Design, Modeling and Synthesis of 1,2,3-Triazole-Linked Nucleoside-Amino Acid Conjugates as Potential Antibacterial Agents

Malkowski, Sarah N.; Dishuck, Carolyn F; Lamanilao, Gene G; Embry, Carter P; Grubb, Christopher S.; Cafiero, Mauricio; Peterson, Larryn W.

doi:10.3390/molecules22101682

Cited by 11 publications

(4 citation statements)

References 37 publications

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“…We evaluated the estrogen-like effect of LA in vitro and in vivo and explored its potential mechanisms. Previous investigations demonstrated that uridine derivatives possess significant biological properties, such as anti-HIV [ 27 ], antibacterial [ 28 ], antiviral activity [ 29 ], and anticancer [ 30 ], but no previous reports have described their estrogen-like effect. Prior evaluations have revealed that the phytoestrogens found in traditional Chinese medicine mainly consist of flavonoids, coumarins, lignans, terpenes, steroids, and other compounds [ 31 ].…”

Section: Discussionmentioning

confidence: 99%

Lepidiumuridine A: A New Natural Uridine Derivative as a Phytoestrogen Isolated from the Seeds of Lepidium apetalum Willd.

Zeng

Zhang

et al. 2018

Evidence-Based Complementary and Alternative Medicine

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There has been great interest in phytoestrogens, which are polyhydric compounds that are derived from plants and have a structure similar to that of the mammalian steroid hormone 17β-estradiol. The present study examined the estrogenic effects of a new natural uridine derivative, lepidiumuridine A (LA), that was isolated from the seeds of Lepidium apetalum. The structure was clarified and determined via analysis of extensive spectroscopic data interpretation. The activity of LA was investigated by measuring the levels of estradiol (E2), luteinizing hormone (LH), follicle stimulating hormone (FSH), and the uterus growth in mice. The proliferation experiment of MCF-7 breast cancer cells was also conducted. Western blot, in-cell western, and antagonist assays with methyl piperidino-pyrazole (MPP) were used for exploring the mechanism of the effects of LA. The results showed that LA elevated the uterine coefficient, the levels of E2, and FSH significantly. In addition, LA significantly elevated ERα expression in the uterus and MCF-7 cells. MPP inhibited the proliferation of LA-stimulated MCF-7 cell and ERα expression in MCF-7 cells. Taken together, LA had an estrogen-like effect, which was mainly mediated by the estrogen receptor ERα.

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Section: Discussionmentioning

confidence: 99%

Lepidiumuridine A: A New Natural Uridine Derivative as a Phytoestrogen Isolated from the Seeds of Lepidium apetalum Willd.

Zeng

Zhang

et al. 2018

Evidence-Based Complementary and Alternative Medicine

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“…The triazole‐hydrazone (Rambabu et al, 2016), 1,2,3‐triazole‐silatrane (Singh et al, 2018), 1,2,3‐triazole‐nucleoside (Malkowski et al, 2017; Tachallait et al, 2018), 1,2,3‐triazole‐guanidine (Bakka et al, 2017), 1,2,3‐triazole‐biotin (Paparella et al, 2018), 1,2,3‐triazole‐betulin (Bębenek et al, 2017), and 1,2,3‐triazole‐pseudoaglycon (Szűcs et al, 2017) are the some other hybrids which possessed weak to moderate activities but were less active than the reference drugs.…”

Section: Biologically Active 123‐triazole‐o‐heterocycle Hybridsmentioning

confidence: 99%

A minireview of 1,2,3‐triazole hybrids with O‐heterocycles as leads in medicinal chemistry

Saroha

Kumar

et al. 2021

Chem Biol Drug Des

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Over the past few decades, the dynamic progress in the synthesis and screening of heterocyclic compounds against various targets has made a significant contribution in the field of medicinal chemistry. Among the wide array of heterocyclic compounds, triazole moiety has attracted the attention of researchers owing to its vast therapeutic potential and easy preparation via copper and ruthenium-catalyzed azide-alkyne cycloaddition reactions. Triazole skeletons are found as major structural components in a different class of drugs possessing diverse pharmacological profiles including anti-cancer, anti-bacterial, anti-fungal, anti-viral, anti-oxidant, anti-inflammatory, anti-diabetic, anti-tubercular, and anti-depressant among B. subtilis(MIC) 26a 1.56 µg/mL 26b 3.125 µg/mL 26c 3.125 µg/mL S. aureus(MIC) 26a 1.56 µg/mL 26b 3.125 µg/mL 26c 1.56 µg/mL A. nigar(MIC) 26d 3.125 µg/mL 26e 3.125 µg/mL C. albians(MIC) 26d 3.125 µg/mL 26e 3.125 µg/mL gram negative bacteria(MIC) 26a 3.125 µg/mL 26b 3.125 µg/mL 26c 3.125 µg/mL

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“…The faculty published 2 peer‐reviewed books, [ 238,239 ] 9 peer‐reviewed book chapters, [ 240–248 ] and 115 peer‐reviewed research papers. [ 249–363 ] This comes to 1.6 peer‐reviewed products/faculty/year during the 3‐year grant period, which is 3.2 times the rate of publication for natural science faculty at PUIs. [ 46 ]…”

Section: Research Accomplishments (Intellectual Merit) and Transformamentioning

confidence: 99%

“…They are also working on the discovery of inhibitors for the LpxC enzyme for Gram‐negative bacteria. [ 285,305,383,384 ]…”

Section: Overview Of Mercury Faculty Research Effortsmentioning

confidence: 99%

Twenty years of exceptional success: The molecular education and research consortium in undergraduate computational chemistry (MERCURY)

Shields

2020

Int J of Quantum Chemistry

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The molecular education and research consortium in undergraduate computational chemistry (MERCURY) consortium, established in 2000, has contributed greatly to the scientific development of faculty and undergraduates. The MERCURY faculty peer-reviewed publication rate from 2001 to 2019 of 1.7 papers/faculty/year is 3.4 times the rate of the physical science faculty at primarily undergraduate institutions. We have worked with over 1000 students on research projects since 2001, and 75% of our undergraduate research students have been under-represented in chemistry, either female or students of color. Approximately half of our alumni attend graduate school for the purpose of obtaining advanced degrees in STEM fields, and two-thirds are female and/or students of color. We have had more than 1600 attendees at 18 MERCURY conferences, including 111 invited speakers, 61 of whom have been female and/or faculty of color. In this paper, the research accomplishments, transformational outcomes, and scientific productivity of the MERCURY faculty are highlighted.

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Design, Modeling and Synthesis of 1,2,3-Triazole-Linked Nucleoside-Amino Acid Conjugates as Potential Antibacterial Agents

Cited by 11 publications

References 37 publications

Lepidiumuridine A: A New Natural Uridine Derivative as a Phytoestrogen Isolated from the Seeds of Lepidium apetalum Willd.

Lepidiumuridine A: A New Natural Uridine Derivative as a Phytoestrogen Isolated from the Seeds of Lepidium apetalum Willd.

A minireview of 1,2,3‐triazole hybrids with O‐heterocycles as leads in medicinal chemistry

Twenty years of exceptional success: The molecular education and research consortium in undergraduate computational chemistry (MERCURY)

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