Maria Cristina S. Lourenço

Fundação Oswaldo Cruz

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M.V.N. De Souza

Fundação Oswaldo Cruz

J.L. Wardell

University of Aberdeen

Carlos R. Kaiser

Universidade Federal do Rio de Janeiro

Ana Esteves

Hospital de São Bernardo

Boletim Da

Sociedade Portuguesa de Cardiologia

Paulo André

Instituto de Telecomunicações

Hélder Gomes

Polytechnic Institute of Bragança

Santos Estatuto

Sociedade Portuguesa de Cardiologia

Bruno Amaral Machado

University Center of Brasília

Augusto Tomé

Sociedade Portuguesa de Cardiologia

Cooperative Institutions

Fundação Oswaldo Cruz

277

Universidade Federal do Rio de Janeiro

198

Instituto Evandro Chagas

Universidade Federal Fluminense

Universidade do Estado do Rio de Janeiro

Universidade Federal de Juiz de Fora

Universidade Federal de Minas Gerais

Ministério da Saúde

Universidade de São Paulo

Faculdades Oswaldo Cruz

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Morbidity and survival in advanced AIDS in Rio de Janeiro, Brazil

Revista do Instituto de Medicina Tropical de São Paulo (2002)

Angela Jourdan Gadelha Náurea Accácio Regina Lana Braga Costa Maria Clara Gutierrez Galhardo Maria Regina Cotrim

Opportunistic diseases (OD) are the most common cause of death in AIDS patients. To access the incidence of OD and survival in advanced immunodeficiency, we included 79 patients with AIDS treated at Hospital Evandro Chagas (FIOCRUZ) from September 1997 to December 1999 with at least one CD4 count

10.1590/s0036-46652002000400001

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Citations (31)

Synthesis and in vitro antimycobacterial activity of N’- benzylidene-2-oxo-2H-chromene-3-carbohydrazides derivatives

DOAJ (DOAJ: Directory of Open Access Journals) (2010)

Sílvia Helena Cardoso M.V.N. De Souza Milena B. Barreto Maria Cristina S. Lourenço Felipe R. C. Vicente

Antimycobacterial

10.17807/orbital.v2i1.159

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Citations (0)

The activity of flavones and oleanolic acid from Lippia lacunosa against susceptible and resistant Mycobacterium tuberculosis strains

Revista Brasileira de Farmacognosia (2011)

Aline Castellar Tatiane S. Coelho Pedro E. A. Silva Daniela Fernandes Ramos Maria Cristina S. Lourenço

Tuberculosis (TB), caused by Mycobacterium tuberculosis, is the world's number one killer among infectious diseases. The search for new naturalproducts that can act as drugs against TB has received increased attention duringthe last years. In this work we describe the isolation and identification of the active antimycobacterial principles of the dichloromethane extract from Lippia lacunosa Mart. & Schauer, Verbenaceae. Compounds were evaluated for their in vitro activity against Mycobacterium tuberculosis (susceptible and rifampicin resistantstrain) using a redox bioassay. From the dichloromethane extract of L. lacunosa leaves, seven methoxy-flavones named cirsimaritin (1), eupatilin (2), eupatorin (3), salvigenin (4), 3'-O-methyl-eupatorin (5), 3',7-dimethoxy-5,6,4'- trihydroxyflavone (6), and 7'-O-methylapigenin (7), and one triterpene, named oleanolic acid (8), were isolated. All compounds were found to display antimycobacterial activity against susceptible strain, with MIC ranging from 25 to 200 µg/mL. None of them was active against rifampicin resistant strain. This is the first report in the antimycobacterial activity of 6-substituted flavones, as well as the first report of the occurrence of these substances in L. lacunosa.

Antimycobacterial

Flavones

Lippia

10.1590/s0102-695x2011005000076

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Citations (21)

Synthesis and Antitubercular Activity of Heteroaromatic Isonicotinoyl and 7-Chloro-4-Quinolinyl Hydrazone Derivatives

The Scientific World JOURNAL (2010)

Marcelle de Lima Ferreira Raoni S. B. Gonçalves Laura Nogueira de Faria Cardoso Carlos R. Kaiser André Luis Peixoto Candéa

Two series of N’ (E)-heteroaromatic-isonicotinohydrazide derivatives (3a-f and 4a-b) and 1-(7-chloroquinolin-4-yl)-2-[(heteroaromatic)methylene]hydrazone derivatives (5a-f and 6a-b) have been synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H 37 Rv. Several compounds were noncytotoxic and exhibited significant minimum inhibitory concentration (MIC) activity (3.12, 2.50, 1.25, or 0.60 μg/mL), which can be compared to that of the first-line drugs ethambutol (3.12 μg/mL) and rifampicin (2.0 μg/ml). These results can be considered an important starting point for the rational design of new leads for anti-TB compounds.

Hydrazone

Methylene

10.1100/tsw.2010.124

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Citations (30)

Erratum

Dermatology (2005)

C.E.M. Griffiths M. Lebwohl G.G. Krueger Ichiro Katayama Kiyoshi Nishioka

10.1159/000088815

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Citations (0)

Synthesis and evaluation of copper(II) complexes with isoniazid-derived hydrazones as anticancer and antitubercular agents

BioMetals (2016)

Gisele S. S. Firmino M.V.N. De Souza Cláudia Pessoa Maria Cristina S. Lourenço Jackson A. L. C. Resende

Hydrazone

IC50

10.1007/s10534-016-9968-7

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Citations (34)

Isoniazid Monoresistance and Antituberculosis Treatment Outcome in Persons With Pulmonary Tuberculosis in Brazil

Open Forum Infectious Diseases (2024)

Mariana Araújo‐Pereira María B. Arriaga Anna Cristina Calçada Carvalho Renata Spener-Gomes Carolina Arana Stanis Schmaltz

The high burden of drug-resistant tuberculosis (TB) is a problem to achieve the goals of the End TB Strategy by 2035. Whether isoniazid monoresistance (Hr) affects anti-TB treatment (ATT) outcomes remains unknown in high-burden countries.

10.1093/ofid/ofad691

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Citations (3)

Synthesis and Antitubercular Evaluation of New Bis-1,2,3-Triazoles Derived from D-Mannitol

Journal of Carbohydrate Chemistry (2010)

Marcelle de Lima Ferreira M.V.N. De Souza J.L. Wardell J.L. Wardell T.R.A. Vasconcelos

Five new bis-1,2,3-triazole derivatives from D-mannitol, namely 2,3,4,5-tetra-O-acetyl-1,6-dideoxy-1,6-bis-(4-substituted-1H-1,2,3-triazol-1-yl)-D-mannitol (4), have been synthesized from 2,3,4,5-tetra-O-acetyl-1,6-diazido-1,6-dideoxy-D-mannitol (3) and alkynes, employing copper (I)-catalyzed azide-alkyne cycloaddition (CuAAC) methodology. Evaluation of their in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv using the Alamar Blue susceptibility test indicated poor activities. However, this study has provided information about the SAR of D-mannitol derivatives in the search for new anti-TB drugs based on this carbohydrate.

Triazole

D-mannitol

10.1080/07328303.2010.511749

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Citations (12)

Synthesis and Antibacterial Activity of Mefloquine-Based Analogs Against Sensitive and Resistant Mycobacterium tuberculosis Strains

Current Topics in Medicinal Chemistry (2019)

Adriele da Silva Araújo Adriana Marques Moraes Maria Cristina S. Lourenço Cláudia Pessoa Emerson T. da Silva

Background and Introduction: Mefloquine, a drug used to prevent and treat malaria is described possessing activity against the Mycobacterium tuberculosis (Mtb) as well as against multidrugresistant tuberculosis (MDR) and other types of bacteria. Despite their importance, few compounds based on the Mefloquine nucleus have been synthesized and evaluated against TB. Materials and Methods: For the synthesis of all the compounds based on the Mefloquine nucleus we used a synthetic route which utilized the key derivative 4-methoxy-2,8-bis(trifluoromethyl)quinoline 2 as starting material. The compounds 3 (a-c), 4 (a-b) were synthesized after one step by reaction of 2 with appropriate amines substituted. The chloro derivatives 5 and 6 were obtained from compounds 4b and 4a by treatment with SOCl2 in CH2Cl2 at reflux in 75 and 80% yield, respectively. The analogue 6 was converted to 7 after treatment with ethanolamine under heating at 90oC in 64% yield and to the azido derivative 8 in 56% after reaction with sodium azide in MeOH at reflux for 2 h. The analogue 9 was obtained after reaction of 5 with ethanolamine at 90oC for 1 h in 90% yield. All the new compounds were identified by detailed spectral data, including 1H NMR, 13C NMR and high resolution mass spectra. All the compound were evaluated for their in vitro antibacterial activity against sensitive Mycobacterium tuberculosis ATCC 27294, using the microplate Alamar Blue assay (MABA). The more active compounds 3c, 7, and 9 were also evaluated against resistant strain SR 2571/0215 (resistant to Rifampicin and Isoniazid) by above method. All compounds were tested against three cancer cell lines: SF-295 (glioblastoma), HCT-116 (colon) and PC-3 (prostate) using the MTT assay. Results: All the planned ten compounds were synthetically obtained in good global yield, displaying activity against sensitive Mycobacterium tuberculosis in vitro, with exception of one, with MIC values between 37.2 and 154.8 µM. The compounds 3c (37.2 µM), 7 (68.1 µM) and 9 (65.6 µM) showed the highest activity in this series with MIC values similar when compare to the standard Mefloquine (30 – 60 µM), being 3c the most potent. The more active compounds 3c, 7, and 9 were also evaluated against resistant strain, displaying MIC of 37.2, 136.2 and 65.6 µM, respectively. All compounds were tested against three cancer cell lines and showed low cytotoxicity. Conclusion: All synthesized compounds, with the exception of 5, exhibited activity against the Mtb. Compound 3c was the most potent against resistant and sensitive Mtb in this series, with MIC value of 37.2 µM. All compounds showed low cytotoxicity. These findings could be considered a good model to develop possible lead compounds in the fight against TB based on Mefloquine nucleus.

Antimycobacterial

10.2174/1568026619666190304124952

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Citations (8)

Synthesis and Anti-bacterial Activity Evaluation against Mycobacterium tuberculosis of New Quinoline Derivatives Coupled with the Camphor Nucleus

Letters in Organic Chemistry (2023)

Gabriel Fernandes de Andrade Emerson T. da Silva Maria Cristina S. Lourenço J.L. Wardell J.L. Wardell

Abstract: Tuberculosis is a serious infectious disease caused by Mycobacterium tuberculosis (Mtb), also known as Koch’s bacillus. The involvement of latent forms and resistant strains has aggravated the situation, making the disease a serious public health problem. : The objective of the study was to synthesize and evaluate ten new compounds containing camphor nucleus coupled to quinolinic derivatives as probable inhibitors of sensitive and resistant strains of Mtb growth. : The synthesis of the final compounds, 3a-e and 4a-e, was based on the use of intermediates previously obtained, in which the coupling of the camphor nucleus to quinoline derivatives was carried out via a convergent route, which resulted in good yields (50-80%). All the final compounds were fully characterized, and the 3-dimensional molecular structure of compound 4c was determined. The antimycobacterial activities of all compounds against Mtb strains were evaluated and the cytotoxicity test was conducted using the in vitro microplate procedure with broth microdilution assay (MTT). : Compound 3e was the most active against sensitive and resistant strains, with a minimal inhibitory concentration (MIC) of 9.5 μM similar to ethambutol, a first-line drug used against the tuberculosis. The most active compound 3e was selected for the potential activity against Vero cells and it displayed no cytotoxicity at a concentration near the MIC value. : The final compounds were obtained in good yields, with derivative 3e being the most promising with high activity and low cytotoxicity. Such findings open new perspectives for drug development based on the incorporation of camphor nucleus in selected compounds.

Antimycobacterial

Camphor

Broth microdilution

Quinoline

Borneol

MTT assay

10.2174/1570178620666230818092746

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Citations (1)