4-Arylamino-6-nitroquinazolines: Synthesis and their activities against neglected disease leishmaniasis

Aryl Quinazolinone Derivatives as Novel Therapeutic Agents against Brain-Eating Amoebae

“…Quinazolinones have previously been shown to demonstrate a wide spectrum of biological properties . Quinazolinones have been shown to act using various mechanisms, including inhibition of deoxyribonucleic acid (DNA) synthesis and inhibition of cell wall synthesis in bacteria, while inducing apoptosis, inhibition of DNA repair and attachment to DNA in cancer cells. − Therefore, we hypothesized that these compound classes may possess antiamoebic activities and tested them against N. fowleri and B. mandrillaris for their amoebicidal properties, amoebistatic properties and their ability to inhibit amoebae-mediated host cell damage.…”

“…Quinazolinones and their derivatives are among one of the most important heterocycles in medicinal chemistry as they possess a wide spectrum of biological properties . It has been reported that quinazolinones demonstrate antifungal activities against organisms such as Aspergillus niger , Candida albicans , and Aspergillus clavatus . − Moreover, quinazolinones also possess antibacterial activity against several bacteria, including Bacillus cereus , Staphylococcus aureus , Bacillus subtilis , Listeria monocytogenes , Klebsiella pneumoniae , Escherichia coli , Enterococcus faecalis , Pseudomonas aeruginosa , and Salmonella typhimurium . ,− Furthermore, the anticancer properties of quinazolinones have been evaluated, and it was reported that the compounds exhibit potent anticancer activity at low concentrations. − Quinazolinones also exhibit noteworthy effects against viruses, such as vaccinia virus, Pox viruses, influenza A virus, and human immunodeficiency virus. ,, Several quinazoline and quinazolinone derivatives have also been reported to exhibit antiparasitic activities such as antileishmanial, antiplasmodial, antiacanthamoebic, antitrypanosoma, and antitoxoplasma activities . However, despite their broad range of biological properties, quinazolinones have not been tested against N. fowleri and B. mandrillaris .…”

“…17−19 Quinazolinones also exhibit noteworthy effects against viruses, such as vaccinia virus, Pox viruses, influenza A virus, and human immunodeficiency virus. 16,20,21 Several quinazoline and quinazolinone derivatives have also been reported to exhibit antiparasitic activities such as antileishmanial, 22 antiplasmodial, 23 antiacanthamoebic, 24 antitrypanosoma, 25 and antitoxoplasma activities. 26 However, despite their broad range of biological properties, quinazolinones have not been tested against N. fowleri and B. mandrillaris.…”

Recent Advances in the Discovery of Novel Antiprotozoal Agents

“…Based on their results, compounds 33a and 33b were reported as the most potent antileishmanial agents, with IC 50 values of 5.12 and 3.56 µM respectively. Among the 4-arylamino-6-nitroquinazolines synthesized by Saad et al [107], compounds 34a and 34b were found to be the most potent inhibitors of L. major promastigotes (IC 50 values of 1.87 and 4.37 µM, respectively) compared to the standard drug, pentamidine (IC 50 = 5.09 µM). Gopinath et al [108] developed a series of substituted quinoline analogs and assessed their antileishmanial activities.…”

Identification of 2-arylquinazolines with alkyl-polyamine motifs as potent antileishmanial agents: synthesis and biological evaluation studies

“…15 The antileishmanial potential of a broad range of 4-arylamino-6-nitroquinazoline compounds was explored by Saad et al The compound with 4-methylsulfanyl substitution ( 6 ) was found to be significantly cytotoxic against L. major and more potent than pentamidine. 16 In an investigation of the activity of quinazoline-2,4,6-triamines against Leishmania mexicana , the N 6 -(ferrocenmethyl) derivative ( 7 ) showed significant activity against promastigotes and intracellular amastigotes. 17 Licochalcone A ( 8 ), a natural product isolated from the roots of Chinese licorice, inhibits both L. major and L. donovani .…”