Investigating biological activity spectrum for novel styrylquinazoline analogues.
Josef Jampilek,Robert Musiol,Jacek Finster,Matus Pesko,James Carroll,Katarina Kralova,Marcela Vejsova,Jim O'Mahony,Aidan Coffey,Jiri Dohnal,Jaroslaw Polanski +10 more
TLDR
The structure-activity relationships (SAR) between the chemical structure and biological effects of the synthesized compounds are described and the relationships between the RP-HPLC retention parameter logK (the logarithm of capacity factor K) and logP data calculated by available programs are illustrated.Abstract:
In this study, series of ring-substituted 2-styrylquinazolin-4(3H)-one and 4-chloro-2-styrylquinazoline derivatives were prepared. The syntheses of the discussed compounds are presented. The compounds were analyzed by RP-HPLC to determine lipophilicity. They were tested for their inhibitory activity on photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts. Primary in vitro screening of the synthesized compounds was also performed against four mycobacterial strains and against eight fungal strains. Several compounds showed biological activity comparable with or higher than that of the standard isoniazid. It was found that the electronic properties of the R substituent, and not the total lipophilicity of the compound, were decisive for the photosynthesis-inhibiting activity of tested compounds.read more
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Recent advances in the synthesis of indole and quinoline derivatives through cascade reactions.
TL;DR: In this Focus Review, some of the most representative and interesting recent reports on the synthesis of indoles and quinolines through cascade reactions are discussed.
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Quinoline-based antifungals.
TL;DR: This current review is focused on the recent findings in the design of quinoline based antifungal agents, as 8-hydroxyquinoline and its metal complexes have been well known as antIfungals for years.
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Recent advances in research of natural and synthetic bioactive quinolines
Po Yee Chung,Zhaoxiang Bian,Ho Yuen Pun,Dessy Chan,Albert S. C. Chan,Chung Hin Chui,Johnny Cheuk On Tang,Kim Hung Lam +7 more
TL;DR: This review covers four main aspects, namely bioactive quinoline alkaloids, the biological activity and mechanism of action of quin Caroline-based compounds as well as various quinolines syntheses.
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Recent advances in the pharmacological diversification of quinazoline/quinazolinone hybrids
TL;DR: The present review summarizes the advances in lead compounds of quinazoline hybrids and their related heterocycles in medicinal chemistry and helps to intensify the drug development process by providing an understanding of the potential role of these hybridized pharmacophoric features in exhibiting various pharmacological activities.
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Povarov-type reaction using methyl as new input: direct synthesis of substituted quinolines by I2-mediated formal [3 + 2 + 1] cycloaddition.
TL;DR: A self-sequenced iodination/Kornblum oxidation/Povarov/aromatization mechanism has been proposed as a possible reaction sequence to account for the results observed in this study.
References
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National Committee for Clinical Laboratory Standards.
TL;DR: Many members of the Academy of Pediatrics seem to be generally unaware of the fact that the Academy has participated for ten years in a very interesting and valuable organization, the National Committee for Clinical Laboratory Standards (NCCLS).
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The Spectral Determination of Chlorophylls a and b, as well as Total Carotenoids, Using Various Solvents with Spectrophotometers of Different Resolution*
TL;DR: In this paper, specific absorption coefficients for individual carotenoids and chlorophylls a and b, as well as the E 1% 1cm values for combined carotensoids, have been (re)estimated using 6 solvents (80 % acetone, chloroform, diethyl ether, dimethyl formamide and methanol) using two different types of spectrophotometer (0.1-0.5 nm and 1-4 nm band pass resolution).
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A diarylquinoline drug active on the ATP synthase of Mycobacterium tuberculosis.
Koen Andries,Peter Verhasselt,Jerome Guillemont,Hinrich W. H. Göhlmann,Jean-Marc Neefs,Hans Winkler,Jef Van Gestel,Philip Timmerman,Min Zhu,Ennis Lee,Peter Williams,Didier de Chaffoy,Emma Huitric,Sven Hoffner,Emmanuelle Cambau,Chantal Truffot-Pernot,Nacer Lounis,Vincent Jarlier +17 more
TL;DR: A diarylquinoline, R207910, is identified that potently inhibits both drug-sensitive and drug-resistant Mycobacterium tuberculosis in vitro and mutants selected in vitro suggest that the drug targets the proton pump of adenosine triphosphate (ATP) synthase.
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Physicochemical Profiling (Solubility, Permeability and Charge State)
TL;DR: This review will consider recent developments in physicochemical profiling used to identify candidate molecules with physical properties related to good oral absorption and focus on the emerging instrumental methods for the measurement of the physicochemical parameters Pe, S, pKa, R, log P, and log D (and their pH-profiles).
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Relationship between inhibitor binding by chloroplasts and inhibition of photosynthetic electron transport.
W. Tischer,H. Strotmann +1 more
TL;DR: The results suggest that triazines, triazinones, pyridazinone derivatives, biscarbamates and phenylureas interfere with the same electron carrier of the photosynthetic electron transport chain, according to the same molecular mechanism.