Fármacos utilizados no tratamento de hipercolesterolemia: uma análise histórica e químico-medicinal / Drugs used in the treatment of hypercholesterolemia: a historical and medicinal chemistry focused analysis

Nesse trabalho, são apresentados aspectos relacionados ao desenvolvimento das principais classes farmacológicas utilizadas no tratamento de hipercolesterolemia, explorando-se as características estruturais importantes a sua ação biológica

Synthesis, antileishmanial activity and QSAR studies of 2-chloro- N -arylacetamides

We describe herein the synthesis and evaluation of the antileishmanial activity against promastigote forms of Leishmania amazonensis and cytotoxicity to murine macrophages of a series of 2-chloro-N-arylacetamide derivatives. All compounds were active, except one (compound 3). Compound 5 presented the most promising results, showing good antileishmanial activity (CI50=5.39±0.67 µM) and moderate selectivity (SI=6.36), indicating that further development of this class is worthwhile. Preliminary QSAR studies, although not predictive, furnished some insights on the importance of electronic character of aryl substituent to biological activity, as well as an indirect influence of hydrophobicity on activity

A chloroacetamide derivative as a potent candidate for fusariosis treatment

Fusariosis has presented a significant increase in their incidence in the last years. This epidemiological panorama probably is due to the increasing profile of refractory susceptibility of Fusarium spp. to available drugs, especially in immunocompromised individuals. Thus, the development of new compounds with effectiveness on these organisms is a necessity. This study evaluated the antifungal potential of a chloroacetamide derivative (4-BFCA) against resistant Fusarium strains. As a result, the compound was effective against all strains (MIC range 12.5–50 μg/mL). The time kill assay demonstrated that 4-BFCA presents a concentration-dependent fungicidal action. Although its action mechanism has not yet been elucidated, it was possible to observe its efficacy through damages and alterations provoked along the hyphae of Fusarium spp. 4-BFCA maintained a high survival rate of Tenebrio molitor larvae, suggesting that it does not cause acute systemic toxicity on this host at the concentration evaluated. In addition, 4-BFCA was 83.33% effective in combating a fungal infection in vivo on the chorioallantoid membrane of embryonated eggs. Our results are very promising and arouse interest to investigate the action of 4-BFCA on Fusarium strains since it acts as a possible candidate for the development of new therapies for the treatment of fusariosis

Synthesis, antileishmanial activity and QSAR studies of 2-chloro- N -arylacetamides

ABSTRACT We describe herein the synthesis and evaluation of the antileishmanial activity against promastigote forms of Leishmania amazonensis and cytotoxicity to murine macrophages of a series of 2-chloro-N-arylacetamide derivatives. All compounds were active, except one (compound 3). Compound 5 presented the most promising results, showing good antileishmanial activity (CI50=5.39±0.67 µM) and moderate selectivity (SI=6.36), indicating that further development of this class is worthwhile. Preliminary QSAR studies, although not predictive, furnished some insights on the importance of electronic character of aryl substituent to biological activity, as well as an indirect influence of hydrophobicity on activity

In vitro activity of 1,3-bisaryloxypropanamines against Trypanosoma cruzi-infected L929 cultures.

Submitted by Nuzia Santos ([email protected]) on 2016-02-16T17:28:54Z No. of bitstreams: 1 In vitro activity of 1,3-bisaryloxypropanamines.pdf: 2773241 bytes, checksum: 63494cccab20510a6edf7eacf0a5087f (MD5)Approved for entry into archive by Nuzia Santos ([email protected]) on 2016-02-16T17:49:14Z (GMT) No. of bitstreams: 1 In vitro activity of 1,3-bisaryloxypropanamines.pdf: 2773241 bytes, checksum: 63494cccab20510a6edf7eacf0a5087f (MD5)Made available in DSpace on 2016-02-16T17:49:14Z (GMT). No. of bitstreams: 1 In vitro activity of 1,3-bisaryloxypropanamines.pdf: 2773241 bytes, checksum: 63494cccab20510a6edf7eacf0a5087f (MD5) Previous issue date: 2015Universidade Federal de Minas Gerais. Faculdade de Farmácia. Departamento de Produtos Farmacêuticos. Belo Horizonte, MG, BrasilFundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Laboratório de Parasitologia Celular e Molecular. Belo Horizonte, MG, BrasilFundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Laboratório de Parasitologia Celular e Molecular. Belo Horizonte, MG, BrasilFundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Laboratório de Parasitologia Celular e Molecular. Belo Horizonte, MG, Brasil/Universidade Federal de Santa Catarina. Departamento de Microbiologia, Imunologia e Parasitologia. Florianópolis, SC, BrasilUniversidade Federal de Minas Gerais. Faculdade de Farmácia. Departamento de Produtos Farmacêuticos. Belo Horizonte, MG, BrasilWe describe herein the antitrypanosomal activity of 20 novel 1,3-bis(aryloxy)propan-2-amine derivatives. Compounds 2, 4, 6, 12, 15, 16 and 19 were significantly active against amastigote and trypomastigote forms, with half maximal inhibitory concentrationvalues in the range of 6-18 µM. In the cytotoxicity tests against L929 cells, only compound 4 presented selectivity index value above 10, indicating low toxicity