Aminoacids in the Synthesis of Heterocyclic Systems: The Synthesis of Triazinoquinazolinones, Triazepinoquinazolinones and Triazocinoquinazolinones of Potential Biological Interest

El‐Sharief, A. M. Sh.; Ammar, Yousry A.; Zahran, M. A.; Ali, Asma; El‐Gaby, Mohamed S. A.

doi:10.3390/60300267

Cited by 32 publications

(5 citation statements)

References 5 publications

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“…One of the most repeatedly encountered heterocycles in medicinal chemistry is quinazoline because of its broad range of pharmacological activities. As medicines, many of its derivatives display antifungal 10, antimicrobial 11, anti‐HIV, and anti‐tobacco mosaic virus (TMV) 12, 13, antitubercular 14, anticancer 15, anti‐inflammatory 16, anticonvulsant 17, antidepressant 18, hypolipidemic 19, antiulcer 20, analgesic 21, or immunotropic activities 22. They are also known to act as thymidylate synthase 23, poly(ADP‐ribose) polymerase (PARP) 24, and protein tyrosine kinase inhibitors 25.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Evaluation of Novel 4‐Substituted Styryl Quinazolines as Potential Antimicrobial Agents

Modh

Patel

Mahajan

et al. 2012

Archiv der Pharmazie

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In an attempt to afford possible antibacterial and anti-human immunodeficiency virus (HIV) agents, a series of 22 novel styryl quinazoline-based heterocyclic entities were designed and synthesized. Various substituted aryl urea and thiourea cores were incorporated at position 4 of quinazoline, followed by styrylation of position 2, aiming at an augmented biological potential. The synthesized compounds were well characterized through IR, (1) H NMR, (13) C NMR and elemental analyses. All compounds were screened for their in vitro anti-HIV activity against the HIV-1 (IIIB) and HIV-2 (ROD) strains. The antibacterial activity was also evaluated against various pathogenic Gram-positive and Gram-negative bacterial strains.

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Section: Introductionmentioning

confidence: 99%

Synthesis and Evaluation of Novel 4‐Substituted Styryl Quinazolines as Potential Antimicrobial Agents

Modh

Patel

Mahajan

et al. 2012

Archiv der Pharmazie

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“…3), which are used clinically as antibacterial agents, are chemically quinoline derivatives 10–12. Moreover, several quinazolines were reported to possess antimicrobial activity 13, 14 in addition to other quinazolines F (Fig. 3) derived from dimedone were found to have antibacterial activity 6.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of New Nonclassical Acridines, Quinolines, and Quinazolines Derived from Dimedone for Biological Evaluation

Sabbagh

Shabaan

Kadry

et al. 2010

Archiv der Pharmazie

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New nonclassical acridines, quinolines, and quinazolines were prepared starting from cyclic β-diketones, namely dimedone, through application of Hantzsch addition, Michael addition, and Mannich reactions, respectively. The antimicrobial activity revealed that decahydroacridin-1,8-dione 2e bearing a 3-nitrophenyl group and hexahydroquinoline 4e having a 2,4-dichlorophenyl moiety were the most active compounds against both Gram-positive and -negative bacteria based upon using the disc diffusion method. Cytotoxic activity studies for decahydroacridin-1,8-diones 2a-e against liver carcinoma cells (HepG(2)) using the MTT cell viability assay revealed that decahydroacridin-1,8-dione bearing a 4-methylphenyl moiety 2d showed a higher cytotoxic activity (IC(50) = 4.42 µg/mL) than the other derivatives.

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“…Quinoxaline derivatives are the subject of considerable interest from both academic and industrial perspective 1 . Among the various classes of nitrogen containing heterocyclic compounds, quinoxalines are important components of several pharmacologically active compounds 2 .…”

Section: Introductionmentioning

confidence: 99%

Synthesis of Some New Quinazolin-4(3h)-One Derivatives and Study of Their Some Antibacterial Activity

Salih

2008

JNUS

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In this work, 2-phenyl-4(3H)-3,1-benzoxazinone (1) was synthesized from benzoylation with simultaneous cyclization of anthranilic acid and benzoyl chloride. Compound 1 was treated with hydrazine hydrate to yield 3-amino-2-phenyl-4(3H)-quinazolinone (2). Reaction of compound 2 with aromatic aldehydes/ketones resulted Schiff bases 3-6. Furthermore, treated of compound 1 with thiosemicarbazide yield compound 7, which on reaction with chloroacetic acid in the presence of sodium acetate gave 3-[(4-oxo-1,3-thiazolidin-2-yliden)amino]-2-phenylquinazolin-4(3H)-one (8). On the other hand, 2-substitutedquinazolin-4(3H)-one (9-12) were also synthesized from the reaction of anthranilic acid with different substituted amides in acetic acid. All newly synthesized compounds were characterized using different methods of spectroscopy such as IR, 1 H-NMR and 13 C-NMR. The antibacterial activity of all of the synthesized compounds was also reported. All synthesized compounds have been found to be active against both Grampositive and Gram-negative bacteria but compounds 4 and 8 were the most active one.

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Aminoacids in the Synthesis of Heterocyclic Systems: The Synthesis of Triazinoquinazolinones, Triazepinoquinazolinones and Triazocinoquinazolinones of Potential Biological Interest

Abstract: A number of novel triazinoquinazolinones (5b,c and 8), triazepinoquinazolinones(5a, 6b, 7 and 9) and triazocinoquinazolinones (6a and 10) were obtained via nucleophilic interaction of 3-aminoquinazolinone derivatives 3 with different reagents.

Cited by 32 publications

References 5 publications

Synthesis and Evaluation of Novel 4‐Substituted Styryl Quinazolines as Potential Antimicrobial Agents

Synthesis and Evaluation of Novel 4‐Substituted Styryl Quinazolines as Potential Antimicrobial Agents

Synthesis of New Nonclassical Acridines, Quinolines, and Quinazolines Derived from Dimedone for Biological Evaluation

Synthesis of Some New Quinazolin-4(3h)-One Derivatives and Study of Their Some Antibacterial Activity

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