12 research outputs found
Explorations of Caffeic Acid Derivatives: Total Syntheses of Rufescenolide, Yunnaneic Acids C and D, and Studies toward Yunnaneic Acids A and B
Yunnaneic
acids A–D, isolated from the roots of Salvia
yunnanensis, are hexameric (A and B) and trimeric
(C and D) assemblies of caffeic acid that feature an array of synthetically
challenging and structurally interesting domains. In addition to being
caffeic acid oligomers, yunnaneic acids A and B are formally dimeric
and heterodimeric adducts of yunnaneic acids C and D. Herein we report
the first total syntheses of yunnaneic acids C and D featuring the
formation of their bicyclo[2.2.2]Âoctene cores in a single step from
simple precursors via an oxidative dearomatization/Diels–Alder
cascade that may have biogenetic relevance. In addition, exploitation
of the key intermediate resulting from this cascade reaction has enabled
rapid access to the structurally related caffeic acid metabolite rufescenolide
through an unexpected Lewis acid-mediated reduction. Finally, we report
the results of extensive model studies toward forming the dimeric
yunnaneic acids A and B. These explorations indicate that the innate
reactivities of the monomeric fragments do not favor spontaneous formation
of the desired dimeric linkages. Consequently, enzymatic involvement
may be required for the biosynthesis of these more complex family
members
Explorations of Caffeic Acid Derivatives: Total Syntheses of Rufescenolide, Yunnaneic Acids C and D, and Studies toward Yunnaneic Acids A and B
Yunnaneic
acids A–D, isolated from the roots of Salvia
yunnanensis, are hexameric (A and B) and trimeric
(C and D) assemblies of caffeic acid that feature an array of synthetically
challenging and structurally interesting domains. In addition to being
caffeic acid oligomers, yunnaneic acids A and B are formally dimeric
and heterodimeric adducts of yunnaneic acids C and D. Herein we report
the first total syntheses of yunnaneic acids C and D featuring the
formation of their bicyclo[2.2.2]Âoctene cores in a single step from
simple precursors via an oxidative dearomatization/Diels–Alder
cascade that may have biogenetic relevance. In addition, exploitation
of the key intermediate resulting from this cascade reaction has enabled
rapid access to the structurally related caffeic acid metabolite rufescenolide
through an unexpected Lewis acid-mediated reduction. Finally, we report
the results of extensive model studies toward forming the dimeric
yunnaneic acids A and B. These explorations indicate that the innate
reactivities of the monomeric fragments do not favor spontaneous formation
of the desired dimeric linkages. Consequently, enzymatic involvement
may be required for the biosynthesis of these more complex family
members
Explorations of Caffeic Acid Derivatives: Total Syntheses of Rufescenolide, Yunnaneic Acids C and D, and Studies toward Yunnaneic Acids A and B
Yunnaneic
acids A–D, isolated from the roots of Salvia
yunnanensis, are hexameric (A and B) and trimeric
(C and D) assemblies of caffeic acid that feature an array of synthetically
challenging and structurally interesting domains. In addition to being
caffeic acid oligomers, yunnaneic acids A and B are formally dimeric
and heterodimeric adducts of yunnaneic acids C and D. Herein we report
the first total syntheses of yunnaneic acids C and D featuring the
formation of their bicyclo[2.2.2]Âoctene cores in a single step from
simple precursors via an oxidative dearomatization/Diels–Alder
cascade that may have biogenetic relevance. In addition, exploitation
of the key intermediate resulting from this cascade reaction has enabled
rapid access to the structurally related caffeic acid metabolite rufescenolide
through an unexpected Lewis acid-mediated reduction. Finally, we report
the results of extensive model studies toward forming the dimeric
yunnaneic acids A and B. These explorations indicate that the innate
reactivities of the monomeric fragments do not favor spontaneous formation
of the desired dimeric linkages. Consequently, enzymatic involvement
may be required for the biosynthesis of these more complex family
members
Explorations of Caffeic Acid Derivatives: Total Syntheses of Rufescenolide, Yunnaneic Acids C and D, and Studies toward Yunnaneic Acids A and B
Yunnaneic
acids A–D, isolated from the roots of Salvia
yunnanensis, are hexameric (A and B) and trimeric
(C and D) assemblies of caffeic acid that feature an array of synthetically
challenging and structurally interesting domains. In addition to being
caffeic acid oligomers, yunnaneic acids A and B are formally dimeric
and heterodimeric adducts of yunnaneic acids C and D. Herein we report
the first total syntheses of yunnaneic acids C and D featuring the
formation of their bicyclo[2.2.2]Âoctene cores in a single step from
simple precursors via an oxidative dearomatization/Diels–Alder
cascade that may have biogenetic relevance. In addition, exploitation
of the key intermediate resulting from this cascade reaction has enabled
rapid access to the structurally related caffeic acid metabolite rufescenolide
through an unexpected Lewis acid-mediated reduction. Finally, we report
the results of extensive model studies toward forming the dimeric
yunnaneic acids A and B. These explorations indicate that the innate
reactivities of the monomeric fragments do not favor spontaneous formation
of the desired dimeric linkages. Consequently, enzymatic involvement
may be required for the biosynthesis of these more complex family
members
Explorations of Caffeic Acid Derivatives: Total Syntheses of Rufescenolide, Yunnaneic Acids C and D, and Studies toward Yunnaneic Acids A and B
Yunnaneic
acids A–D, isolated from the roots of Salvia
yunnanensis, are hexameric (A and B) and trimeric
(C and D) assemblies of caffeic acid that feature an array of synthetically
challenging and structurally interesting domains. In addition to being
caffeic acid oligomers, yunnaneic acids A and B are formally dimeric
and heterodimeric adducts of yunnaneic acids C and D. Herein we report
the first total syntheses of yunnaneic acids C and D featuring the
formation of their bicyclo[2.2.2]Âoctene cores in a single step from
simple precursors via an oxidative dearomatization/Diels–Alder
cascade that may have biogenetic relevance. In addition, exploitation
of the key intermediate resulting from this cascade reaction has enabled
rapid access to the structurally related caffeic acid metabolite rufescenolide
through an unexpected Lewis acid-mediated reduction. Finally, we report
the results of extensive model studies toward forming the dimeric
yunnaneic acids A and B. These explorations indicate that the innate
reactivities of the monomeric fragments do not favor spontaneous formation
of the desired dimeric linkages. Consequently, enzymatic involvement
may be required for the biosynthesis of these more complex family
members
Explorations of Caffeic Acid Derivatives: Total Syntheses of Rufescenolide, Yunnaneic Acids C and D, and Studies toward Yunnaneic Acids A and B
Yunnaneic
acids A–D, isolated from the roots of Salvia
yunnanensis, are hexameric (A and B) and trimeric
(C and D) assemblies of caffeic acid that feature an array of synthetically
challenging and structurally interesting domains. In addition to being
caffeic acid oligomers, yunnaneic acids A and B are formally dimeric
and heterodimeric adducts of yunnaneic acids C and D. Herein we report
the first total syntheses of yunnaneic acids C and D featuring the
formation of their bicyclo[2.2.2]Âoctene cores in a single step from
simple precursors via an oxidative dearomatization/Diels–Alder
cascade that may have biogenetic relevance. In addition, exploitation
of the key intermediate resulting from this cascade reaction has enabled
rapid access to the structurally related caffeic acid metabolite rufescenolide
through an unexpected Lewis acid-mediated reduction. Finally, we report
the results of extensive model studies toward forming the dimeric
yunnaneic acids A and B. These explorations indicate that the innate
reactivities of the monomeric fragments do not favor spontaneous formation
of the desired dimeric linkages. Consequently, enzymatic involvement
may be required for the biosynthesis of these more complex family
members
Explorations of Caffeic Acid Derivatives: Total Syntheses of Rufescenolide, Yunnaneic Acids C and D, and Studies toward Yunnaneic Acids A and B
Yunnaneic
acids A–D, isolated from the roots of Salvia
yunnanensis, are hexameric (A and B) and trimeric
(C and D) assemblies of caffeic acid that feature an array of synthetically
challenging and structurally interesting domains. In addition to being
caffeic acid oligomers, yunnaneic acids A and B are formally dimeric
and heterodimeric adducts of yunnaneic acids C and D. Herein we report
the first total syntheses of yunnaneic acids C and D featuring the
formation of their bicyclo[2.2.2]Âoctene cores in a single step from
simple precursors via an oxidative dearomatization/Diels–Alder
cascade that may have biogenetic relevance. In addition, exploitation
of the key intermediate resulting from this cascade reaction has enabled
rapid access to the structurally related caffeic acid metabolite rufescenolide
through an unexpected Lewis acid-mediated reduction. Finally, we report
the results of extensive model studies toward forming the dimeric
yunnaneic acids A and B. These explorations indicate that the innate
reactivities of the monomeric fragments do not favor spontaneous formation
of the desired dimeric linkages. Consequently, enzymatic involvement
may be required for the biosynthesis of these more complex family
members
PENGARUH KEPEMIMPINAN, LINGKUNGAN KERJA DAN STRES KERJA TERHADAP TURNOVER INTENTION PADA KARYAWAN BANK MUAMALAT KC YOGYAKARTA
This study aims to explain the influence of leadership, work environment, and work stress on turnover intention on employees of Bank Muamalat KC Yogyakarta. The dependent variable in this study is turnover intention. While the independent variables are leadership, work environment, and work stress. The sampling used is 56 employees. The sampling method uses purposive sampling using several criteria. Data collection techniques are done by distributing questionnaires and interviews. The analytical tool used is multiple linear regression techniques. The results of the analysis state that leadership and work environment do not have a effect on turnover intention. While job stress has a positive and significant effect on turnover intention
Discovery and Optimization of a Novel Macrocyclic Amidinourea Series Active as Acidic Mammalian Chitinase Inhibitors
Our research group has been involved for a long time
in the development
of macrocyclic amidinoureas (MCAs) as antifungal agents. The mechanistic
investigation drove us to perform an in silico target
fishing study, which allowed the identification of chitinases as one
of their putative targets, with 1a showing a submicromolar
inhibition of Trichoderma viride chitinase. In this
work, we investigated the possibility to further inhibit the corresponding
human enzymes, acidic mammalian chitinase (AMCase) and chitotriosidase
(CHIT1), involved in several chronic inflammatory lung diseases. Thus,
we first validated the inhibitory activity of 1a against
AMCase and CHIT1 and then designed and synthesized new derivatives
aimed at improving the potency and selectivity against AMCase. Among
them, compound 3f emerged for its activity profile along
with its promising in vitro ADME properties. We also
gained a good understanding of the key interactions with the target
enzyme through in silico studies
Identification of New Fyn Kinase Inhibitors Using a FLAP-Based Approach
The
abnormal activity of Fyn tyrosine kinase has been shown to
be related to various human cancers. Furthermore, its involvement
in signaling pathways that lead to severe pathologies, such as Alzheimer’s
and Parkinson’s diseases, has also been demonstrated, thus
making Fyn an attractive target for the discovery of potential novel
therapeutics for brain pathologies and tumors. In this study we evaluated
the reliability of various screening approaches based on the FLAP
software. By the application of the best procedure, the virtual screening
workflow was used to filter the Gold and Platinum database from Asinex
to identify new Fyn inhibitors. Enzymatic assays revealed that among
the eight top-scoring compounds five proved to efficiently inhibit
Fyn activity with IC<sub>50</sub> values in the micromolar range.
These results demonstrate the validity of the methodologies we followed.
Furthermore, the five active compounds herein described may be considered
as interesting leads for the development of new and more efficient
Fyn inhibitors