S-Alkylated/aralkylated 2-(1H-indol-3-yl-methyl)-1,3,4- oxadiazole-5-thiol derivatives. 2. Anti-bacterial, enzymeinhibitory and hemolytic activities

Abstract

Purpose: To evaluate the antibacterial, enzyme-inhibitory and hemolytic activities of Salkylated/aralkylated 2-(1H -indol-3-ylmethyl)-1,3,4-oxadiazole-5-thiol (IC50 38.25 ± 0.12 µg/mL). Another compound had 1.5 % hemolytic activity. -indol-3-ylmethyl)-1,3,4-oxadiazole-5-thiol Conclusion: S-Alkylated/aralkylated 2-(1H

Novel indole based hybrid oxadiazole scaffolds with N-(substituted-phenyl)butanamides: synthesis, lineweaver–burk plot evaluation and binding analysis of potent urease inhibitors

“…The methine carbon resonances appearing at δ 122.97 (C-2), 121.35 (C-6), 118.66 (C-5 & 7), 111.83 (C-4) were also coherent with the indole moiety. 13 The C and N -substituted butanamido group was confirmed by two discrete resonances, one for a carbonyl group at δ 170.51 (C-1′′′) and other for three methylene groups at δ 34.62 (C-2′′′), 32.15 (C-4′′′) and 25.68 (C-2′′′). The 2,4-dimethylphenyl group attached to a nitrogen atom was thoroughly substantiated by three quaternary signals at δ 134.63 (C-1′′′′), 134.18 (C-2′′′′) and 132.22 (C-4′′′′), three methine signals at δ 131.17 (C-5′′′′), 126.80 (C-3′′′′) and 125.71 (C-6′′′′), and two methyl signals at δ 20.91 (CH 3 -4′′′′) and 18.20 (CH 3 -2′′′′).…”

“…The signals in its 13 C-NMR spectrum were rational for all the twenty ve carbons, where the most downeld quaternary carbons signals at d 168.32 (C-5 00 ) and 163.36 (C-2 00 ) belonged to the cyclized 1,3,4-oxadiazole ring, thus conrming the formation of , 111.83 (C-4) were also coherent with the indole moiety. 13 The C and N-substituted butanamido group was conrmed by…”

“…10,11 The bioactivity of indole and oxadiazole moieties prompted us to synthesize some new butanamide molecules bearing these moieties altogether. Hence, in continuation of our previous efforts on bioactivity study of indole containing compounds 12,13 and urease inhibitory activity of bi-heterocyclic bi-amide molecules, 14 the present investigation was designed to explore the urease inhibitory potential and the kinetic mechanism of newly synthesized bi-heterocyclic butanamides. The binding interactions with the targeted enzyme were ascertained by molecular docking, and the cytotoxicity of these scaffolds was evaluated by hemolysis to identify their therapeutic utility as promising drug candidates in drug discovery programs.…”

“…13 C-NMR spectrum of 8g molecule.25926 | RSC Adv., 2018, 8, 25920-25931 This journal is © The Royal Society of Chemistry 2018 RSC Advances Paper Open Access Article. Published on 19 July 2018.…”

Synthesis, characterization, anti-mycobacterial activity and in silico study of new 2,5-disubstituted-1,3,4-oxadiazole derivatives

“…1,3,4-oxadiazole is better known and widely studied owing to its many significant chemical and biological properties. Substituted 1,3,4-oxadiazole derivatives display various biological activities including antibacterial (Koul et al, 2011;Song et al, 2018), antimicrobial (Khalilullah et al, 2016;Rubab et al, 2016;Chortani et al, 2020;Hannoun et al, 2020), anti-mycobacterial (Navarrete-Vazquez et al, 2007;Karabanovich et al, 2016;Ambhore et al, 2019), antifungal (Wani et al, 2015;Shi et al, 2020), anti-inflammatory (Abd-Ellah et al, 2017;Zheng et al, 2020), and anti-viral activities (Li et al, 2011b). Among the substituted 1,3,4-oxadiazole derivatives; 5-substituted-1,3,4-oxadiazole-2thioether continuously draws interest for the development of new drug moieties and have increasing importance as compounds with biological activities including anti-TB agents.…”