119053-70-2Relevant academic research and scientific papers
New 1,2,3-triazole-based analogues of benznidazole for use against Trypanosoma cruzi infection: In vitro and in vivo evaluations
Leite, Débora Inácio,Fontes, Fábio de Vasconcellos,Bastos, Monica Macedo,Hoelz, Lucas Villas Boas,Bianco, Maria da Concei??o Avelino Dias,de Oliveira, Andressa Paula,da Silva, Patricia Bernardino,da Silva, Cristiane Fran?a,Batista, Denise da Gama Jean,da Gama, Aline Nefertiti Silva,Peres, Raiza Brand?o,Villar, Jose Daniel Figueroa,Soeiro, Maria de Nazaré Correia,Boechat, Nubia
, p. 1670 - 1682 (2018)
Chagas disease has spread throughout the world mainly because of the migration of infected individuals. In Brazil, only benznidazole (Bnz) is used; however, it is toxic and not active in the chronic phase, and cases of resistance are described. This work aimed at the synthesis and the trypanocidal evaluation in vitro and in vivo of six new Bnz analogues (3–8). They were designed by exploring the bioisosteric substitution between the amide group contained in Bnz and the 1,2,3-triazole ring. All the compounds were synthesized in good yields. With the exception of compound 7, the in vitro biological evaluation shows that all Bnz analogues were active against the amastigote form, whereas only compounds 3, 4, 5, and 8 were active against trypomastigote. Compounds 4 and 5 showed the most promising activities in vitro against the form of trypomastigote, being more active than Bnz. In vivo evaluation of compounds, 3–8 showed lower potency and higher toxicity than Bnz. Although the 1,2,3-triazole ring has been described in the literature as an amide bioisostere, its substitution here has reduced the activity of the compounds and made them more toxic. Thus, further molecular optimization could provide novel therapeutic agents for Chagas’ disease.
1H-1,2,3-Triazolyl-substituted 1,3,4-oxadiazole derivatives containing structural features of ibuprofen/naproxen: Their synthesis and antibacterial evaluation
Neeraja, Papigani,Srinivas, Suryapeta,Mukkanti, Khagga,Dubey, Pramod Kumar,Pal, Sarbani
, p. 5212 - 5217 (2016/10/30)
1H-1,2,3-Triazolyl-substituted 1,3,4-oxadiazole derivatives containing structural features of ibuprofen/naproxen were synthesized for the first time using a Cu catalyzed azide–alkyne cycloaddition (CuAAC) strategy. An optimized reaction condition was established for this purpose and twenty new compounds were synthesized using this methodology. Several of these compounds showed good to reasonable antibacterial activities when tested against three gram-positive and three gram-negative species. The compound 4m i.e. N-(2-chlorophenyl)-2-(4-((5-(1-(6-methoxynaphthalen-2-yl)ethyl)-1,3,4-oxadiazol-2-ylthio)methyl)-1H-1,2,3-triazol-1-yl)acetamide showed promising activities across both the species.
FORMULATIONS OF N-OXIDE PRODRUGS OF LOCAL ANESTHETICS FOR THE TREATMENT OF PULMONARY INFLAMMATION ASSOCIATED WITH ASTHMA, BROCHITIS, AND COPD
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Page/Page column 20; 21, (2008/06/13)
A prodrug of lidocaine and related local anesthetic composition or formulation for delivery by aerosolization is described. The formulation containing an efficacious amount of lidocaine N-oxide prodrug or local anesthetic N-oxide prodrug able to inhibit i
SUBSTITUTED ACETANILIDES AND BENZAMIDES FOR THE TREATMENT OF ASTHMA AND PULMONARY INFLAMMATION
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Page/Page column 48, (2008/06/13)
Substituted acetanilide or benzamide compositions or formulations for delivery by aerosolization are described. The formulation contains an efficacious amount of acetanilide or benzamide compound able to inhibit inflammation in asthmatic lungs. Compounds of the invention are formulated in 5 ml solution of a quarter normal saline having pH between 5.0 and 7.0. The method for treatment of respiratory tract inflammation by a formulation delivered as an aerosol having mass medium average diameter predominantly between 1 to 5 μ, produced by nebulization or dry powder inhaler.
