3,4,5,3′,5′-Pentabromo-2-(2′-hydroxybenzoyl)pyrrole: a potential lead compound as anti-Gram-positive and anti-biofilm agent

Schillaci, Domenico; Petruso, Salvatore; Sciortino, Vincenza

doi:10.1016/j.ijantimicag.2004.11.014

Cited by 44 publications

(30 citation statements)

References 11 publications

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“…MICs were determined by the previously described micro-method (Schillaci et al, 2005). Briefly, a series of solutions of 5GC was prepared with a range of concentrations from 2.5 to 0.07 μg/mL (obtained by two-fold serial dilution).…”

Section: Microbial Strains and Growth Conditions And Minimum Inhibitomentioning

confidence: 99%

Gender differences in the immune system activities of sea urchin Paracentrotus lividus

Arizza

Vazzana

Schillaci

et al. 2013

Comparative Biochemistry and Physiology Part A: Molecular &

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In the immune system of vertebrates, gender-specific differences in individual immune competence are well known. In general, females possess more powerful immune response than males. In invertebrates, the situation is much less clear. For this purpose we have chosen to study the immune response of the two sexes of the echinoderm Paracentrotus lividus in pre-and post-spawning phases. The coelomic fluid from the echinoderms contains several coelomocyte types and molecules involved in innate immune defenses. In this article we report that the degree of immune responses in the P. lividus differs according to sex in both pre-and post-spawning phases. We found in all tests that females were more active than males. The results indicate that females possess a significant higher number of immunocytes consisting of phagocytes and uncolored spherulocytes. Since the immunological activity is mainly based on immunocytes, it was not surprising that females possessed the highest values of cytotoxicity and hemolysis activity and showed a greater ability to uptake neutral red and phagocyte yeasts cells, while the average number of ingested particles per active phagocyte was not significantly different. Furthermore, agglutinating activity was more evident in the coelomocyte lysate and coelomic fluid of females than in those of males. Finally we found that the acidic extract of female gonads possessed greater antimicrobial activity than that of male gonads. These results make it very likely that gender differences in the immune response are not restricted to vertebrates; rather, they are a general evolutionary phenomenon.

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Section: Microbial Strains and Growth Conditions And Minimum Inhibitomentioning

confidence: 99%

Gender differences in the immune system activities of sea urchin Paracentrotus lividus

Arizza

Vazzana

Schillaci

et al. 2013

Comparative Biochemistry and Physiology Part A: Molecular &

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“…Minimum inhibitory concentrations (MICs) against tested strains were determined as previously described by a broth dilution micromethod [28]. A series of solutions with a range of concentrations from 40 to 0.1 μg/mL (obtained by twofold serial dilution) was made in Mueller-Hinton broth (Merck) in a 96-well plate.…”

Section: Determination Of Micsmentioning

confidence: 99%

Synthesis, characterization, crystal structures and in vitro antistaphylococcal activity of organotin(IV) derivatives with 5,7-disubstituted-1,2,4-triazolo[1,5-a]pyrimidine

Girasolo

Canfora

Sabatino

et al. 2012

Journal of Inorganic Biochemistry

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New organotin(IV) complexes of 5,7-ditertbutyl-1,2,4-triazolo[1,5-a]pyrimidine (dbtp) and 5,7-diphenyl-1,2,4-triazolo [1,5-a]pyrimidine (dptp) with 1:1 and/or 1:2 stoichiometry were synthesized and investigated by X-ray diffraction, Sn Mössbauer in the solid state and by 1 H and 13 C NMR spectroscopy, in solution. Moreover, the crystal and molecular structures of Et 2 SnCl 2 (dbtp) 2 and Ph 2 SnCl 2 (EtOH) 2 (dptp) 2 are reported. The complexes contain hexacoordinated tin atoms: in Et 2 SnCl 2 (dbtp) 2 two 5,7-ditertbutyl-1,2,4-triazolo[1,5-a]pyrimidine molecules coordinate classically the tin atom through N(3) atom and the coordination around the tin atom shows a skew trapezoidal structure with axial ethyl groups. In Ph 2 SnCl 2 (EtOH) 2 (dptp) 2 two ethanol molecules coordinate tin through the oxygen atom and the 5,7-diphenyl-1,2,4-triazolo [1,5-a]pyrimidine molecules are not directly bound to the metal center but strictly H-bonded, through N (3), to the \OH group of the ethanol moieties; Ph 2 SnCl 2 (EtOH) 2 (dptp) 2 has an all-trans structure and the C-Sn-C fragment is linear. On the basis of Mössbauer data, the 1:2 diorganotin(IV) complexes are advanced to have the same structure of Et 2 SnCl 2 (dbtp) 2 , while Me 2 SnCl 2 (dptp) 2 to have a regular all-trans octahedral structure. A distorted cis-R 2 trigonal bipyramidal structure is assigned to 1:1 diorganotin(IV) complexes. The in vitro antibacterial activities of the synthesized complexes have been tested against a group of reference pathogen micro-organisms and some of them resulted active with MIC values of 5 μg/mL, most of all against staphylococcal strains, which shows their inhibitory effect.

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“…The antibacterial activity of these derivatives may be closely related to their halogen content, because it increases as the degree of halogenation [38,39]. Table 2.…”

Section: Natural Pyrrolomycinsmentioning

confidence: 99%

“…Important structural features of the pyrrolomycins are: (i) their high halogenation degree, which is usually represented by chlorine substituents; and (ii) in some cases, the presence of a nitro group at the position 3 of the pyrrole ring. The antibacterial activity of these derivatives may be closely related to their halogen content, because it increases as the degree of halogenation [38,39].…”

Section: Natural Pyrrolomycinsmentioning

confidence: 99%

“…Results, expressed as MIC values, showed that the antibacterial activity was correlated to the number of bromine atoms present on the molecule and the most active compound was the pentabromo analog 4 ( Table 7). The authors continued the studies by testing, in vitro, compound 4 on seven reference Gram-positive bacterial strains including S. epidermidis, S. aureus, Listeria monocytogenes, Streptococcus agalactiae, Bacillus subtilis, and Enterococcus faecalis [38]. The activity of compound 4 was compared to the activity of vancomycin, and MIC and MBC values were determined.…”

Section: Synthetic Pyrrolomycinsmentioning

confidence: 99%

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Pharmaceutical Potential of Synthetic and Natural Pyrrolomycins

et al. 2015

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Abstract:The emergence of antibiotic resistance is currently considered one of the most important global health problem. The continuous onset of multidrug-resistant Gram-positive and Gram-negative bacterial strains limits the clinical efficacy of most of the marketed antibiotics. Therefore, there is an urgent need for new antibiotics. Pyrrolomycins are a class of biologically active compounds that exhibit a broad spectrum of biological activities, including antibacterial, antifungal, anthelmintic, antiproliferative, insecticidal, and acaricidal activities. In this review we focus on the antibacterial activity and antibiofilm activity of pyrrolomycins against Gram-positive and Gram-negative pathogens. Their efficacy, combined in some cases with a low toxicity, confers to these molecules a great potential for the development of new antimicrobial agents to face the antibiotic crisis.

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3,4,5,3′,5′-Pentabromo-2-(2′-hydroxybenzoyl)pyrrole: a potential lead compound as anti-Gram-positive and anti-biofilm agent

Cited by 44 publications

References 11 publications

Gender differences in the immune system activities of sea urchin Paracentrotus lividus

Gender differences in the immune system activities of sea urchin Paracentrotus lividus

Synthesis, characterization, crystal structures and in vitro antistaphylococcal activity of organotin(IV) derivatives with 5,7-disubstituted-1,2,4-triazolo[1,5-a]pyrimidine

Pharmaceutical Potential of Synthetic and Natural Pyrrolomycins

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