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Your search keyword '"Dias, Rafael M."' showing total 27 results
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27 results on '"Dias, Rafael M."'

26. Quinolines derivatives as novel sunscreening agents.

Author

Polonini HC, Dias RM, Souza IO, Gonçalves KM, Gomes TB, Raposo NR, and da Silva AD

Subjects
Chemistry, Pharmaceutical, Molecular Structure, Quinolines chemistry, Spectrophotometry, Sunscreening Agents chemistry, Quinolines chemical synthesis, Sunscreening Agents chemical synthesis
Abstract

Currently, the research and development of sunscreens play an important role on the synthesis of actives that are stable in various kinds of formulations-in addition to their efficiency and broad spectrum of protection against ultraviolet radiation. Our objective here was to synthesize new sunscreening chemical agents using quinoline as a base molecule. Twelve quinoline derivatives were synthesized, four of them novel molecules, and their photoprotective activity was determined in vitro using diffuse transmittance spectrophotometry. We determined their SPF, UVAPF, UVA/UVB ratio, critical wavelength and Boots Star Rating. The quinolines derivatives presented a varied profile of photoprotection, their SPF ranging from 2 to 11 and their UVAPF from 2 to 7. In terms of the critical wavelength, all molecules were considered of broad-spectrum by different classifications. Regarding the Boots Star Rating, one compound received no rating, seven of them received a three stars rating, three received a four stars rating and three were given a five stars rating. The molecules showed in the present work have a wide range of possibilities for creating new sunscreen products, once they have good SPF or UVAPF for single molecules, and they also possess other different qualities that can act synergistically., (Copyright © 2013 Elsevier Ltd. All rights reserved.)

Published
2013
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27. Synthesis, cytotoxicity, antibacterial and antileishmanial activities of imidazolidine and hexahydropyrimidine derivatives.

Author

de Carvalho GS, Dias RM, Pavan FR, Leite CQ, Silva VL, Diniz CG, de Paula DT, Coimbra ES, Retailleau P, and da Silva AD

Subjects
Animals, Anti-Bacterial Agents chemistry, Cells, Cultured, Crystallography, X-Ray, Humans, Mice, Microbial Viability drug effects, Models, Molecular, Molecular Structure, Mycobacterium tuberculosis drug effects, Anti-Bacterial Agents chemical synthesis, Anti-Bacterial Agents pharmacology, Antiparasitic Agents chemical synthesis, Antiparasitic Agents chemistry, Antiparasitic Agents pharmacology, Bacteria drug effects, Imidazolidines chemical synthesis, Imidazolidines chemistry, Imidazolidines pharmacology, Leishmania drug effects, Pyrimidines chemical synthesis, Pyrimidines chemistry, Pyrimidines pharmacology
Abstract

This paper describes the synthesis and in vitro biological activities of imidazolidine and hexahydropyrimidine derivatives against bacteria (Escherichia coli, Staphylococcus aureus and Mycobacterium tuberculosis) and Leishmania protozoa. Out of sixteen heterocyclic derivatives tested, none were cytotoxic against mammalian cells. The compounds showed significant bacterial effects and leishmanicidal activity. Compounds 4a and 4c were active against S. aureus and E. coli, respectively. Compounds 3a-3f, 4h and 4i presented promising results against M. tuberculosis, with MIC values ranging from 12.5 to 25.0 μg/mL, comparable to the "first and second line" drugs used to treat tuberculosis. Compounds 4a, 4c and 4e were active against L major. Three of them were structurally characterized by single-crystal X-ray diffraction.

Published
2013
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