Gao, Feng; Wang, Tengfei; Gao, Meixiang; Zhang, Xia; Liu, Zhuqing; Zhao, Shi Jia; Lv, Zao Sheng; Xiao, Jiaqi published the artcile< Benzofuran-isatin-imine hybrids tethered via different length alkyl linkers: Design, synthesis and in vitro evaluation of anti-tubercular and anti-bacterial activities as well as cytotoxicity>, Product Details of C11H12O3, the main research area is benzofuran isatin imine preparation antitubercular antibacterial cytotoxicity; Anti-bacterial; Anti-tubercular; Benzofuran; Hybrid compounds; Imine; Isatin; Multi-drug resistant; Structure-activity relationship.
The design and synthesis of twenty-two novel benzofuran-isatin-imine hybrids I [R1 = H, F, OCH3; X = (CH2)n; Y = NOCH3, NOC2H5, NNHC(S)NH2, NOH; R3 = H, OCH3, F; n = 1, 2, 3, 4] tethered through propylene, butylene, pentylene and hexylene, and for the evaluation of their in vitro anti-tubercular and anti-bacterial activities as well as cytotoxicity were reported. All benzofuran-isatin-imine hybrids exhibited considerable in vitro anti-TB (MIC: <0.016-0.218 μg/mL and 0.062-14.15 μg/mL against drug-sensitive and MDR MTB, resp.) and anti-bacterial (MIC: 0.25-64 μg/mL and 0.06-16 μg/mL against Gram-pos. and Gram-neg. strains, resp.) activities. All of them also showed acceptable cytotoxicity towards VERO (CC50: 8-128 μg/mL). The most active hybrid I (R1 = H; X = CH2CH2; Y = NOCH3; R3 = OCH3) (MIC: <0.016, 0.062 and 0.16 μg/mL, resp.) was >4.8 and >48 folds more potent than the first line anti-TB agents RIF and INH against both drug-sensitive MTB H37Rv and MDR-TB isolates, resp. Moreover, hybrid I (R1 = H; X = CH2CH2; Y = NOCH3; R3 = OCH3) also demonstrated promising anti-bacterial activities with MIC values of ≤1 μg/mL against the majority of the tested Gram-neg. and Gram-pos. pathogens, which was comparable to vancomycin (MIC: 0.5-4 μg/mL) and CPFX (MIC: 0.125-8 μg/mL) against Gram-pos. bacteria, but slightly less potent than CPFX (MIC: ≤0.03-0.5 μg/mL) against Gram-neg. bacteria. The results indicated that benzofuran-isatin-imine hybrids could act as candidates for the development of anti-TB and anti-bacterial agents.
European Journal of Medicinal Chemistry published new progress about Aliphatic amines Role: RCT (Reactant), RACT (Reactant or Reagent). 94-02-0 belongs to class esters-buliding-blocks, and the molecular formula is C11H12O3, Product Details of C11H12O3.
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