Fused-Ring Oxazolopyrrolopyridopyrimidine Systems with Gram-Negative Activity

Chen, Yiyuan; Moloney, Jonathan G.; Christensen, Kirsten E.; Moloney, Mark G.

doi:10.3390/antibiotics6010002

Cited by 5 publications

(3 citation statements)

References 35 publications

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“…As 3-acyltetramic acids were frequently shown to have antimicrobial effects [ 8 , 9 , 12 , 18 , 19 , 20 ], the new macrocidin derivatives were tested for activity against three different bacteria, namely the Gram-positive strain Staphylococcus aureus (SH1000) and the Gram-negative strains Acinetobacter baumannii , Escherichia coli with the wild-type strain K12 and the ΔTolC mutant (JW5503), which lacks the AcrAB−TolC efflux system. None of the macrocidin analogues displayed activity against the wild-type strain of E. coli .…”

Section: Resultsmentioning

confidence: 99%

Dual Agents: Fungal Macrocidins and Synthetic Analogues with Herbicidal and Antibiofilm Activities

et al. 2021

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Eight analogues of the bioherbicides macrocidin A (1) and Z (2) with structural variance in the size of the macrocycle, its para- or meta-cyclophane character, and its functional groups were synthesized on two modular routes and tested for herbicidal, antibiotic, and antibiofilm activities. Apart from the lead compounds 1 and 2, the structurally simplified dihydromacrocidin Z (3) and normacrocidin Z (4) showed high herbicidal activity in either thistles, dandelions or in both. The derivatives 2, 3, and dibromide 9 also inhibited the growth of Staphylococcus aureus biofilms by ca 70% when applied at subtoxic concentrations as low as ca 20 µM, which are unlikely to induce bacterial resistance. They also led to the dispersion of preformed biofilms of S. aureus, exceeding a similar effect by microporenic acid A, a known biofilm inhibitor. Compounds 3 and 9 showed no noticeable cytotoxicity against human cancer and endothelial cells at concentrations below 50 µM, making them conceivable candidates for application as anti-biofilm agents in a medicinal context.

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Section: Resultsmentioning

confidence: 99%

Dual Agents: Fungal Macrocidins and Synthetic Analogues with Herbicidal and Antibiofilm Activities

et al. 2021

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“…This process proved to be highly reliable, and opened the door to the preparation of a large number of analogues that were suitable for biological evaluation. 110,[112][113][114][115][116] We were able to use these systems to access unusual polycyclic 67 117 and spirocyclic 68 118 systems, including the core system of isatisine 69 (Figure 4), 119 and to apply the same concept to the elaboration of barbiturates, which had better aqueous solubility characteristics arising from their higher polarity. 120 Another route exploiting these templates was to acetylate the tetramate 59a to generate derivative 70a and then to condense it with an aldehyde to give unsaturated ketone 71, either by direct enolate formation or via the intermediate enamine (Scheme 9).…”

Section: Short Review Syn Thesismentioning

confidence: 99%

Functionalised Nitrogen Heterocycles and the Search for New Antibacterials and Bioactives

Khan

Wang²,

Moloney³

2020

Synthesis

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The importance of, and synthetic routes to, pyrrolidines and piperidines, along with their relevance to natural product synthesis and antibacterial drug discovery, are surveyed in the context of an extended programme of investigation from our own laboratories.1 Introduction2 Pyroglutamates2.1 Synthesised by Modification of an Existing Ring2.2 Synthesised by Construction of a New Ring3 Tetramates4 Metal Chelation5 Biological Activity6 Conclusion

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“…Typically, biogas contains methane (CH4), carbon dioxide (CO2), and hydrogen sulfide (H2S) (Arutyunov et al, 2020). CH4 can be used as an energy source for electricity generation, vehicle fuel, or as a raw material in the industry ( Wahyuono et al, 2015;Chen et al, 2017). However, the other gases contained in biogas are considered impurities.…”

Section: Introductionmentioning

confidence: 99%

A Novel Simple Dipping-Nebulizing Water Absorption for Biogas Purification

Soehartanto¹,

Wahyuono²,

Aisyah³

et al. 2021

IJTech

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Biogas impurities CO2 and H2S decrease the quality of biogas, which leads to a reduced caloric value and corrosive behavior, respectively. A vertical/columnar wet scrubber has been widely employed for biogas purification in which the absorption of impurities strongly depends on the contact time and surface area between the biogas and water. The drawback of this method lies in the stability of CH4 production due to the influence of the bioreactor conditions and the fluctuating condition of the surrounding environment. In this work, we present a novel design of simple water absorption columns embedded with an ultrasonic nebulizer for biogas purification. In this designed system, CO2 and H2S become dissolved in the water, as the CH4 characterized by water low solubility is released on the surface of the water by using an ultrasonic diffuser/nebulizer. We optimized the water absorption performance by varying the water pH in the range 6.0-7.3. The results indicate that water pH affects biogas purification in the designed system. The optimum pH condition was 6.78, which yielded CH4 enrichment of 11%, O2 increase of 29%, CO2 reduction of 32%, and H2S reduction of 99.8%. To evaluate the biogas purification process in the upscaled system, a model and SIMULINK-based simulation were developed to predict the biogas purification process.

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Fused-Ring Oxazolopyrrolopyridopyrimidine Systems with Gram-Negative Activity

Cited by 5 publications

References 35 publications

Dual Agents: Fungal Macrocidins and Synthetic Analogues with Herbicidal and Antibiofilm Activities

Dual Agents: Fungal Macrocidins and Synthetic Analogues with Herbicidal and Antibiofilm Activities

Functionalised Nitrogen Heterocycles and the Search for New Antibacterials and Bioactives

A Novel Simple Dipping-Nebulizing Water Absorption for Biogas Purification

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