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Mechanism of Drug Resistance in Staphylococcus aureus and Future Drug Discovery
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2020
Felipe Wakasuqui, Ana Leticia Gori Lusa, Sven Falke, Christian Betzel, Carsten Wrenger
Even though natural products are main sources of antibiotics, chemical screening continues to be important and several heterocyclic scaffolds have been explored. Among them, quinazolinones have emerged as a privileged structure (Khan et al., 2016), possessing a wide range of biological properties with antibacterial, antifungal, anti-inflammatory, anticonvulsant, anticancer, anti-HIV, and analgesic activities (Dohle et al., 2018; Noolvi et al., 2011; El-Hashash et al., 2018; Abbas et al., 2018; Hrast et al., 2017; Yang et al., 2018; Abuelizz et al., 2018; Ighachane et al., 2017; Alaa et al., 2016; Dash et al., 2017; Dinari et al., 2018; Jain et al., 2018; Zhang et al., 2018). Utilization of the quinazolinone core for the synthesis of new antibacterial agents has recently gained importance. The 2-methyl quinazolinone 1 has been reposted with substantial antibacterial activity (Zhan et al., 2018), whereas the quinazolinone compounds 2 and 3 have antimicrobial properties (Saravanan et al., 2013 and Poudapally et al., 2017). The 2-styryl quinazolinones 4 are potent antimycobacterial agents (Jadhavar et al., 2016 and Kumar et al., 2015). And recently 4(3H)-quinazolinones 5 and related compounds have been reported as potent PBP1 and PBP2a inhibitors of MRSA, demonstrating promising in vivo activities (Bouley et al., 2015 and 2016). Further, a series of newly designed 1,2,3-triazole linked 4(3H)-quinazolinone derivatives have been synthesized. In summary, these compounds exhibit the potential to be further developed as narrow spectrum anti-staphylococcal leads with the potential to evade drug resistance.
Nickel(II) complex anchored on MCM-41, a reusable catalyst for the synthesis of benzimidazole and quinazolinone
Published in Journal of Coordination Chemistry, 2022
Udai P. Singh, Saurabh Sharma, Arti Malik
Nitrogen-containing heterocyclic compounds, viz., quinazolin-4(3H)-ones and benzimidazoles are found in many natural products and play important role in medicinal chemistry [1] due to their different biological activities like anticancer [2], antifungal [3], antihypertensive [4], antimalarial [5], antibacterial [6,7], etc. Benzimidazoles and their derivatives exhibit significant activity against viruses, including hepatitis C, HIV and herpes simplex virus (HSV-1) [8]. The benzimidazole system was also used as carbon skeletons for N-heterocyclic carbenes (NHCs); NHCs have been used as ligands [9–11] in many transition metal complexes. The quinazolinone derivatives also display biological activities such as antihistamine, antitumor, and antiinflammatory and used as ligands in the central nervous system, including CNS stimulant, analgesic, tranquilizer, and antianxiety [12–16]. Due to biological functions, the preparation of these heterocycles using a simple method is still in demand. In general, these compounds are prepared from condensation of 1,2-diaminoarenes, anthranilamide either with carboxylic acid derivative [17] or aldehyde [18] under oxidative conditions. A number of homogeneous and heterogeneous catalysts have been employed for catalyzing these reactions [19–23].
A Quinazolinone based fluorescent chemosensor for selective detection of Fe(III) in aqueous media: Applications to pharmaceutical and environmental analysis
Published in Inorganic and Nano-Metal Chemistry, 2018
Pravin R. Dongare, Anil H. Gore, Uttam R. Kondekar, Govind B. Kolekar, Balu D. Ajalkar
Quinazolinone derivatives which belong to N-containing heterocyclic compounds find potential applications in the field of pharmaceutical and pesticides due to their different biological properties[38–40] such as, antimalarial, anticancer, muscle relaxant, anticonvulsant, antibacterial and antifungal property. To the best of our knowledge, few quinazolinone derivatives have been reported as a fluorescent chemosensor for different metal ions such as Co2+, Cu2+, Hg2+, Fe3+[41–44] with good photostability and large emission intensity. Thus, keeping this point in mind herein we report a 2-(1,3-thiazol-2-yl)-2,3-dihydroquinazolin-4(1 H)-one as a highly selective and sensitive fluorescent chemosensor that recognizes Fe3+ in an aqueous solution. The sensing properties of 1 towards different metal ions are carried out in Ethanol: Water (3:7, v/v) and investigated in details through fluorescence, UV-Visible absorption spectra, FTIR studies and DFT calculations.
One-pot synthesis of novel fused mesoionic compounds: 1-substituted-5-thioxo-5,6-dihydro-[1,2,4]triazolo[1,5-c]quinazolin-1-ium-2-thiolates
Published in Journal of Sulfur Chemistry, 2020
Sergiy M. Kovalenko, Oleksandr G. Drushlyak, Illia O. Mariutsa
Quinazolin-4(3H)-one derivatives are in abundance among pharmacological active materials of natural or synthetic sources. The biological behavior of quinazolinones varies essentially with even minor modifications in their molecular structure [1] and provides diverse pharmacological properties. Depending on the position and nature of substituents, 4-oxoquinazolines exhibit different biological activities such as natural alkaloids [2], antioxidant [3], antimicrobial [1,3–7], antibacterial [8,9], antifungal [10,11], antihypertensive [12–14], anti-inflammatory [15–18], anticonvulsant [19,20], and anticancer [21–27]. Among the variety of quinazolinones, those bearing amino function at the 3 position of the quinazoline ring are of particular interest. So, the introduction at the 3 position, an arylideneamino substituent increases antibacterial action [9]. 3-N-sulfonamides [5] and 3-N-phosphorylated quinazolinones [6,7] seem to be promising antimicrobial agents. 3-N-amides possess anticonvulsant action [19]. On the other hand, 2-thioxoquinazolin-4(3H)-ones [24] and 2-alkylthioquinazolin-4(3H)-ones [26] show promising antitumor activity. Against this background, biological and chemical properties of the N-substituted-N'-(4-oxo-2-thioxo-1,4-dihydroquinazolin-3(2H)-yl)thioureas are insufficiently explored. However, these compounds have recently become interesting as inhibitors of myeloperoxidase and useful for the treatment of inflammatory conditions including neuroinflammatory diseases such as Parkinson’s and Alzheimer’s [28]. Therefore, the initial aim of our investigation is to develop the effective synthesis of (4-oxo-2-thioxo-1,4-dihydroquinazolin-3(2H)-yl)thioureas.