Design, Synthesis and Antifungal Activity of Some New Imidazole and Triazole Derivatives

Rezaei, Zahra; Khabnadideh, Soghra; Zomorodian, Kamiar; Pakshir, Keyvan; Kashi, Giti; Sanagoei, Narges; Gholami, Sanaz

doi:10.1002/ardp.201000357

Cited by 27 publications

(23 citation statements)

References 16 publications

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“…However, replacement of diphenyl group in bifonazole by benzoxazolone ring ( 103 ) led to completely lost anti‐ Candida efficacy . The high antifungal potency of 102a ‐ b might be attributed to their small size, which made them convenient to penetrate into fungi cell, and the chlorine atoms with a positive effect was helpful for improving affinity toward the heme binding site …”

Section: Imidazoles As Antifungal Agentsmentioning

confidence: 99%

Comprehensive Review in Current Developments of Imidazole-Based Medicinal Chemistry

et al. 2013

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Imidazole ring is an important five-membered aromatic heterocycle widely present in natural products and synthetic molecules. The unique structural feature of imidazole ring with desirable electron-rich characteristic is beneficial for imidazole derivatives to readily bind with a variety of enzymes and receptors in biological systems through diverse weak interactions, thereby exhibiting broad bioactivities. The related research and developments of imidazole-based medicinal chemistry have become a rapidly developing and increasingly active topic. Particularly, numerous imidazole-based compounds as clinical drugs have been extensively used in the clinic to treat various types of diseases with high therapeutic potency, which have shown the enormous development value. This work systematically gives a comprehensive review in current developments of imidazole-based compounds in the whole range of medicinal chemistry as anticancer, antifungal, antibacterial, antitubercular, anti-inflammatory, antineuropathic, antihypertensive, antihistaminic, antiparasitic, antiobesity, antiviral, and other medicinal agents, together with their potential applications in diagnostics and pathology. It is hoped that this review will be helpful for new thoughts in the quest for rational designs of more active and less toxic imidazole-based medicinal drugs, as well as more effective diagnostic agents and pathologic probes.

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Section: Imidazoles As Antifungal Agentsmentioning

confidence: 99%

Comprehensive Review in Current Developments of Imidazole-Based Medicinal Chemistry

et al. 2013

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“…These analyses underlined a relationship between antimicrobial potency and molecular penetration into fungi cell. Consequently, the presence of bulky substituents, as OCH 3 , was believed to be responsible for the activity decrease [77,78].…”

Section: Benzotriazole As Antimycotic Agentmentioning

confidence: 99%

“…21). Throughout drug-design studies, applying Autodock on MT-CYP51, the best in silico promising derivatives were synthesized and their antimycotic activity was compared to that of fluconazole and itraconazole, used as reference drugs [78]. Unfortunately, benzotriazole derivatives did not show antifungal activity against Candida species.…”

Section: Benzotriazole As Antimycotic Agentmentioning

confidence: 99%

Benzotriazole: An overview on its versatile biological behavior

Briguglio

Piras

Corona

et al. 2015

European Journal of Medicinal Chemistry

163

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Discovered in late 1960, azoles are heterocyclic compounds class which constitute the largest group of available antifungal drugs. Particularly, the imidazole ring is the chemical component that confers activity to azoles. Triazoles are obtained by a slight modification of this ring and similar or improved activities as well as less adverse effects are reported for triazole derivatives. Consequently, it is not surprising that benzimidazole/benzotriazole derivatives have been found to be biologically active. Since benzimidazole has been widely investigated, this review is focused on defining the place of benzotriazole derivatives in biomedical research, highlighting their versatile biological properties, the mode of action and Structure Activity Relationship (SAR) studies for a variety of antimicrobial, antiparasitic, and even antitumor, choleretic, cholesterol-lowering agents.

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“…Perhaps we have gotten as much out of a family of compounds as is possible with only minimal increments in advantages. However, new imidazole and triazole derivatives are in development and appear promising [66]. …”

Section: Conclusion and Future Perspectivementioning

confidence: 99%

Antifungal Drug Discovery: The Process and Outcomes

et al. 2014

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New data suggest that the global incidence of several types of fungal diseases have traditionally been under-documented. Of these, mortality caused by invasive fungal infections remains disturbingly high, equal to or exceeding deaths caused by drug-resistant tuberculosis and malaria. It is clear that basic research on new antifungal drugs, vaccines and diagnostic tools is needed. In this review, we focus upon antifungal drug discovery including in vitro assays, compound libraries and approaches to target identification. Genome mining has made it possible to identify fungal-specific targets; however, new compounds to these targets are apparently not in the antimicrobial pipeline. We suggest that ‘repurposing’ compounds (off patent) might be a more immediate starting point. Furthermore, we examine the dogma on antifungal discovery and suggest that a major thrust in technologies such as structural biology, homology modeling and virtual imaging is needed to drive discovery.

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Design, Synthesis and Antifungal Activity of Some New Imidazole and Triazole Derivatives

Cited by 27 publications

References 16 publications

Comprehensive Review in Current Developments of Imidazole-Based Medicinal Chemistry

Comprehensive Review in Current Developments of Imidazole-Based Medicinal Chemistry

Benzotriazole: An overview on its versatile biological behavior

Antifungal Drug Discovery: The Process and Outcomes

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