In vitro Investigation of the Antimicrobial Activity of a Series of Lipophilic Phenols and Naphthols

Five groups of phenols/naphthols (42 compounds in total) were synthesized and screened against Gram-positive Staphylococcus aureus and Bacillus subtilis, Gram-negative Escherichia coli and Klebsiella pneumoniae, and the fungus Candida albicans. Whereas compounds were found inactive against Gram-negative bacteria, potent activities against Gram-positive bacteria were observed. The activities correlate with the ability of molecules to form quinone methides, suggesting potential new modes of action.KEYWORDS Antimicrobial activity, phenols, naphthols, quinone methides

Photodecarboxylation of Adamantane Amino Acids Activated by Phthalimide

Adamantane alpha-, beta-, and delta-amino acids activated by phthalimide (i.e., 3-6) were synthesized, and their photochemical reactivities were investigated. Amino acid derivatives 3-6 underwent a photoinduced electron transfer (PET) and decarboxylation reaction sequence, most probably through a triplet excited state. The decarboxylations of the beta-amino acid derivatives were succeeded by cyclization reactions that afforded complex polycyclic molecules with potential biological interest. The adamantyl radical that is produced by the photoinduced decarboxylation could be trapped by alkenes or oxygen to deliver adducts or alcohols, respectively. The photodecarboxylation process was shown to be more efficient under acetone sensitization conditions (with quantum yields, Phi = 0.02-0.5) than upon direct excitation, and the reactivity was dependent on the chain length (intramolecular distance) between the electron donor (carboxylate) and acceptor (phthalimide in the triplet excited state) of the derivative. The formation of different radicals, that is, the 1- or 2-adamantyl intermediate, probably does not affect the overall rate of the decarboxylation This current report provides a better understanding of photodecarboxylation and the rational design of molecular systems to undergo photoinduced decarboxylation and cyclization reactions

Substituted adamantylphthalimides: Synthesis, antiviral and antiproliferative activity

In this study, three groups of adamantylphthalimides, bearing different substituents at the phthalimide moiety, N-(4'-R2 )phthalimidoadamantanes (1-7), 3-[N-(4'-R2 )phthalimido]-1-adamantanols (8-10), and 3-[N-(4'-R2 )phthalimido]adamantane-1-carboxylic acids (11-15), were synthesized and screened against tumor cells and viruses. The most potent compounds are not substituted at the adamantane and bear an OH or NH2 substituent at the phthalimide (compounds 3 and 5). The antiproliferative activities of compounds 3 and 5 are in the micromolar range, much higher than the one of thalidomide. A minor antiviral activity against cytomegalovirus and varicella-zoster virus was found for compounds 3 and 5, but these compounds lacked selectivity. The results presented are important for the rational design of the next-generation compounds with anticancer and antiviral activities.status: publishe

Splenectomy for Visceral Leishmaniasis Out of an Endemic Region: A Case Report and Literature Review

Visceral leishmaniasis (also known as kala-azar) is characterized by fever, weight loss, swelling of the spleen and liver, and pancytopenia. If it is not treated, the fatality rate in developing countries can be as high as 100% within 2 years. In a high risk situation for perioperative bleeding due to severe thrombocytopenia/coagulopathy, we present a rare challenge for urgent splenectomy in a patient with previously undiagnosed visceral leishmaniasis. A histologic examination of the spleen revealed a visceral leishmaniasis, and the patient was successfully treated with amphotericin B