<span style="font-size:10.0pt;font-family: "Times New Roman";mso-fareast-font-family:"Times New Roman";mso-bidi-font-family: Mangal;mso-ansi-language:EN-US;mso-fareast-language:EN-US;mso-bidi-language: HI;mso-bidi-font-weight:bold" lang="EN-US">Design and synthesis of new <i><span style="font-size:10.0pt;font-family:"Times New Roman";mso-fareast-font-family: "Times New Roman";mso-bidi-font-family:Mangal;mso-ansi-language:EN-US; mso-fareast-language:EN-US;mso-bidi-language:HI" lang="EN-US">N</span></i><span style="font-size:10.0pt;font-family:"Times New Roman";mso-fareast-font-family: "Times New Roman";mso-bidi-font-family:Mangal;mso-ansi-language:EN-US; mso-fareast-language:EN-US;mso-bidi-language:HI" lang="EN-US">'-substituted- 2-methylquinoline-3-carbohydrazides with antioxidant and antimicrobial activity</span></span>

930-935Ten new N'-substituted-2-methylquinoline-3-carbohydrazide scaffolds have been synthesized, characterized by their physical and spectral data (IR, 1H NMR, and MS) and screened for in vitro antimicrobial and antioxidant activities. Results clearly reveal that all the synthesized compounds possess in vitro <span style="mso-bidi-font-weight: bold">antioxidant activity at the tested dose as compared to the standard drug, ascorbic acid. From the results, it can be assumed that the presence of an electron donating group on the aromatic ring is an important requirement for the antioxidant activity of the synthesized compounds, <b style="mso-bidi-font-weight: normal">5a-j. The synthesized compounds have also been screened for antibacterial and antifungal activity against three different strains of Gram-positive (<i style="mso-bidi-font-style: normal">Bacillus subtilis, S. pyogens<span style="mso-bidi-font-style: italic">, and Staphylococcus aureus) and three strains of Gram-negative bacteria (<i style="mso-bidi-font-style: normal">Escherichia coli, Enterobactor aerogens and<span style="mso-bidi-font-style: italic"> Klebsiella pneumoniae) and two fungal strains (Candida albicans and <i style="mso-bidi-font-style: normal">Fusarium oxysporium). Some of the compounds are found to be active against all the tested organisms, but are equipotent and less active as compared to the standard drug streptomycin. Compounds 5b and 5j exhibit almost equipotent activity compared with the standard drug Itraconazol against fungal strain <i style="mso-bidi-font-style: normal">Fusarium oxysporium and another compound 5f which is <span style="mso-bidi-font-weight: bold">active against Candida albicans. </span

Fe3O4 nanoparticles mediated synthesis of novel spirooxindole‐dihydropyrimidinone molecules as Hsp90 inhibitors

Heat shock protein 90 (Hsp90) is a validated molecular chaperone considered as the new key recipient for cancer intervention. The current study illustrates the synthesis of novel spirooxindole-dihydropyrimidinones (4a-j) by Fe 3 O 4 nanoparticles intervened synthesis and their Hsp90 ATPase inhibitory activity was investigated by the malachite green assay. All the compounds in the study demonstrated a moderate to potent ATPase inhibitory profile, with IC 50 values ranging from 0.18 to 6.80 μM. Compounds 4j, 4h, 4f, and 4i exhibited maximum inhibitory potential with IC 50 values of 0.18, 0.20, 0.35, and 0.55 μM, respectively. They were found to be better than the standard drug, geldanamycin (Hsp9 ATPase inhibition IC 50 = 0.90 μM). Compounds 4h and 4j with IC 50 values of 22.82 ± 0.532, 20.78 ± 0.234 and 21.32 ± 0.765, 28.43 ± 0.653 µM showed significantly greater potencies against the MCF-7 and HepG2 cell lines, respectively. Compound 4j showed good antioxidant activities in the DPPH test and H 2 O 2 assay (IC 50 = 20.13.23 ± 0.32 and 23.27 ± 0.32 μg/mL) when compared with the standard ascorbic acid (IC 50 = 19.16 ± 0.20 and 20.66 ± 1.09 μg/mL). A molecular docking study was performed to observe the binding efficiency and steric interactions of the lead moiety.Fil: Maddela, Srinubabu. Jawaharlal Nehru Technological University Hyderabad; IndiaFil: Makula, Ajitha. Jawaharlal Nehru Technological University Hyderabad; IndiaFil: Galigniana, Mario Daniel. Consejo Nacional de Investigaciones Científicas y Técnicas. Instituto de Biología y Medicina Experimental. Fundación de Instituto de Biología y Medicina Experimental. Instituto de Biología y Medicina Experimental; ArgentinaFil: Parambi, Della G. T.. Jouf University; Arabia SauditaFil: Federicci, Fernando. Consejo Nacional de Investigaciones Científicas y Técnicas. Instituto de Biología y Medicina Experimental. Fundación de Instituto de Biología y Medicina Experimental. Instituto de Biología y Medicina Experimental; ArgentinaFil: Mazaira, Gisela Ileana. Consejo Nacional de Investigaciones Científicas y Técnicas. Instituto de Biología y Medicina Experimental. Fundación de Instituto de Biología y Medicina Experimental. Instituto de Biología y Medicina Experimental; ArgentinaFil: Hendawy, Omnia M.. Beni Seuf University; Egipto. Jouf University; Arabia SauditaFil: Dev, Sanal. Al Shifa College of Pharmacy; IndiaFil: Mathew, Githa E.. Grace College Of Pharmacy ; IndiaFil: Mathew, Bijo. Ahalia School of Pharmacy ; Indi