Researches and applications of nitroimidazole heterocycles in medicinal chemistry

Identification of Unique Quinazolone Thiazoles as Novel Structural Scaffolds for Potential Gram-Negative Bacterial Conquerors

“…Heteroaromatic thiazole, as a member of the current research mainstream azoles, gains wide appreciations and cultivations in drug design and development due to the character of abundant electrons, which empowers it to engage with functional targets for improving biological activity. − Naturally, thiazole provides enormous contributions to successful development of clinical antibiotics such as the third and fourth cephalosporins. , Consequently, to confront drug-resistant infections, recent numerous studies endeavored to incorporate it with the antibacterial nucleus like quinolone, , sulfanilamide, , and berberine , for discovery of novel antimicrobials, among which some availably perturbed essential cellular behavior of microorganisms, holding meaningful exploring potential. Moreover, our previous research revealed that quinazolone thiazoles delivered promising antibacterial effects and low bacterial resistance .…”

Azolylpyrimidinediols as Novel Structural Scaffolds of DNA-Groove Binders against Intractable Acinetobacter baumannii

“…General Procedures for the Synthesis of Chloromethylcoumarin (17) and Naphthalimides (20 and 21). Chloromethylcoumarin 17 was prepared in a good yield of 78.5% according to the synthetic methods reported in the literature.…”

“…The six-membered heterocyclic pyrimidine with two nitrogen atoms is widely present in a lot of biomolecules like DNA and clinical drugs such as antibacterial sulfonamides in which pyrimidine ring plays a positive role in exerting biological activities. − It is revealed that many antimicrobial pyrimidine derivatives could bind to DNA via weak interactions to block bacterial DNA replication and thus reduce the viability of microorganisms. − The incorporation of pyrimidines and versatile functional fragments has been extensively studied to discover new pyrimidine-based antimicrobial agents. − Especially, the pyrimidine-hybridized azoles like pyrazole and benzothiazole were reported to exhibit admirable antimicrobial efficacy. − It is well known that the aromatic heterocyclic azoles as drugs are exerting positive impact in treating a variety of diseases especially microbial infections; it has been found that the various biological effects are derived from the effective interactions via noncovalent bonds between the electron-rich aromatic azole ring and the biological targets. , Therein, imidazole as a significant moiety in endogenous biomolecules arouses great attention in antimicrobial medicinal chemistry. , Plenty of imidazole-based drugs like metronidazole, ornidazole, morinidazole, and so on, make great contribution to the treatment of clinical microbial infections. , Our previous work showed that the combination of imidazole and pyrimidines produced some potential multitargeting antibacterial molecules, , manifesting that such an incorporation was a promising strategy anticipated to the discovery of diverse antibacterial pyrimidine derivatives. In this content, imidazolylpyrimidinediols and their analogues as novel structural scaffolds were constructed for the first time, which might be a new lenitive for the abominable drug resistance.…”

“…14−16 It is well known that the aromatic heterocyclic azoles as drugs are exerting positive impact in treating a variety of diseases especially microbial infections; it has been found that the various biological effects are derived from the effective interactions via noncovalent bonds between the electron-rich aromatic azole ring and the biological targets. 17,18 Therein, imidazole as a significant moiety in endogenous biomolecules arouses great attention in antimicrobial medicinal chemistry. 19,20 Plenty of imidazole-based drugs like metronidazole, ornidazole, morinidazole, and so on, make great contribution to the treatment of clinical microbial infections.…”

Discovery of Alkaloid Quinazolone‐Derived Imidazolenones with Novel Structural Scaffolds of Multitargeting Antibacterial Potential

“…As one of the nitrogen‐containing five‐membered heterocycles, imidazoles receive extensive attention in drug design and development [ 7 ] and have been used in clinic, such as anti‐anaerobes metronidazole and antifungal miconazole and ketoconazole. Imidazoles with electron‐rich aromatic structures are able to bind to biomacromolecules such as DNA, enzymes and receptors through a variety of noncovalent interactions, [ 8 ] which is conducive to promoting bacterial death. Further, the presence of imidazole ring may be favorable for improving low water solubility to some extent due to its two nitrogen atoms easily leading to the formation of hydrogen bonds with water.…”