammatory properties: design, synthesis and biological evaluation(Taylor & Francis, 2024-12) Sakhuja, RajeevThis study aimed to develop novel molecular hybrid conjugates integrating isatin, rhodanine, and phthalimide pharmacophores to create effective analgesic and anti-inflammatory agents with improved safety profiles over existing treatments.Item RH(III)-catalyzed fabrication of [4,3,1]-bridged azaheterocycles using quinone monoacetals(ACS, 2025-06) Sakhuja, RajeevA rhodium-catalyzed annulation strategy for the fabrication of cyclohexanone-bridged indazolones and other related diazole-ones and diazine-ones was established using quionone monoacetals under mild conditions. On the other hand, the use of 4-hydroxy-4-methylcyclohexa-2,5-dienone under the optimized Rh-conditions produced an ortho-CAr-arylated product in moderate reactivity. Mechanistic studies suggested that the coupling proceeded via one-pot C–H activation-Michael/hetero-Michael additions into the enone moiety. Interestingly, the [4,3,1]-bridged-1,2-dihydro-3H-indazol-3-ones underwent unexpected migratory aromatization in acidic condition to produce 3-hydroxy-14H-benzo[c]indazolo[1,2-a]cinnolin-14-ones in high yields.Item Synthesis, Antibacterial Evaluation, and Computational Studies of a Diverse Set of Linezolid Conjugates(MDPI, 2022) Sakhuja, RajeevThe development of new antibiotics to treat multidrug-resistant (MDR) bacteria or possess broad-spectrum activity is one of the challenging tasks. Unfortunately, there are not many new antibiotics in clinical trials. So, the molecular hybridization approach could be an effective strategy to develop potential drug candidates using the known scaffolds. We synthesized a total of 31 diverse linezolid conjugates 3, 5, 7, 9, 11, 13, and 15 using our established benzotriazole chemistry with good yield and purity. Some of the synthesized conjugates exhibited promising antibacterial properties against different strains of bacteria. Among all the synthesized compounds, 5d is the most promising antibacterial agent with MIC 4.5 µM against S. aureus and 2.25 µM against B. subtilis. Using our experimental data pool, we developed a robust QSAR (R2 = 0.926, 0.935; R2cvOO = 0.898, 0.915; R2cvMO = 0.903, 0.916 for the S. aureus and B. subtilis models, respectively) and 3D-pharmacophore models. We have also determined the drug-like properties of the synthesized conjugates using computational tools. Our findings provide valuable insight into the possible linezolid-based antibiotic drug candidates.Item Regiodivergent Synthesis of Cinnoline-Fused Indazolones through Pd-Catalyzed Annulation of 1-Arylindazolones with Allenoates(ACS, 2022-01) Sakhuja, RajeevA tender-hearted Pd(II)-catalyzed C–H activation of 1-arylindazolones followed by an oxidative [4 + 2] annulation reaction has been accomplished, engaging allenoates as annulating partners. Using this strategy, two different regioisomeric forms of cinnoline-fused indazolones possessing internal and exocyclic double bonds were synthesized in acetic acid and dioxane, respectively. Mild and aerobic conditions, avoiding the use of any metal–oxidant, highlights the rewards of this oxidative annulation protocol.