Structure and Properties of the di- ((2S) -2-amino-3- (1H-indol-3-yl)propionate)-dihydro-tetraiodide

New organic iodine complex in the amino acid - alkali metal salt - iodine - water systemwas synthesized. The physico-chemical properties of complexdi- ((2S) -2-amino-3- (1H-indol-3-yl) propionate)-dihydro-tetraiodide were studied. Microscopic analysis shows that particles of complex have elongated needle-like linear stick-like shapes with average size 2.50-4.00 µm. The cytotoxicity test on MDCK cell culture, antimicrobial activity on S. aureus ATCC 6538-Р (museum susceptible strain); S. aureus ATCC-BAA-39 (museum multiresistant strain); E. coli ATCC 8739 (museum susceptible strain); E. coli ATCC-BAA-196 (museum multiresistant strain); P. aeruginosa ATCC 9027 (museum susceptible strain); P. aeruginosa TA2were observed. Complex has low cytotoxicity, direct antiviral effect, and antimicrobial activity against antibiotic-resistant strains of microorganisms. Di- ((2S) -2-amino-3- (1H-indol-3-yl) propionate)-dihydro-tetraiodide does not cause any mutagenic effect on mammalian cells of the L5178Y line, both in the presence and in the absence of metabolic activation.

New Acyl Derivatives of 3-Aminofurazanes and Their Antiplasmodial Activities

An N-acylated furazan-3-amine of a Medicines for Malaria Venture (MMV) project has shown activity against different strains of Plasmodium falciparum. Seventeen new derivatives were prepared and tested in vitro for their activities against blood stages of two strains of Plasmodium falciparum. Several structure–activity relationships were revealed. The activity strongly depended on the nature of the acyl moiety. Only benzamides showed promising activity. The substitution pattern of their phenyl ring affected the activity and the cytotoxicity of compounds. In addition, physicochemical parameters were calculated (log P, log D, ligand efficiency) or determined experimentally (permeability) via a PAMPA. The N-(4-(3,4-diethoxyphenyl)-1,2,5-oxadiazol-3-yl)-3-(trifluoromethyl)benzamide possessed good physicochemical properties and showed high antiplasmodial activity against a chloroquine-sensitive strain (IC50(NF54) = 0.019 µM) and even higher antiplasmodial activity against a multiresistant strain (IC50(K1) = 0.007 µM). Compared to the MMV compound, the permeability and the activity against the multiresistant strain were improved.

Inhibitory Effect of Methanolic and Methanolic-Aqueous Mixture Extract of Leaves of Plectranthus neochilus Schltr (Lamiaceae) and Bauhinia rufescens Lam (Fabaceae) on Two Strains of Enterobacteria Producing Beta-lactamases

The objective of the study was to evaluate in vitro inhibitory effect of methanolic and methanolic-aqueous mixture extracts of Plectranthus neochilus Schltr (P. neochilus) and Bauhinia rufescens Lam (B. rufescens) on the growth of Escherichia coli 25922 and Proteus mirabilis. A phytochemical screening was carried out to highlight compounds (phenolic compounds, flavonoids, alkaloids) with antibacterial activity. Then, an antibiogram was Carried out to investigate the enzymes rendering the resistance. Finally, the E-test was used to evaluate the antibacterial activity of the extract mixture. The Screening results showed that both plants contain total phenolics, flavonoids and alkaloids compounds. The antibiogram has made it possible to establish the sensitivity profile of the strains tested with regard to certain antibiotics. The extract mixture showed antibacterial activity on both strains tested. In the present work, the different mixtures of extracts showed an inhibitory effect on Escherichia coli 25922 [a strain sensitive to almost all the antibiotics tested, in particular the three classes: beta-lactams (Ceftazidine, Ceftriaxone, Meropenem), quinolones (Levofloxacin, Ciprofloxacin) and aminoglycosides (Gentamicin, Amikacin)] and on Proteus mirabilis (a multiresistant strain with almost all the antibiotics tested).

Cajachalcone: An Antimalarial Compound fromCajanus cajanLeaf Extract

Cajanus cajanL, a member of the family Fabaceae, was identified from the Nigerian antimalarial ethnobotany as possessing antimalarial properties. The bioassay-guided fractionation of the crude methanol extract ofC. cajanleaves was donein vitrousing the multiresistant strain ofPlasmodium falciparum(K1) in the parasite lactate dehydrogenase assay. Isolation of compound was achieved by a combination of chromatographic techniques, while the structure of the compound was elucidated by spectroscopy. This led to the identification of a cajachalcone, 2′,6′-dihydroxy-4-methoxy chalcone, as the biologically active constituent from the ethyl acetate fraction. Cajachalcone had an IC50value of 2.0 μg/mL (7.4 μM) and could be a lead for anti-malarial drug discovery.

Cloning and Functional Analysis of the Gene Encoding the 33- to 36-Kilodalton Outer Membrane Protein Associated with Carbapenem Resistance in Acinetobacter baumannii

ABSTRACT We investigated a multiresistant strain of Acinetobacter baumannii isolated in our hospital. Analysis of the N-terminal peptide sequence of the outer membrane proteins (OMPs) purified from the strain allowed us to clone and sequence the nucleotides of the gene encoding the 33- to 36-kDa OMP associated with carbapenem resistance in A. baumannii