Synthesis and antimalarial evaluation of some 4-quinazolinone derivatives based on febrifugine

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Synthesis and antimalarial activity of febrifugine derivatives.

The regioisomers (2a,b) of the piperidine ring of febrifugine (1a) and isofebrifugine (1b) were synthesized from 4-allyl-3-piperidone (5). Reduction of 5 afforded a mixture of the trans and cis alcohols (6a,b) without diastereoselectivity; this result differentiated it from the reduction of 2-allyl-3-piperidone (14). The antimalarial activity of 2a,b and related compounds was tested.

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Synthesis of some new tricyclic 4(3H)-quinazolinone derivatives

Quinazolinones are interesting molecules with a wide range of biological activities. We prepared a number of quinazolinone derivatives by the condensation of 5-bromo- or 5-nitro-substituted anthranilic acids with chloro-acyl chlorides. Anthranilic acid derivatives were treated with either 3-chloro-propionyl chloride or 4-chloro-butyryl chloride to yield the corresponding N-acyl-anthranilic acid...

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Synthesis of some new 2,3-disubstituted-4(3H)quinazolinone derivatives

Quinazolinones are interesting materials because of their valuable biological effects. In this study some new 2,3-disubstituted-4(3H)quinqzolinone derivatives were synthesized from anthranilic acid in six steps by introducing a new chiral center to the aliphatic side chain of the quinazolinone. In the last step, a single acylation on the hydrazine moiety afforded final compounds. The structures...

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Synthesis and antileishmanial evaluation of some 2,3-disubstituted-4(3H)-quinazolinone derivatives

BACKGROUND Leishmaniasis is a neglected tropical parasitic diseases affecting millions of people around the globe. Quinazolines are a group of compounds with diverse pharmacological activities. Owing to their promising antileishmanial activities, some 3-aryl-2-(substitutedstyryl)-4(3H)-quinazolinones were synthesized in good yields (65.2% to 86.4%). RESULTS The target compounds were synthesiz...

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Synthesis and cytotoxicity evaluation of some new 6-nitro derivatives of thiazole-containing 4-(3H)-quinazolinone

Quinazolinones are a group of fused heterocyclic compounds which have valuable biological properties including cytotoxic, antibacterial and antifungal activities. Thiazole group-containing compounds have been also reported to have a wide range of biological activities such as antitumor, anti-inflammatory, analgesic and antibacterial effects. Due to valuable cytotoxic effects of both thiazole gr...

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ژورنال

عنوان ژورنال: Journal of Advanced Pharmaceutical Technology & Research

سال: 2010

ISSN: 0110-5558

DOI: 10.4103/0110-5558.76439