International Journal of Bioorganic and Medicinal Chemistry

A dual responsive probe based on bromo substituted salicylhydrazone moiety for the colorimetric detection of Cd2+ ions and fluorometric detection of F‒ ions: Applications in live cell imaging

Krishnaveni Karuppiah, Iniya Murugan, Murugesan Sepperumal, Siva Ayyanar — Wed, 17 Feb 2021 00:00:00 +0000

A new fluorimetric and colorimetric dual-mode probe, 4-bromo-2-(hydrazonomethyl) phenol (BHP) has been synthesized and successfully utilized for the recognition of Cd²⁺/F^‒ ions in DMSO/H₂O (9:1, v/v) system. The probe displays dual channel of detection via fluorescence enhancement and colorimetric changes upon binding with F^‒ and Cd²⁺ ions respectively. The Job’s plot analysis, ESI-MS studies, Density Functional Theoretical (DFT) calculations, ¹H NMR and ¹⁹F NMR titration results were confirmed and highly supported the 1:1 binding stoichiometry of the probe was complexed with Cd²⁺/F^‒ ions. Furthermore, intracellular detection of F^‒ ions in HeLa cells and fluorescence imaging analysis in Zebrafish embryos results of the probe BHP might be used to reveal their potential applications in a biological living system.

Molecular Entities of Antimicrobial Drugsand Resistance Mechanism Underlying: Bioaccessibility, Bioavailability, and Bioaccumulation

Rajiv Kumar — Fri, 25 Jun 2021 00:00:00 +0000

The three major groups of antifungal agents are there that are used in clinical use, azoles, polyenes, and allylamine/thiocarbamates, all own their antifungal activities to inhibit the reactivity of microbial or stop direct interaction of microbial with healthy cells.³ Microbial organometallic assimilation, the bioaccessibility, bioavailability, and bioaccumulation properties of inorganic metals in different antimicrobial moieties that are interrelated and classified as abiotic (e.g., organic carbon) and biotic (e.g., uptake and metabolism).⁴

The relatively higher concentrations of trace elements to arsenic may have influenced on methylation process of inorg- As in humans

Uttam K Chowdhury — Fri, 16 Jul 2021 00:00:00 +0000

Trace elements (As, Se, Zn, Co, Cu, Pb, Cd, Ni, Mn, and Hg) were analyzed in blood as well as urine of arsenic exposed people in Mexico by using ICP-MS to know the influence of trace elements for biotransformation process of inorganic arsenic.

The concentrations of Cu and Mn were significantly higher, and the concentrations of As, Zn, and Pb were significantly lower in blood for females compared to males. The correlations between the ratios of the concentrations of Se, Zn, Co, Cu, Pb, Cd, Ni, Mn, or Hg to As in blood as well as urine and urinary arsenic metabolites were stronger than the correlations found between the concentrations of above elements and urinary arsenic metabolites for both females and males. The concentrations of trace elements (for examples: Se, Mn, Hg, etc.) relative to As in urine and blood were positively correlated with urinary % inorg As as well as % MMA, and negatively correlated with % DMA as well as the ratios of % DMA to % MMA.

On the other hand, due to low level of creatinine in urine, adjusted urinary trace elements concentrations express as µg/g cre were significantly higher than the unadjusted concentrations express as µg/L for the urine groups with arsenic concentrations ≤50 µg As/L. But there were no significant correlations observed between adjusted and unadjusted concentrations of trace elements for the urine groups with arsenic concentrations >50 µg As/L. Adjusted urinary Se, Mn, and Hg concentrations were negatively and significantly associated with urinary creatinine for both females and males.

The results of this study suggest that trace elements may have influenced for biotransformation process of inorganic arsenic in humans. The results also suggest that Se, Mn as well as Hg may decrease arsenic methylation with decreasing creatinine formation for both sexes, but it could be concentration dependent.

Abbreviation: SAM, S-adenosyl-L-methionine; SAHC, S-adenosyl-L-homocysteine.

Revisit: The Synthesis of 3-amino pyrazoles promoted by p-toluenesulfonic acid as an efficient catalyst under solvent and solvent-free conditions

Suryakiran Navath — Sat, 17 Jul 2021 00:00:00 +0000

An efficient and facile synthesis of 3-amino pyrazoles has been described. The reaction of b-keto nitriles with hydrazines using p-toluenesulfonic acid as an efficient catalyst under solvent and solvent-free conditions afford corresponding 3-amino pyrazoles in excellent yields

Synthesis and structural elucidation of a series of isoflavones-based on FPR antagonists

Eugenio Uriarte, Fernanda Borges, Alexandra Gaspar — Thu, 25 Feb 2021 00:00:00 +0000

Isoflavones are naturally occurring compounds well-known for their beneficial role in several diseases, such as cancer and inflammation. Recently some isoflavones derivatives were reported as potent and competitive antagonists of formyl peptide receptors (FPRs) with an important role in regulating the inflammatory process. As a result of their biological activities, there is a huge interest in developing synthetic procedures to obtain isoflavones. Surprisingly, and as far as our knowledge goes, the synthetic work and full characterisation of the isoflavones described as FPR antagonists weren’t yet reported. The work herein described comprises the synthesis of two series of 2-trifluoromethyl isoflavones, including the ones described as FPR antagonists and their complete characterisation by 1D, 2D NMR techniques and high-resolution mass spectroscopy.