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Synthesis, Characterization and Complex Evaluation of Antibacterial Activity an...
Slavchev, Ivaylo M.; Mitrev, Yavor; Shivachev, Boris; Valcheva, Violeta; Dogonadze, Marine; Solovieva, Natalia; Vyazovaya, Anna; Mokrousov, IgorThe synthesis of 20 arylidenecamphors and 15 pyrimidines with camphane skeleton is described in the current report. A modified method for preparation of sterically hindered 2-aminopyrimidines in two steps was demonstrated. The evaluation of their in vitro activity against Mycobacterium tuberculosis H37Rv showed different MIC values (up to 0.91 μM for ketone 39). Compound 35 demonstrated moderate (8.23 μM), but ...
Quinolin-(1H)-imines as a new chemotype against leishmaniasis: biological evalu...
Alves, Ana G. Gomes; Duarte, Margarida; Cruz, Tânia; Castro, Helena; Lopes, Francisca; Moreira, Rui; Ressurreição, Ana S.; Tomás, Ana M.Leishmaniasis is one of the most challenging neglected tropical diseases and remains a global threat to public health. Currently available therapies for leishmaniases present significant drawbacks and are rendered increasingly inefficient due to parasite resistance, urging the need for more effective, safer, and cheaper drugs. In our efforts to identify novel chemical scaffolds for the development of antileishm...
O contributo para a estratégia de internacionalização e branding, da empresa E-goi
Lopes, FranciscaO presente relatório tem por base a descrição de 460 horas de estágio curricular, do Mestrado de Direção Comercial e Marketing, realizado na empresa E-goi, decorrido no período entre dia 17 de setembro a 20 de dezembro de 2019, tendo como supervisora a Professora Doutora Cristina Mocetão. O relatório acadêmico tem como finalidade a contribuição para a melhoria do desempenho comercial da equipa Sales e Marketing...
Novel and Modified Neutrophil Elastase Inhibitor Loaded in Topical Formulations...
Nunes, Andreia; Marto, Joana; Gonçalves, Lídia; Simões, Sandra; Félix, Rita; Ascenso, Andreia; Lopes, Francisca; Ribeiro, HelenaHuman neutrophil elastase (HNE) is a serine protease that degrades matrix proteins. An excess of HNE may trigger several pathological conditions, such as psoriasis. In this work, we aimed to synthesize, characterize and formulate new HNE inhibitors with a 4-oxo-β-lactam scaffold with less toxicity, as well as therapeutic index in a psoriasis context. HNE inhibitors with 4-oxo-β-lactam scaffolds were synthesized...
Bis{(E)-3-[(diethylmethylammonio)methyl]-N-[3-(N,N-dimethylsulfamoyl)-1-methylp...
Rodrigues, Tiago; Moreira, Rui; Dacunha-Marinho, Bruno; Lopes, FranciscaThe title compound, 2C(21)H(34)N(4)O(3)S(2+)center dot 4I(-)center dot 5H(2)O, was prepared exclusively as the E isomer by methylation of the corresponding N-phenylpyridin-4-amine. There are two symmetry-independent molecules in the asymmetric unit with no significant differences in bond lengths and angles. The aromatic rings are not coplanar with the pyridin-4-imine groups, as indicated by the C-N-C-C torsion ...
Design, synthesis and structure-activity relationships of (1H-pyridin-4-ylidene...
Rodrigues, Tiago; Guedes, Rita C.; dos Santos, Daniel J. V. A.; Carrasco, Marta; Gut, Jiri; Rosenthal, Philip J.; Moreira, Rui; Lopes, Francisca(1H-Pyridin-4-ylidene)amines containing lipophilic side chains at the imine nitrogen atom were prepared as potential clopidol isosteres in the development of antimalarials. Their antiplasmodial activity was evaluated in vitro against the Plasmodium falciparum W2 (chloroquine-resistant) and FCR3 (atovaquone-resistant) strains. The most active of these derivatives, 4m, had an IC50 of 1 mu M against W2 and 3 mu M ...
Artemisinin-dipeptidyl vinyl sulfone hybrid molecules
Capela, Rita; Oliveira, Rudi; Goncalves, Lidia M.; Domingos, Ana; Gut, Jiri; Rosenthal, Philip J.; Lopes, Francisca; Moreira, RuiA series of artemisinin-vinyl sulfone hybrid molecules with the potential to act in the parasite food vacuole via endoperoxide activation and falcipain inhibition was synthesized and screened for antiplasmodial activity and falcipain-2 inhibition. All conjugates were active against the Plasmodium falciparum W2 strain in the low nanomolar range and those containing the Leu-hPhe core inhibited falcipain-2 in low ...
Unanticipated acyloxymethylation of sumatriptan indole nitrogen atom and its im...
Rodrigues, Tiago; Moreira, Rui; Guedes, Rita C.; Iley, Jim; Lopes, FranciscaSumatriptan is a potent and selective 5-HT1B and 5-HT1D agonist used in the symptomatic treatment of migraine; it shows poor oral bioavailability ascribed, in part, to its low lipophilicity. In an attempt to develop acyloxymethyl prodrugs of sumatriptan suitable for oral administration, we carried out the reaction of sumatriptan with chloromethyl esters. To our surprise, acyloxymethylation occurred preferential...
Reactivity of imidazolidin-4-one derivatives of primaquine
Chambel, Paula; Capela, Rita; Lopes, Francisca; Iley, Jim; Morais, Jose; Gouveia, Luis; Gomes, Jose R. B.; Gomes, Paula; Moreira, RuiIn contrast to peptide-based imidazolidin-4-ones, those synthesized from N-(alpha-aminoacyl) derivatives of the antimalarial drug, primaquine and ketones are unexpectedly stable in pH 7.4 at 37 degrees C. The kinetics of hydrolysis of primaquine-based imidazolidin-4-ones were investigated in the pH range 0.3-13.5 at 60 degrees C. The hydrolysis to the parent alpha-aminoacylprimaquine is characterized by sigmoid...