- Alkyl-guanidine Compounds as Potent Broad-Spectrum Antibacterial Agents: Chemical Library Extension and Biological Characterization
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Nowadays, the increasing of multidrug-resistant pathogenic bacteria represents a serious threat to public health, and the lack of new antibiotics is becoming a global emergency. Therefore, research in antibacterial fields is urgently needed to expand the currently available arsenal of drugs. We have recently reported an alkyl-guanidine derivative (2), characterized by a symmetrical dimeric structure, as a good candidate for further developments, with a high antibacterial activity against both Gram-positive and Gram-negative strains. In this study, starting from its chemical scaffold, we synthesized a small library of analogues. Moreover, biological and in vitro pharmacokinetic characterizations were conducted on some selected derivatives, revealing notable properties: broad-spectrum profile, activity against resistant clinical isolates, and appreciable aqueous solubility. Interestingly, 2 seems neither to select for resistant strains nor to macroscopically alter the membranes, but further studies are required to determine the mode of action.
- Pasero, Carolina,D'Agostino, Ilaria,De Luca, Filomena,Zamperini, Claudio,Deodato, Davide,Truglio, Giuseppina I.,Sannio, Filomena,Del Prete, Rosita,Ferraro, Teresa,Visaggio, Daniela,Mancini, Arianna,Guglielmi, Mario B.,Visca, Paolo,Docquier, Jean-Denis,Botta, Maurizio
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p. 9162 - 9176
(2018/10/24)
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- CATALYTIC ALKYL GROUP EXCHANGE REACTION OF PRIMARY AND SECONDARY AMINES.
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It has been shown that primary and secondary amines undergo alkyl group exchange reactions upon treatment with palladium catalyst as depicted in an operationally simple and efficient reaction which provides a convenient method for synthesis of unsymmetrical amines. The application of the reaction for the preparation of various substituted amines and heterocyclic compounds such as hexahydropyrimidine tetrahydropyrimidine, imidazolidine, and imidazoles is described. The preparation of polyamines such as H//2N(CH//2)//mNH(CH//2)//nNH//2 (10) and H//2N(CH//2)//lNH(CH//2)//mNH(CH//2)//nNH//2 (l-n, equals 2,3; 11) is readily performed by the appadium-catalyzed reactions of azetidine (6) and aziridine (7) via azetine (9) and azirine intermediates. The mechanism the palladium-catalyzed reaction has been extensively studied on the carbonylation, racemization, and deuteurium-exchange reaction of (S)-( minus )- alpha -phenylethylamine (17).
- Murahashi,Yoshimura,Tsumiyama,Kojima
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p. 5002 - 5011
(2007/10/02)
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- Mixtures having antimicrobial or pesticidal effect
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The present invention relates to mixtures of guanidated aliphatic polyamines, or their acid addition salts, having antimicrobial or pesticidal effect. More particularly the invention relates to such mixtures which have a total degree of guanidation exceeding 30%. The mixtures are suitable for agricultural and industrial use.
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