The title molecule, C9H7ClN4OS, is almost planar, with an r.m.s. deviation of 0.034 (2) Å for the mean plane through all the non-H atoms. Intramolecular N—H⋯O and N—H⋯N hydrogen bonds form S(6) and S(5) ring motifs, respectively. In the crystal, molecules are assembled into inversion dimers through pairs of co-operative N—H⋯Cl interactions. These dimers are connected along the b axis by N—H⋯O and N—H⋯S hydrogen bonds, generating layers parallel to (103). The layers are further connected along the a axis into a three-dimensional network, through weak π–π stacking interactions [centroid–centroid distance = 3.849 (2) Å].
The continuous emergence of resistant Mycobacterium tuberculosis keeps tuberculosis (TB) treatment options still insufficient, and new therapeutic alternatives are urgently needed. Considering the antimycobacterial activity of phenazine derivatives previously reported by our research group, we aimed to explore possible applications to circumvent the resistance in M. tuberculosis. Firstly, we evaluated the antimicrobial activity of seven benzo[a]phenazine derivatives against eleven M. tuberculosis strains: ten resistant and one susceptible (H37Rv). Then, we determined the cytotoxicity of benzo[a]phenazine derivatives and investigated the possible mechanism of action of the most promising compound. Among them, compound 10 was the only one active against all strains evaluated, with a minimum inhibitory concentration between 18.3 and 146.5 µM. For some resistant strains, this compound showed antimicrobial activity higher than rifampicin and it was also active against MDR strains, indicating an absence of cross‐resistance with anti‐TB drugs. Also, 10 showed a pharmacological safety for further in vivo studies and its mechanism of action seems to be related to oxidative stress. Thus, our findings indicate that benzo[a]phenazine derivatives are promising scaffolds for the development of new anti‐TB drugs, mainly focusing on the treatment of resistant TB cases.
ResumoEstudos têm contribuído para a definição de importantes diretrizes acerca da conservação de documentos de arquivo e, em especial, a conservação preventiva, fomentando a discussão e a consolidação de políticas que busquem auxiliar na preservação dos acervos. Nessa perspectiva, a presente pesquisa, realizada em parceria entre o Instituto de Ciências Humanas e da Informação -curso de Arquivologia -, e a Escola de Química e Alimentos da Universidade Federal do Rio Grande, tem como objetivo avaliar possíveis ações de danos provocados pelo uso das folhas autoadesivas nos documentos textuais em suporte papel, visando contribuir com as discussões e estudos sobre a temática de conservação e preservação dos acervos. A metodologia para o desenvolvimento deste trabalho foi dividida em etapas que consistiram em: seleção da amostragem e pesquisa sobre o surgimento dos blocos autoadesivos, revisão do referencial teórico, análise dos dados coletados través da técnica de microscopia eletrônica de varredura e posterior divulgação dos resultados da pesquisa.
Palavras-chave:Autoadesivo. Conservação. Documentos textuais. Microscopia eletrônica de varredura. Papel.
Abstract
Studies have contributed to the definition of important guidelines on the file record keeping and in particular preventive conservation fostering discussion and the consolidation of policies that seek to assist in the preservation of collections. In this perspective the present research, which is a work in partnership between the Institute of Humanities and information -
Sporothrix spp. are the major dimorphic fungus associated with a type of subcutaneous mycosis, sporotrichosis. The limitation of antifungal availability and the past reports of in vitro resistance of Sporothrix spp. clinical isolates makes it important to search for new compounds with antifungal activities. In this study, we therefore evaluate the in vitro activities of complexes coordinated with Co(II) and cobalt chloride hexahydrate against clinical isolates of Sporothrix spp. Broth microdilution test was performed as per M38-A2 from CLSI (2008) in duplicate for 31 clinical isolates of Sporothrix spp. (27 S. brasiliensis e 04 S. schenckii stricto sensu). The antifungal activities of the complexes coordinated with Co(II) and cobalt chloride hexahydrate were detected at a concentration range of 32-128 µg/mL for all isolates. None of the compounds demonstrated any cytotoxicity (to macrophage cells) at the concentration of 200 µg/mL. The activity against Sporothrix spp. recorded in this study instigate the continuity of experimental studies with Co(II) to search for the mechanisms of antifungal action as well as to evaluate its interaction with the commercial antifungal drugs.
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