Restoration ecology is gaining momentum on the international conservation scene. In particular, restoring degraded ecosystems is central to Aichi Biodiversity Targets 14 and 15 set by the Convention on Biological Diversity. Depending on the definition of degradation, from 2 to 47% of the global ...
Ethnopharmacological relevanceTetradenia (T.) riparia (Hochst.) Codd (Lamiaceae), formerly known as Iboza riparia (Hochst.) N.E.Br., is one of the most frequently used medicinal plants in traditional Rwandese medicine. It was used as a remedy against a wide range of diseases including malaria, a...
In a previous study, we synthesized endocyclic enone jasmonate derivatives that function as anti-inflammatory and PPAR-γ-activating entities by using key functional moieties of anti-inflammatory algal metabolites. Herein, we designed additional derivatives containing an exocyclic enone moiety t...
Renal cell carcinoma (RCC) is relatively resistant to chemotherapy and radiotherapy. Clear cell RCC (ccRCC) accounts for the majority of RCC, which have mutations or epigenetic silencing of the von Hippel–Lindau (VHL) gene. VHL-positive Caki-2 cells are killed by an endogenous anticancer substa...
The stereochemical preferences of N-nitroso- and N-formyl-c-3,t-3-dimethyl-r-2,c-7-diphenyl-1,4-diazepan-5-ones 3 & 4, respectively, have been determined using 1D and 2D NMR spectral techniques. Interestingly, the N-nitroso compound 3 is found to prefer an equilibrium between alternate chair con...
Primary S-nitrosothiols (RSNOs) have received significant attention for their ability to modulate NO signaling in many physiological and pathophysiological processes. Such actions and their potential pharmaceutical uses demand a better knowledge of their stability in aqueous solutions. Herein, w...
An efficient and mild protocol for regioselective synthesis of N-Nitroso aryl ketones by palladium-catalyzed direct acylation of arenes using N-Nitroso as directing groups is described. This reaction proceeded smoothly and could tolerate a variety of functional groups. Moreover, this chemistry o...
Diet is associated with the development of cancer in the gastrointestinal (GI) tract, because dietary nitrate and nitrite are the main nitrosating agents that are responsible for the formation of carcinogenic N-nitroso compounds (NOCs) when nitrosatable substrates, such as amine and amide, are p...
In this work, the inclusion complex of DCY/CENS: N-(2-chloroethyl), N-nitroso, N′, N′-dicyclohexylsulfamid and β-cyclodextrin (β-CD) is investigated using the fluorescence spectroscopy, PM3, ONIOM2 and DFT methods. The experimental part reveals that DCY/CENS forms a 1:1 stoichiometric ratio ...
N-Nitroso-N-methylurea (NMU) is a potent carcinogen and suspected as a cause of human cancer. In this study, mutagenic NMU was detected by HPLC after the transnitrosation of non-mutagenic N-nitrosoproline (NP) to N-methylurea in the presence of thiourea (TU) under acidic conditions. The structur...
N-nitroso compounds (NOC) are a class of potent environmental carcinogens and some NOC have been classified as “probably” or “possibly” carcinogenic to humans. NOC are chemically rather simple compounds, encompassing N-nitrosamines and N-nitrosamides, and compounds carrying further functiona...
Transition metal-catalyzed directed C-H functionalization promises a straightforward route to polymerization but remains highly underexplored. We report herein the development of a polymer synthesis protocol based on Rh(III)-catalyzed N-nitroso-directed C-H olefination reaction. The single bifun...
While stimulation of formyl peptide receptors (FPRs) on the surface of human neutrophils induces several immune responses, under conditions of continuous activation of the receptor by agonists such as formyl-Met-Leu-Phe-OH (fMLP), neutrophil-dependent tissue damage ensues. Thus, FPR antagonists ...
Semipermanent side-chain protection of Orn and Lys with p-nitrobenzyloxycarbonyl (pNZ) for Fmoc/tBu chemistry does not result in the unwanted removal of α-Fmoc that occurs when groups such as Alloc are used for the same application. Furthermore, pNZ can be used in conjuction with p-nitrobenzyl ...
A rapid and efficient Fmoc/t-Bu solid-phase peptide synthesis (SPPS) of cyclic aza-β3-peptide analogs by allyl strategy is described. Our synthetic approach includes the synthesis of two new aza-β3-amino acids, Fmoc-aza-β3-Lys-OAllyl and Fmoc-aza-β3-Asp-OAllyl, then the resin attachment of t...
Benzyl (2R,3S)-(−)-6-oxo-2,3-diphenyl-4-morpholinecarboxylate (4) was successively alkylated with methyl iodide and 1,4-diiodobutane using a base. In each alkylation step anti-alkylated product formed exclusively. The iodo group was displaced with azide, which served as a precursor for the side-...
An efficient preparation of N-α-Fmoc-4-phosphono(difluoromethyl)-L-phenylalanine 5 is described. The synthesis of this phosphotyrosine isostere involves deprotection of the penultimate diethylphosphonate intermediate 4 with BSTFA/TMSI as the key step. Building block 5 can be utilized directly f...
2-(2-Chloro-benzylidene)-Cyclododecanone, a cyclic ketone has been synthesized by direct aldol condensation reaction and the single crystals were grown in mixed solved (Tetrahydrofuran and ethanol) by slow evaporation method. The linear optical property of the crystal has been studied in the wav...
This paper solves three open problems about the decidability of the vector and scalar reachability problems and the point to point reachability by fractional linear transformations over finitely generated semigroups of matrices from SL(2,Z). Our approach to solving these problems is based on the...
For an abelian group G and an integer t>0, the modified Erdös–Ginzburg–Ziv constant st′(G) is the smallest integer ℓ such that any zero-sum sequence of length at least ℓ with elements in G contains a zero-sum subsequence (not necessarily consecutive) of length t. We compute st′(G) for G=Z∕n...
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