Corrigendum to “Design, synthesis and evaluation of hybrid of tetrahydrocarbazole with 2,4-diaminopyrimidine scaffold as antibacterial agents” [Eur. J. Med. Chem. 162 (162) (2019) 203–211]

Su, Liqiang; Li, Jiahui; Zhou, Zhen; Huang, Dan; Zhang, Yuanjin; Pei, Haixiang; Guo, Weikai; Wu, Haigang; Wang, Xin; Liu, Mingyao; Yang, Cai‐Guang; Chen, Yihua

doi:10.1016/j.ejmech.2019.02.059

Cited by 6 publications

(4 citation statements)

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“…The antibacterial SAR of indole–pyrimidine hybrids 82 (MIC: 0.39‐6.25 μg/ml) against S. aureus Newman and E. coli AB1157 indicated that the electron‐withdrawing group was favorable to the activity, whereas the electron‐donating group was detrimental to the activity. [ 161 ] Hybrid 82a (MIC: 0.39–0.78 μg/ml) was found to be most active against the two tested strains, and the activity was ≥2‐fold higher than that of vancomycin (MIC: 0.78 to >50 μg/ml) and kanamycin (MIC: 3.12–12.5 μg/ml). Moreover, this hybrid (MIC: 0.39–1.56 μg/ml) was also highly active against five multidrug‐resistant strains of S. aureus (NRS‐1, NRS‐70, NRS‐100, NRS‐108, and NRS‐271).…”

Section: Indole–pyridine/pyrimidine Hybridsmentioning

confidence: 99%

Indole/isatin‐containing hybrids as potential antibacterial agents

Song

Bian

et al. 2020

Archiv der Pharmazie

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The emergence and worldwide spread of drug-resistant bacteria have already posed a serious threat to human life, creating the urgent need to develop potent and novel antibacterial drug candidates with high efficacy. Indole and isatin (indole-2,3-dione) present a wide structural and mechanistic diversity, so their derivatives possess various pharmacological properties and occupy a salient place in the development of new drugs. Indole/isatin-containing hybrids, which demonstrate a promising activity against a panel of clinically important Gram-positive and Gram-negative bacteria, are privileged scaffolds for the discovery of novel antibacterial candidates. This review, covering articles published between January 2015 and May 2020, focuses on the development and structure-activity relationship (SAR) of indole/isatincontaining hybrids with potential application for fighting bacterial infections, to facilitate further rational design of novel drug candidates.

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Section: Indole–pyridine/pyrimidine Hybridsmentioning

confidence: 99%

Indole/isatin‐containing hybrids as potential antibacterial agents

Song

Bian

et al. 2020

Archiv der Pharmazie

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“…Furthermore, the pyrimidine structure is closely related to the nucleobases—uracil, thymine, and cytosine—which makes pyrimidine molecules important building blocks in all living cells [ 28 , 29 ]. Pyrimidine-based compounds exhibit a broad spectrum of pharmacological activity, such as antimalarial [ 30 ], antidiabetic [ 31 ], antimicrobial [ 32 , 33 ], and anticancer activities [ 34 , 35 , 36 ]. Therefore, combining thienopyridine and pyrimidine cores in the same molecular architecture, forming a pyridothienopyrimidine nucleus, serves as an attractive strategy for designing a novel scaffold with more favorable pharmacological effects [ 37 ].…”

Section: Introductionmentioning

confidence: 99%

Novel Pyridothienopyrimidine Derivatives: Design, Synthesis and Biological Evaluation as Antimicrobial and Anticancer Agents

et al. 2022

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The growing risk of antimicrobial resistance besides the continuous increase in the number of cancer patients represents a great threat to global health, which requires intensified efforts to discover new bioactive compounds to use as antimicrobial and anticancer agents. Thus, a new set of pyridothienopyrimidine derivatives 2a,b–9a,b was synthesized via cyclization reactions of 3-amino-thieno[2,3-b]pyridine-2-carboxamides 1a,b with different reagents. All new compounds were evaluated against five bacterial and five fungal strains. Many of the target compounds showed significant antimicrobial activity. In addition, the new derivatives were further subjected to cytotoxicity evaluation against HepG-2 and MCF-7 cancer cell lines. The most potent cytotoxic candidates (3a, 4a, 5a, 6b, 8b and 9b) were examined as EGFR kinase inhibitors. Molecular docking study was also performed to explore the binding modes of these derivatives at the active site of EGFR-PK. Compounds 3a, 5a and 9b displayed broad spectrum antimicrobial activity with MIC ranges of 4–16 µg/mL and potent cytotoxic activity with IC50 ranges of 1.17–2.79 µM. In addition, they provided suppressing activity against EGFR with IC50 ranges of 7.27–17.29 nM, higher than that of erlotinib, IC50 = 27.01 nM.

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“…[1,2] Moreover, the efficacy of existing antibacterial therapeutics has been severely affected due to their indiscriminate use, engaging the whole scientific world once again in a never-ending search for novel antibacterial agents. [3] It is estimated by World Health Organization (WHO) that these drug-resistant strains are responsible for the death of approximately 700,000 people worldwide annually, and if the current trend continues, it would threaten ∼ 10 million human lives by 2050. [4] Therefore, the development of new and effective antibacterial agents capable of defying the resistance mecha-nism of these microbes is highly desirable and remains an unmet need.…”

Section: Introductionmentioning

confidence: 99%

“…The increasing incidences of invasive microbial infections coupled with the emergence of resistant bacterial strains have become a leading cause of morbidity and mortality worldwide . Moreover, the efficacy of existing antibacterial therapeutics has been severely affected due to their indiscriminate use, engaging the whole scientific world once again in a never‐ending search for novel antibacterial agents . It is estimated by World Health Organization (WHO) that these drug‐resistant strains are responsible for the death of approximately 700,000 people worldwide annually, and if the current trend continues, it would threaten ∼10 million human lives by 2050 .…”

Section: Introductionmentioning

confidence: 99%

Ferulic Hydroxamic Acid Triazole Hybrids as Peptide Deformylase Inhibitors: Synthesis, Molecular Modelling and Biological Evaluation

et al. 2020

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Design and development of peptide deformylase (PDF) inhibitors has gained attention as it is a highly conserved and specific enzyme for bacterial protein synthesis. This makes it a specific and attractive drug target. Therefore, based on the targeted drug-discovery approach, a series of ferulic acid-based nonpeptidic hydroxamic acid-triazole hybrids was synthesized. All the semi-synthetic compounds (8 a-p) were evaluated against a panel of Gram-positive and Gram-negative bacterial strains. Most of the compounds showed antibacterial activities against S. pneumoniae while few were active against E. coli. Among all, the compound 8 j showed strong potency against S. pneumoniae with IC 50 value 34.57 μg/mL whereas for E. coli the observed IC 50 was 66.20 μg/mL. Growth kinetics study showed the bacteriostatic nature of compound 8 j against S. pneumoniae. Interestingly, in the studied concentration range, no significant hemolysis or cytotoxicity was observed towards human cells, suggesting the non-toxic nature of compound 8 j. Molecular docking studies showed that compound 8 j occupies the same active site where actinonin (a known inhibitor of PDF) binds and it also mimics the mode of interactions by offering significant interactions with the corresponding amino acid residues of PDF. The outcome of this study suggested the potential implications of the present scaffold for the development of antibacterial molecules targeting PDF.

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Corrigendum to “Design, synthesis and evaluation of hybrid of tetrahydrocarbazole with 2,4-diaminopyrimidine scaffold as antibacterial agents” [Eur. J. Med. Chem. 162 (162) (2019) 203–211]

Cited by 6 publications

References 0 publications

Indole/isatin‐containing hybrids as potential antibacterial agents

Indole/isatin‐containing hybrids as potential antibacterial agents

Novel Pyridothienopyrimidine Derivatives: Design, Synthesis and Biological Evaluation as Antimicrobial and Anticancer Agents

Ferulic Hydroxamic Acid Triazole Hybrids as Peptide Deformylase Inhibitors: Synthesis, Molecular Modelling and Biological Evaluation

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