3 research outputs found
Antibiotic Coordination Frameworks against Antibiotic Resistance: How to Involve Students through Experimental Practices in the Search for Solutions to Public Health Problems
For decades, multiple varieties of antibiotics have been
successfully
used for therapeutic purposes. Nevertheless, antibiotic resistance
is currently one of the major threats to global health. This work
presents an innovative laboratory practice carried out in an inorganic
medicinal chemistry course within the Degrees of Pharmacy and Biochemistry
for undergraduate students. This experiment includes three classes
of 2 h each. The first class consisted of the mechanochemical synthesis
of an antibiotic coordination framework (ACF) using a known antibiotic
(nalidixic acid) and zinc as the ligand. The prepared Zn-nalidixic
acid ACF (Zn-ACF) was obtained in up to 82% yield with high purity.
On the second day, the synthesized Zn-ACF was characterized by Fourier-transform
infrared spectroscopy (FTIR) and powder X-ray diffraction (PXRD).
Finally, during the last class, the antimicrobial activity was tested
against Escherichia coli by the well diffusion method.
The students verified the higher antimicrobial activity of Zn-ACF
compared to nalidixic acid, proving that small changes in the chemical
structure can result in great biological differences. In the end,
the students presented their results in a poster format, encouraging
the development of their soft skills and scientific results communication
and dissemination. In the future, it is expected that such a laboratory
experiment at the interface between medicinal chemistry, microbiology,
analytical techniques, public health, and pharmacology will lead to
the development and implementation of some service-learning practices
and will serve as a model to look at for other courses and institutions
Stilbenoids as Antifungals to Counteract Rice Blast Pathogen Pyricularia oryzae
Fungi are among the greatest biotic threats to agricultural
and
food security. Intensive monoculture cropping and resistance to single-site
fungicides in plant pathogens urge the discovery and development of
novel compounds that possibly interfere with essential cellular processes
in multiple ways. In this article, we describe our recent efforts
addressed to the identification of natural compounds as multitarget
biofungicides. A set of natural monomeric and dimeric compounds belonging
to the class of stilbenoids were synthesized and tested against wild-type
(WT) and strobilurin-resistant (RES) strains of Pyricularia oryzae, one
of the most dangerous fungal phytopathogens. Monomers deoxyrhapontigenin,
pinostilbene, and DMHS showed inhibitory activity higher than 40%,
with deoxyrhapontigenin having the highest activity on mycelial growth
(60–80% inhibition) on both WT and RES P. oryzae strains. Furthermore,
we designed and synthesized a set of molecules having a nature-derived
stilbene fragment merged with the pharmacophoric portion of strobilurins,
namely, a β-methoxyacrylate moiety. We identified two molecules
with activity comparable to the reference commercial fungicide azoxystrobin.
However, low mycelium growth inhibition of resistant strains indicates
that these compounds most likely retain the strobilurin-like mechanism
of action. Overall, the results suggest that natural stilbenoids might
be used as environmentally friendly biofungicides in rice blast management
Antibiotic Coordination Frameworks against Antibiotic Resistance: How to Involve Students through Experimental Practices in the Search for Solutions to Public Health Problems
For decades, multiple varieties of antibiotics have been
successfully
used for therapeutic purposes. Nevertheless, antibiotic resistance
is currently one of the major threats to global health. This work
presents an innovative laboratory practice carried out in an inorganic
medicinal chemistry course within the Degrees of Pharmacy and Biochemistry
for undergraduate students. This experiment includes three classes
of 2 h each. The first class consisted of the mechanochemical synthesis
of an antibiotic coordination framework (ACF) using a known antibiotic
(nalidixic acid) and zinc as the ligand. The prepared Zn-nalidixic
acid ACF (Zn-ACF) was obtained in up to 82% yield with high purity.
On the second day, the synthesized Zn-ACF was characterized by Fourier-transform
infrared spectroscopy (FTIR) and powder X-ray diffraction (PXRD).
Finally, during the last class, the antimicrobial activity was tested
against Escherichia coli by the well diffusion method.
The students verified the higher antimicrobial activity of Zn-ACF
compared to nalidixic acid, proving that small changes in the chemical
structure can result in great biological differences. In the end,
the students presented their results in a poster format, encouraging
the development of their soft skills and scientific results communication
and dissemination. In the future, it is expected that such a laboratory
experiment at the interface between medicinal chemistry, microbiology,
analytical techniques, public health, and pharmacology will lead to
the development and implementation of some service-learning practices
and will serve as a model to look at for other courses and institutions