In 2019.0 EUR J MED CHEM published article about NATURAL-PRODUCTS; ANTIPROLIFERATIVE ACTIVITY; TRYPANOSOMA-CRUZI; IN-VITRO; 1,2,3-TRIAZOLE; PHTHALIDE; APOPTOSIS; TOXICITY; EXTRACTS; DRUGS in [Rodrigues, Michelle Peixoto; Tomaz, Deborah Campos; Teixeira, Robson Ricardo] Univ Fed Vicosa, Dept Quim, Vicosa, MG, Brazil; [de Souza, Luciana Angelo; Onofre, Thiago Souza; de Menezes, Wemerson Aquiles; de Almeida, Marcia Rogeria; Bressan, Gustavo Costa; Rangel Fietto, Juliana Lopes] Univ Fed Vicosa, Dept Bioquim & Biol Mol, Vicosa, MG, Brazil; [Onofre, Thiago Souza] Univ Fed Sao Paulo, Escola Paulista Med, Campus Sao Paulo, Sao Paulo, SP, Brazil; [Almeida-Silva, Juliana; Suarez-Fontes, Ana Marcia; Vannier-Santos, Marcos Andre] Fiocruz MS, Inst Oswaldo Cruz, Rio De Janeiro, RJ, Brazil; [Silva, Adalberto Manoel] Inst Fed Educ Ciencia & Tecnol Catarinense, Araquari, SC, Brazil in 2019.0, Cited 63.0. The Name is Benzyl Alcohol. Through research, I have a further understanding and discovery of 100-51-6. Recommanded Product: 100-51-6
Leishmania braziliensis is one of the pathogenic agents of cutaneous and mucocutanoeous leishmaniasis. There are no validated vaccines to prevent the infection and the treatment relies on drugs that often present severe side effects, which justify the efforts to find new potential antileishmanial drugs. An alternative to promote the discovery of new drugs would be the association of different chemical groups of bioactive compounds. Here we describe the synthesis and bioactivity evaluation against L. braziliensis of cinnamic acid derivatives possessing isobenzofuranone and 1,2,3-triazole functionalities. We tested 25 compounds at 10 mu M concentration against extracellular promastigotes and intracellular amastigotes during macrophage infection. Most compounds were more active against amastigotes than to promastigotes. The derivatives (E)-3-oxo-1,3-dihydroisobenzofuran-5-yl-(3,4,5-trimethoxy) cinnamate (5c), (1-(3,4-difluorobenzyl)-1H-1,2,3-triazol-4-yl)methyl cinnamate (9g), and (1-(2-bromobenzyl)-1H-1,2,3triazol-4-yl)methyl cinnamate (91) were the most effective presenting over 80% toxicity on L braziliensis amastigotes. While compound 5c is a cinnamate with an isobenzofuranone portion, 9g and 9l are triazolic cinnamic acid derivatives. The action of these compounds was comparable to amphotericin B used as positive control. Ultrastructural analysis revealed that 5c-treated parasites showed impaired cytokinesis and apoptosis triggering. Taken together, these results highlight the potential of cinnamic acid derivatives in development of novel anti-leishmanial drugs. (C) 2019 Elsevier Masson SAS. All rights reserved.
Recommanded Product: 100-51-6. Welcome to talk about 100-51-6, If you have any questions, you can contact Rodrigues, MP; Tomaz, DC; de Souza, LA; Onofre, TS; de Menezes, WA; Almeida-Silva, J; Suarez-Fontes, AM; de Almeida, MR; Silva, AM; Bressan, GC; Vannier-Santos, MA; Fietto, JLR; Teixeira, RR or send Email.
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Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles