Triazole derivatives and their anti-tubercular activity

Self Cite

A new class of isatin-1,2,3-triazole-moxifloxacin (MXFX) hybrids 5a-j was designed, synthesized, and screened for their in vitro antimycobacterial activities against Mycobacterium tuberculosis H 37 Rv and MDR-TB. All the synthesized hybrids (MIC: 0.10-0.78 μg/mL) exhibited excellent activities against MTB H 37 Rv and MDR-TB, in spite of none of them were more potent than the parent MXFX (MIC: 0.10 and 0.12 μg/mL). Against MTB H 37 Rv, the most active 5f (MIC: 0.10 μg/mL) was comparable with MXFX and 4 times more potent than RIF (MIC: 0.39 μg/mL). Against MDR-TB, all hybrids were more active than RIF (MIC: 32 μg/mL) and INH (MIC: >128 μg/mL). In particular, hybrid 5e (MIC: 0.10 μg/ mL) was comparable with MXFX and 256 and >1,024 times more potent than RIF and INH. Both conjugates 5e and 5f warrant further investigations.

Section: Tuberculosismentioning

confidence: 99%

Design, Synthesis and in vitro Antimycobacterial Activities of Isatin‐1,2,3‐triazole‐moxifloxacin Hybrids

Qiang

et al. 2017

Self Cite

“…In general, targets 5-9 showed low cytotoxicity at concentration of 20 μM while compounds 10-14 were less potent with IC 50 values more than 30 μM. Amongst them, the most active compound 7 with IC 50 ranging from 6.76 to 8.67 μM against the tested three cell lines, which was 1.46-2.47 and 3.48-4.93 times more potent than 5-FU and Hoechst 33258, respectively, warrant further investigations.…”

Section: Resultsmentioning

confidence: 99%

“…13 A mixture of compound 4 (0.5 g, 1.8 mmol), substituted benzaldehyde (1.8 mmol), and sodium hydrogensulfite (0.37 g, 3.6 mmol) in methanol (40 mL) were heated to reflux for 8 h. After removal of the solvent under reduced pressure, the residue was purified by gel column chromatography (CHCl 3 : CH 3 OH = 30:1) to give the targets 5-14. 114.5, 121.2, 122.1, 124.3, 128.3, 128.9, 133.6, 134.0 Table 1 The antitumor activities of the targets (5)(6)(7)(8)(9)(10)(11)(12)(13)(14) The experiments were performed twice, and the average values were obtained from two independent experiments. 13 The antitumor properties of all these compounds were tested by the standard MTT assay technique.…”

Section: Spectral Studiesmentioning

confidence: 99%

“…Benzimidazole derivatives, which exhibited diverse biological properties such as anti-tubercular [6][7][8], antimalarial [9], anti-microbial [10], and anticancer [11][12][13] activities, have received considerable attention. However, most investigators focused on single benzimidazole derivatives, and only a few literatures related bisbenzothiazole derivatives as anticancer agents have reported so far to the best of our knowledge.…”

Section: Introductionmentioning

confidence: 99%

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Design, Synthesis, and Evaluation of Bis‐Benzothiazole Derivatives as DNA Minor Groove Binding Agents

Yang

Zhang

Wang

et al. 2017

A series of novel bis-benzothiazole derivatives with head-to-head orientation were designed, synthesized, and evaluated for their anti-proliferative activities on U937, HL60, and HeLa cells. A significant part of the targets exhibited considerable in vitro anticancer activity, and some of them were more potent than the reference 5-FU. Molecular modeling, fluorescence, and viscosimetry studies revealed that these compounds could bind into the minor groove of DNA. Amongst them, the most active compound 7 with IC 50 in a range of 6.76 to 8.67 μM against the tested three cell lines, which was 1.46-2.47 and 3.48-4.93 times more potent than 5-FU and Hoechst 33258, respectively, warrant further investigations.

“…The first-line anti-TB drugs isoniazid, rifampicin (RIF), pyrazinamide, and ethambutol have been used in clinical for more than 50 years, in spite of they are effective for the treatment of the disease or latent infection, drugresistant TB (DR-TB) including multidrug-resistant TB (MDR-TB), extremely drug-resistant TB, and totally drug resistant TB have emerged and spread globally [8][9][10].…”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis, and in vitro Antimycobacterial Activity of Propylene‐tethered Isatin Dimmers

Song

Fan

2017

A set of propylene-tethered isatin dimmers 2a-i was synthesized via click chemistry and screened for their in vitro antimycobacterial activities against Mycobacterium tuberculosis (MTB) H 37 Rv and multidrugresistant TB. In spite of all dimmers (minimum inhibitory concentration: 25-> 128 μg/mL) only exhibited weak to moderate activities against the tested MTB H 37 Rv and multidrug-resistant TB, the structure-activity relationship was enriched and the results warrant further development of the anti-TB properties of this kind of dimmers.