Synthesis of Novel Azetidinone Derivatives as Antitubercular Agents

Himaja, M.; Asif, Karigar; Ramana, M. V.; Munirajasekhar, D.; Sikarwar, Mukesh S.

doi:10.2174/157018012800673038

Cited by 17 publications

(15 citation statements)

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“…μg/mL [103]. This finding was consistent with literature report on the antibacterial activity of indole-3carboxylic acid, from which a novel series of indole-3-carboxylic acid derivatives were previously reported to possess potent antibacterial activity against Enterococcus faecalis [104]. In addition, it has been reported that indole-3-carboxylic acid had weak cytotoxic effects on both normal and tumor cells, and its antioxidant activity is weak [103].…”

Section: Bioactivity Evaluation Of Fungal Endophytessupporting

confidence: 90%

Diversity and bioactivities of fungal endophytes from Distylium chinense, a rare waterlogging tolerant plant endemic to the Three Gorges Reservoir

Duan

Qin

et al. 2019

Preprint

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Background The present study involves diversity and biological activities of the endophytic fungal community from Distylium chinense , a rare waterlogging tolerant plant endemic to the Three Gorges Reservoir. This study has been conducted hypothesizing that the microbial communities in the TGR area would contribute to the host plant tolerating a range of abiotic stress such as summer flooding, infertility, drought, salinity and soil erosion etc., and they may produce new metabolites, which may possess plentiful bioactive property, especially antioxidant activity. Therefore in the current study, the antioxidant, antimicrobial and anticancer activities of 154 endophytes recovered from D. chinense have been investigated. Furthermore, the active metabolites of the most broad-spectrum bioactive strain have also been studied.Results A total of 154 fungal endophytes were isolated from roots and stems. They were categorized into 30 morphotypes based on cultural characteristics and were affiliated with 27 different taxa. Among these, the most abundant fungal orders included Diaporthales (34.4%) and Botryosphaeriales (30.5%), which were predominantly represented by the species Phomopsis sp. (24.7%) and Neofusicoccum parvum (23.4%). Fermentation extracts were evaluated, screening for antioxidant, antimicrobial and anticancer activities. Among the 154 isolates tested, 99 (64.3%) displayed significant antioxidant activity, 153 (99.4%) exhibited inclusive antimicrobial activity against at least one tested microorganism and 27 (17.5%) showed exclusive anticancer activity against one or more cancer cell lines. Specifically, the crude extract of Irpex lacteus DR10-1 exhibited note-worthy bioactivities. Further chemical investigation on DR10-1 strain resulted in the isolation and identification of two known bioactive metabolites, indole-3-carboxylic acid ( 1 ) and indole-3-carboxaldehyde ( 2 ), indicating their potential roles in plant growth promotion and human medicinal value.Conclusion These results indicated that diverse endophytic fungal population inhabits D. chinense . One of the fungal isolate DR10-1 ( Irpex lacteus ) exhibited significant antioxidant, antimicrobial and anticancer potential. Further, its active secondary metabolites 1 and 2 also showed antioxidant, antimicrobial and anticancer potential.

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Section: Bioactivity Evaluation Of Fungal Endophytessupporting

confidence: 90%

Diversity and bioactivities of fungal endophytes from Distylium chinense, a rare waterlogging tolerant plant endemic to the Three Gorges Reservoir

Duan

Qin

et al. 2019

Preprint

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“…Later, Himaja et al. synthesized a series of azetidin‐2‐one derivatives and observed that compound 8 displayed high anti‐TB activity (MIC = 0.8 μg/mL) that was superior compared to standard drugs pyrazinamide (MIC = 3.12 μg/mL) and streptomycin (MIC = 6.25 μg/mL) …”

Section: Azetidin‐2‐onesmentioning

confidence: 99%

New structural classes of antituberculosis agents

Kumar

Patel

Jain

2017

Medicinal Research Reviews

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Tuberculosis (TB), one of the deadliest diseases is shattering the health and socioeconomic status of the society. The emergence of multidrug resistant (MDR) and extremely drug resistant (XDR) strains has provided unprecedented lethal character to TB. The development of MDR and XDR strains of TB results in more deaths, longer duration of therapy, and appearance of the disease in the immunocompromised patients. Because of the development of rapid resistance by Mycobacterium tuberculosis, researchers are confronted with serious challenges in combating TB. For instance, the need for potency and specificity in therapeutic agents approaching clinics, and the increasing demand of low toxicity due to long duration of treatment. Recently, it is proposed that such challenges could be addressed by a shift from contemporary or known classes of drugs to new scaffold-containing or entirely new structural classes of drugs that possibly act on the previously unknown targets, resulting in possibly less instances of resistance development. The exploitation of advances made in the biology of TB in the last and present decades have created opportunities to discover a large number of new structural classes that specifically targets TB by molecular mechanism of action(s) unknown earlier. We have earlier reviewed new structural classes of anti-TB agents up to year 2005. This review covers literature reports of the subsequent 10 years on the discovery of new structural classes of synthetic anti-TB agents. Due to the availability of large number of research reports, we have divided new compounds in 38 structural classes, 368 structures, and 307 references.

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“…Quinazoline-derived fluorescent nucleobases have been developed by fusion of the electron-rich ring into electron-deficientp yrimidine and used as fluorescent probes. [28][29][30][31][32] Moreover,d ioxoloquinazoline derivatives have been investigated because of their biological activities as inhibitors of botulinum neurotoxin serotype Aa nd substrate-competitive inhibitors of G9a (histonel ysine methyltransferase). [23,24,55] Luedtke and coworker synthesized an ucleoside analogue based on the quinazoline structure with an amineg roup at the C6 position, and it was used for various studies such as determining the kinetics of metallo-base pairs.…”

Section: Introductionmentioning

confidence: 99%

New Size‐Expanded Fluorescent Thymine Analogue: Synthesis, Characterization, and Application

Hirashima

Han

Tsuno

et al. 2019

Chemistry A European J

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Here, the synthesis, photophysical characterization, and application of an ew size-expanded thymine nucleoside, diox T,i sd escribed. diox T has desirable qualities as aT surrogate, including excellent quantum yield (0.36) and high environmental sensitivity.W hen incorporatedi nto singleand double-stranded DNA, diox T showede xcellent photophysical characteristics including ahighquantum yield (average 0.20), and unlike BgQ, demonstrated dependenceo n neighboring bases withouts ignificantd estabilizationof the duplex. Interestingly,t he matched base pair of adenine (A) and diox T has the unique property that it exhibits higher fluorescence than mismatched base pairs, and diox T has selfquenching effects. As one example of the possible applications of thesep romising features, single nucleoside polymorphism typing is demonstrated for discrimination of Ab y using diox T.T he results suggestt hat diox T can be used for a broad range of applications in chemical biology.[a] S.Calculations were carried out with the B3LYP density functional method and 6-31G* basis set. The HOMO energy of each nucleobase was calculated by DFT (B3LYP/6-31G*) at the optimized geometry by using the Spartan "16 program. A = 9-methyladenine, T = 1-methylthymine, G = 9-methylguanine, C = 1-methylcytosine.

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Synthesis of Novel Azetidinone Derivatives as Antitubercular Agents

Cited by 17 publications

References 0 publications

Diversity and bioactivities of fungal endophytes from Distylium chinense, a rare waterlogging tolerant plant endemic to the Three Gorges Reservoir

Diversity and bioactivities of fungal endophytes from Distylium chinense, a rare waterlogging tolerant plant endemic to the Three Gorges Reservoir

New structural classes of antituberculosis agents

New Size‐Expanded Fluorescent Thymine Analogue: Synthesis, Characterization, and Application

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