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Ravula Sharada Nukala Satheesh Kumar Thirukovela Narasimha Swamy Sirassu Narsimha Dasari Gouthami Kurma Srimathi Bandari Srinivas 《Russian Journal of General Chemistry》2022,92(4):702-708
Russian Journal of General Chemistry - In the current study, some new quinoxaline linked 1,3,4-oxadiazole sulfonamide hybrids have been designed, synthesized and characterized by IR, 1H and 13C... 相似文献
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Sreerama Rakesh Kumar N. Manoj Nukala Satheesh Kumar Sucharitha E. Ramya Babu H. Ramesh Narsimha Sirassu 《Russian Journal of General Chemistry》2021,91(12):2515-2521
Russian Journal of General Chemistry - This study is devoted to the efficient and practical synthesis of a novel series of pyrido[4,3-d]pyrimidine derivatives attached to 1,2,3-triazole ring and... 相似文献
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Nagavelli Vasudeva Reddy Sirassu Narsimha Lavudya Sudhakar Kumara Swamy Battula S K Althaf Hussain 《Phosphorus, sulfur, and silicon and the related elements》2016,191(8):1118-1122
Thirteen novel bis-1,2,3-triazole derivatives were synthesized under copper (I)-catalyzed azide-alkyne 1,3-dipolar cycloaddition of N,N′-(hexane-1,6-diyl)bis(4-methyl-N-(prop-2-yn-1-yl)benzenesulfonamide) with different aryl azides and evaluated their biological activity. All the newly synthesized compounds were confirmed by 1H-NMR, infrared, and elemental analysis and mass spectral studies. The synthesized bis-1,2,3-triazoles were evaluated for their antioxidant activity, and some of them were found to exhibit good to excellent antioxidant activity (IC50: 11.13 ± 1.5 to 98.98 ± 1.7 μM) in comparison with standard references, Trolox (11.73 ± 1.5 μM) and ascorbic acid (3.34 ± 1.8 μM). The bistriazoles also exhibited excellent-to-moderate anti-bacterial activity (MIC: 2.253 to 75 µg mL?1 against Bacillus subtilis, Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa when compared with streptomycin. N,N′-(hexane-1,6-diyl)bis(N-((1-(3,5-dimethylphenyl)-1H-1,2,3-triazol-4-yl)methyl)-4-methyl benzenesulfonamide) has completely cleaved the DNA at a concentration of 100 mg mL?1, and the remaining compounds have partially cleaved the DNA. 相似文献
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An efficient protocol has been developed for the synthesis of fused imidazo[2,1-a]isoindol-5-ones (2a–d) from 2-iodo benzoic acids and N,N-carbonyldiimidazole (CDI) using one-pot Pd-catalyzed C?C bond coupling. The reaction of imidazo[2,1-a]isoindol-5-one (2a–d) with substituted α-bromo ketones in toluene afforded corresponding imidazo[2,1-a]isoindolium derivatives (3a–i) in good yields. The structures of the title compounds were well established on the basis of infrared (IR), 1H NMR, carbon-13 nuclear magnetic resonance (13C NMR), mass spectral data, and elemental analysis (C, H, and N). In vitro antibacterial results revealed that, the compounds 3b and 3i were found to possess an excellent broad spectrum of inhibiting potency against all the tested bacterial strains with minimum inhibitory concentration values ranging from 3.125 to 25?µg mL?1. 相似文献
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Rajkumar Samala Ranadheer Kumar M Ashok Kumar Bapuram Venkatarathnam Nasipireddy Sirassu Narsimha 《Journal of heterocyclic chemistry》2024,61(4):600-610
In this study, we designed and synthesized several novel fused [1,2,3]triazolo [4′,5′:3,4]pyrrolo[1,2-a]thieno[2,3-d]pyrimidine derivatives using in a single [3 + 2] reaction cycloaddition reaction of 3-(3-iodoprop-2-yn-1-yl)thieno[2,3-d]pyrimidin-4(3H)-one ( 4 ) followed by C-C bond coupling with various aryl azides in a PEG-400 medium. All of the newly synthesized compounds were evaluated in vitro for EGFR kinase inhibitory action as well as anti-breast cancer activity against MDA-MB-231 and MCF-7 breast cancer cell lines. When compared to the reference molecule, erlotinib, the majority of the compounds demonstrated adequate efficacy. The most promising compounds, 5g and 5i , demonstrated excellent anticancer activity against both cancer cell lines, with IC50 values ranging from 04.17 ± 0.55 to 8.65 ± 0.89 μM, respectively, as well as excellent kinase inhibitory activities (EGFR: IC50 = 0.467 ± 0.063 and 0.412 ± 0.081 μM). The in silico studies of five potent compounds 5f , 5g , 5h , 5i , and 5k were also carried out to identify the interactions against the EGFR receptor and found that the energy calculations were covenant with the obtained IC50 values. 相似文献
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Sirassu Narsimha Sathesh Kumar Nukala T. Savitha Jyostna M. Ravinder M. Srinivasa Rao N. Vasudeva Reddy 《Journal of heterocyclic chemistry》2020,57(4):1655-1665
In search of better antibacterial and anticancer agents, a series of novel 4-[3-fluoro-4-(morpholin-4-yl)]phenyl-1H-1,2,3-triazole derivatives were synthesized ( 6a - l and 8a - j ) by using 3-fluoro-4-morpholinoaniline, alkyne, and triflyl azide via an in situ generated 4-(4-azido-2-fluorophenyl)morpholine and evaluated for their antibacterial and anticancer activity in vitro. Antibacterial activity against three G+ bacterial strains and anticancer activity against breast cancer cell line (MCF-7) and cervical carcinoma cell line (HeLa) was evaluated. Among all the tested compounds, 6h , 6i , and 8b exhibited potent antibacterial activity against tested gram-positive bacterial strains. The anticancer activity screening results of 8f , 8h , and 8i exhibited potent cytotoxic activity against two cancer cell lines with IC50 values nearer to the standard drug, doxorubicin. The remaining compounds have shown good to moderate activity against the tested cell lines. On the basis of the results obtained, a structure-activity relationship (SAR) is discussed. 相似文献
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Narsimha Sirassu Battula Kumara Swamy Reddy Yellu Narasimha Nagavelli Vasudeva Reddy 《Chemistry of Heterocyclic Compounds》2018,54(12):1161-1167
Chemistry of Heterocyclic Compounds - A copper-catalyzed one-pot synthesis of fused benzothiazino[1,2,3]triazolo[4,5-c]quinolinone derivatives from 1-iodoalkynes with different aryl azides via an... 相似文献
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A series of novel pyrimido[4,5-c]isoquinolines (3a–3h) and 1,2,3-triazole-coupled pyrimido[4,5-c]isoquinolines (4a–4h) were synthesized in good to excellent yields in the one-pot method. The reaction of 6-amino-1,3-dimethyluracil with different 2-iodo benzoyl chlorides using Pd catalyst in dimethylformamide afforded corresponding pyrimido[4,5-c]isoquinolines (3a–3h). One-pot reaction of pyrimido[4,5-c]isoquinolines with propargyl bromide and benzyl azide in THF at room temperature furnished 1,2,3-triazole-coupled pyrimido[4,5-c]isoquinoline (4a–4h). In vitro antioxidant activity examination revealed that compounds 4d and 4c found to exhibit potent antioxidant activity as compared to the standard drug Trolox with IC50 values 6.02?±?0.6 and 12.18?±?0.9?µM, respectively. 相似文献
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