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Parasitic infections like amebiasis, trichomoniasis, and giardiasis are major health threats in tropical and subtropical regions of the world. Metronidazole (MTZ) is the current drug of choice for amebiasis, giardiasis, and trichomoniasis but it has several adverse effects and potential resistance is a concern. In order to develop alternative antimicrobials, a library of 1H-1,2,3-triazole-tethered metronidazole-isatin conjugates was synthesized using Huisgens azide-alkyne cycloaddition reaction and evaluated for their amebicidal, anti-trichomonal, and anti-giardial potential. Most of the synthesized conjugates exhibited activities against Trichomonas vaginalis, Tritrichomonas foetus, Entamoeba histolytica, and Giardia lamblia. While activities against T. vaginalis and T. foetus were comparable to that of the standard drug MTZ, better activities were observed against E. histolytica and G. lamblia. Conjugates 9d and 10a were found to be 2-3-folds more potent than MTZ against E. histolytica and 8-16-folds more potent than MTZ against G. lamblia. Further analysis of these compounds on fungi and bacteria did not show inhibitory activity, demonstrating their specific anti-protozoal properties.

A series of N-alkyl tethered C-5 functionalized bis-isatins were synthesized and evaluated for antimicrobial activity against pathogenic microorganisms. The preliminary evaluation studies revealed the compound 4t, with an optimal combination of bromo-substituent at the C-5 position of isatin ring along with propyl chain linker being most active among the synthesized series exhibiting an IC50 value of 3.72 μM against Trichomonas vaginalis while 4j exhibited an IC50 value of 14.8 μM against Naegleria fowleri, more effective than the standard drug Miltefosine. The compound 3f with an octyl spacer length was the most potent among the series against Giardia lamblia with an IC50 of 18.4 μM while 3d exhibited an IC50 of 23 μM against Entamoeba histolytica. This library was also screened against the fungal pathogen Aspergillus parasiticus. A number of the compounds demonstrated potency against this fungus, illustrating a possible broad-spectrum activity. Furthermore, an evaluation of these synthesized compounds against a panel of normal flora bacteria revealed them to be non-cytotoxic, demonstrating the selectivity of these compounds. This observation, in combination with previous studies that isatin is non-toxic to humans, presents a new possible scaffold for drug discovery against these important protozoal pathogens of humans and animals.

Quinazolinone derivatives have garnered attention for their diverse biological activities, including anticancer properties. This review combines findings from 2018 to 2024, focusing on the impact of quinazolinones on cancer cells, tubulin formation, and EGFR/PI3 K pathways. By unraveling the intricacies of structure‐activity relationships, this review endeavors to provide guidance for researchers in identifying promising avenues for the development of cancer treatments. Although in vitro studies underscore significant potential, it is imperative that future research prioritizes pre‐clinical investigations to seamlessly traverse the transitional phase towards clinical applications, thereby propelling the advancement of quinazolinone‐based cancer therapy. [ABSTRACT FROM AUTHOR]

Plastics are versatile materials, offering lightweight, durable, and affordable solutions across various industries. However, their non‐degradable nature poses challenges by end of their life. This study presented an innovative carbonyl extraction method to utilize waste poly(bisphenol A carbonate) (PC) as reaction precursor to synthesis of activated furan as precursor for photoswitchable Stenhouse adducts. This innovative chemical strategy not only generated N,N'‐functionalized barbiturates but also provided an eco‐friendly and cost‐effective alternative to traditional synthesis methods. The method presented hereby not only promotes sustainability by repurposing waste polycarbonate as carbonyl equivalent under green conditions but also yielded reusable bisphenol A (BPA). Furthermore, the derived activated furans exhibited their functionality by forming colored donor‐acceptor Stenhouse adducts (DASAs) on aminated polymer surfaces. This work demonstrated a transition from a linear plastics economy toward a circular one, highlighting the potential of plastic waste as a resource for creating materials with improved properties. [ABSTRACT FROM AUTHOR]

A series of β-amino alcohol tethered 4-aminoquinoline-isatin conjugates were synthesized with the aim of probing their antimalarial structure activity relationship. Two of the most active conjugates (11b and 11f) exhibited antimalarial efficacy comparable to that of chloroquine, with IC50 values of 11.8 and 13.5 nM, respectively against chloroquine resistant W2 strain of Plasmodium falciparum and are devoid of any cytotoxicity.

Nebraska is the number one producer of food‐grade white corn in the United States. Pollen‐mediated gene flow (PMGF) from genetically engineered high alpha‐amylase corn, known as Enogen corn, to food‐grade white corn can have undesirable outcomes. Alpha‐amylase can convert starch in white corn to sugar during or after its processing, degrading the quality of processed products. Thus, proximity to Enogen corn puts white corn production at risk. The objectives of this study were to evaluate the PMGF from herbicide‐resistant yellow corn to food‐grade white corn and assess the significance of wind speed and direction. Field experiments were set up using a Nelder‐wheel design in 2021 and 2022 in Nebraska, with yellow field corn as pollen donor in the center and white corn surrounding it as pollen receptor. At the end of the season, samples of white corn cobs were collected up to 50 and 70 m from four cardinal and ordinal directions, respectively. PMGF was detected by counting the number of yellow kernels on the white cobs. More than 4 million kernels were screened and the highest frequency of PMGF (0.0621–0.1950) was detected at the nearest distance (1 m). PMGF decreased exponentially with distance; however, it was still observed (0.0020–0.0032) at the greatest distance (70 m) evaluated in this study. Wind profile played a significant role in PMGF. Wind frequency (r = 0.58 ≤ 0.86) and wind run (r = 0.36 ≤ 0.95) were moderately to strongly correlated with PMGF in 2021 and 2022, respectively. The results are concerning for white corn growers due to the coexistence of Enogen corn and food‐grade white corn. Core Ideas: The pollen‐mediated gene flow (PMGF) from yellow corn to white corn was greatest at the nearest distance (1 m).The exponential decay model was the best fit to explain PMGF with distance from the yellow corn.Wind parameters such as wind speed, direction, and frequency affected PMGF, signifying the role of wind in PMGF in corn. [ABSTRACT FROM AUTHOR]

The manuscript presents an efficient method for the synthesis of various cis-azetidin-2-ones with high regio- and diastereoselectivity. This approach utilizes Kinugasa reaction involving diverse functionalized nitrones, including diaryl nitrones and α,β-unsaturated nitrones, in conjunction with acetylenic alcohols. Copper (I) serves as a catalyst to facilitate the transformation. [ABSTRACT FROM AUTHOR]