Synthesis and biological activity of some new 3,6-dinitro-1:8-naphthaloyl- and 3,6-diamino-1:8-naphthaloylamino acids and dipeptide derivatives

Synthesis of a series of 3,6-dinitro-1:8-naphthaloylamino acids (II-IX) and some of their corresponding methyl esters (X-XVI) and 3,6-diamino-1:8-naphthaloylamino acid derivatives (XXIX-XXXVI) is described. Coupling of 3,6-dinitro-1:8-naphthaloylamino acids with amino acid methyl ester hydrochlorides in dioxane-DMF-Et3N medium using DCC method furnishes the desired 3,6-dinitro-1:8-naphthaloyldipeptide methyl esters (XVII-XXVIII). Most of the synthesized 3,6-dinitro-1:8-naphthaloylamino acids, esters and dipeptide derivatives (compounds III-VI, XI-XV, XVII, XIX-XXI, XXIII and XXV) and 3,6-diamino-1:8-naphthaloylamino acid derivatives (XXIX-XXXV) were found to be active against a number of microorganisms.     

Sorption behavior of Co and Eu radionuclides onto chitosan derivatives

Chitosan benzoyl thiourea derivative has been synthesized and used successfully for the removal of the hazardous ⁶⁰Co and ^152+154Eu radionuclides from aqueous solutions. Different parameters were applied for studying the adsorbitivity of these radionuclides, including change in pH, time, ion concentration, and equilibrium concentration. Freundlich and Langmuir isotherms were applied successfully to fit the experimental data. Two more isotherm models, Lagergren and Morris–Webber, have been applied. All the parameters and the constants calculated for the kinetic isotherms and models are evaluated and listed. A mechanism for the complex formation of Co⁺² with the chitosan derivative has been suggested.     

Ischemic bowel disease

The clinical, radiologic and pathologic features of 25 cases of ischemic bowel disease are presented. The majority of patients presented with the triad of abdominal pain, diarrhea and vomiting. In 13 patients the diarrhea was associated with the passage of bright red blood per rectum. There were 10 cases of infarction, 11 of enterocolitis and 4 had resulted in stricture formation. In five cases of enterocolitis the lesion was transient; symptoms improved with conservative medical management and the radiologic findings returned to normal. Barium enema examination yielded abnormal findings in the majority of the cases in which it was performed. Plain films of the abdomen, however, were not helpful. The actual mortality in this group of patients was 44%, 80% in those with infarction of the bowel and 20% in the other two groups.     

Improved synthesis and pharmacologic activity of the enantiomers of a new benzofurane type antiarrhythmic compound

An improved synthesis of the enantiomers of the new benzofurane-type antiarrhythmic compound 1 is described, which makes use of the enantiomerically pure mbe-lactol. Thus, acylation of the benzofurane 4 with acetic anhydride and subsequent bromination gave the bromoacetyl-derivative 6 , which, after reduction with LiAlH₄, was protected with mbe-lactol to give a mixture of the diastereomers 8A and 8b . After separation via column chromatography assignment of absolute configuration was carried out using a well-established NMR- method. Reaction with propylamine and cleavage of the protective group gave (R)- 1 and (S)- 1 , respectively. Enantiomeric purity was confirmed using a direct HPLC method with rsp-cyclodextrine as stationary phase. Pharmacological investigations on isolated guinea pig heart muscle preparations showed that GE 68 and its two enantiomers did not significantly differ from each other with regard to their negative inotropic, negative chronotropic, and lack of β-adrenoceptor blocking action. In contrast, the reference drug propafenone was equally potent in its negative inotropic and chronotropic activity as GE 68, but additionally showed a weak β-adrenoceptor blocking activity. © 1994 Wiley-Liss, Inc.     

Immunoregulatory functions of paf-acether. IV. Enhancement of IL-1 production by muramyl dipeptide-stimulated monocytes

paf-Acether (paf) is a phospholipid mediator of inflammation released from monocytes along with IL-1. In this study, we have examined the role of paf on IL-1 production by human monocytes. When paf from 1 nM to 5 microM, but not its precursor lyso paf, was added to monocytes in the presence of muramyl dipeptide (MDP) or LPS, a marked increase in IL-1 activity over the value with MDP alone was observed. In contrast, paf alone had minimal activity over the same dose range. Antibodies against rHu IL-1 alpha and rHu IL-1 beta neutralized the increased IL-1 activity. Interestingly, MDP that prompts monocytes to synthesize IL-1, induced the synthesis of paf, as well. Most of the paf produced remained cell-associated and always preceded IL-1 synthesis. When the paf receptor antagonist, L-652,731 was added to monocytes, it prevented the enhancement of IL-1 activity induced by exogenous paf. In contrast, L-652,731 had little effect on MDP-induced IL-1 synthesis in the absence of exogenous paf. This may indicate that there are alternative mechanisms involved in the sequences of events leading to IL-1 production. It is also conceivable that the paf receptor antagonist is not able to compete or inhibit endogenous paf as well as it does for exogenous paf. Nevertheless, exogenous paf in association with a second signal, modulates IL-1 production from human monocytes in a positive manner. This may constitute another means through which paf can modulate inflammatory and immune reactions.     

Validated spectrofluorimetric and resonance Rayleigh scattering methods for determining naftidrofuryl in varied pharmaceutical samples based on its interaction with erythrosin B

Naftidrofuryl is a vasodilator medication used for treating cerebral and peripheral vascular diseases. In this study, two spectroscopical techniques, spectrofluorimetric and resonance Rayleigh scattering (RRS), were utilized to quantify naftidrofuryl in its pharmaceutical samples. The developed methodologies in this study rely on a facile process of forming an association complex between erythrosine B reagent and naftidrofuryl under acidic conditions. The fluorimetric assay is based on the ability of naftidrofuryl to quench and decrease the native fluorescence intensity of the reagent when measured at ${\lambda }_{\mathit{\text{emis}}.}$ = 550 nm ( ${\lambda }_{\mathit{\text{excit}}.}$ = 526 nm). Under similar reaction conditions, the RRS method relies on the observed amplification in the RRS spectrum of the reagent at a wavelength of 577 nm following its interaction with naftidrofuryl. The methods exhibited linearity within the ranges 0.2–1.6 μg/ml (r² = 0.999) and 0.1–1.4 μg/ml (r² = 0.9994), with limit of quantitation values of 0.146 and 0.099 μg/ml, and limit of detection values of 0.048 and 0.032 μg/ml, for the fluorometric and the RRS methods, respectively. Moreover, the quenching between the dye and naftidrofuryl was studied using Stern–Volmer analysis, and the methodologies were experimentally optimized and validated. Additionally, acceptable recoveries were achieved when the procedures were applied to determine naftidrofuryl in pharmaceutical samples.     

SARS-CoV-2 spike L452R variant evades cellular immunity and increases infectivity

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Rapid Construction of a Random Genomic Library from Date-Palm (Phoenix Dactylifera L.)

A random genomic library of Tunisian date-palm varieties has been built from total cellular DNA, previously amplified according to an RAPD procedure. The resultant recombinant DNA is characterised by a size ranging from 200 to 1600 bp inserts. This DNA would constitute a large number of anonymous probes useful in Southern hybridisation experiments. It would also provide potential markers aimed at the molecular characterisation of date-palm varieties, aid the search of those associated with bayoud disease and suggest a sex determination of trees.