Synthesis, Characterization of Some New Five Membered Heterocycles Based on Imidazole Moiety and their Applications on Therapeutics

Satyanarayana, V. S. V.; Sivakumar, A.; Ghosh, Asit Ranjan

doi:10.2174/157018011794578196

Cited by 8 publications

(5 citation statements)

References 22 publications

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“…Additionally, some acyl‐bridged triphenyl imidazole adducts were also reported to show good antibacterial activities. Pyrrolyl imidazole 139b displayed equivalent anti‐ E. coli potency with an MIC value of 250 μg/mL to tetracycline (MIC = 250 μg/mL) . Schiff base derivative 139c could effectively inhibit the growth of E. coli and S. aureus with MIC values in the range of 0.5–0.25 mg/mL, which was comparable to tetracycline (MIC = 0.25 mg/mL) .…”

Section: Imidazoles As Antibacterial Agentsmentioning

confidence: 98%

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 Antibacterial Agentsmentioning

confidence: 98%

Comprehensive Review in Current Developments of Imidazole-Based Medicinal Chemistry

et al. 2013

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“…The active pharmacophore (-N=CH-) of Schiff bases plays a major role in these significant biological activities. However, the attached neighbouring groups may also affect the activity [21]. Biological activities of Schiff bases metal complexes have also been reported [22,23].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Crystal Structure, DFT Studies and Evaluation of the Antioxidant Activity of 3,4-Dimethoxybenzenamine Schiff Bases

et al. 2014

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Schiff bases of 3,4-dimethoxybenzenamine 1 – 25 were synthesized and evaluated for their antioxidant activity. All the synthesized compounds were characterized by various spectroscopic techniques. In addition, the characterizations of compounds 13 , 15 and 16 were supported by crystal X-ray determinations and their geometrical parameters were compared with theoretical DFT calculations at the B3LYP level of theory. Furthermore, the X-ray crystal data of two non-crystalline compounds 8 and 18 were theoretically calculated and compared with the practical values of compounds 13 , 15 , 16 and found a good agreement. The compounds showed good DPPH scavenging activity ranging from 10.12 to 84.34 μM where compounds 1 – 4 and 6 showed stronger activity than the standard n -propyl gallate. For the superoxide anion radical assay, compounds 1 – 3 showed better activity than the standard.

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“…A hydrazide hydazone derived from safrole was found to be s potent antiinflammatory/antinociceptive agent [25], while benzylidene 10 H -phenothiazine-1-carbohydrazide has also been reported as an important anti-platelet agent [26]. The active pharmacophore (-CONH-N=CH-) of hydrazide hydrazones is mainly responsible for the significant biological activities although the attached neighboring groups may also be responsible [27]. Metal complexes of hydrazide hydrazones are also biologically active, besides having an important role in catalytic chemistry [28,29,30,31].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Evaluation of Antioxidant Activity and Crystal Structure of 2,4-Dimethylbenzoylhydrazones

et al. 2013

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2,4-Dimethylbenzoylhydrazones 1-30 were synthesized by condensation reactions of 2,4-dimethylbenzoylhydrazide with various aromatic aldehydes and characterized. The assigned structures of compounds 10, 15 and 22 were further supported by single-crystal X-ray diffraction data. The synthesized compounds were evaluated for their in vitro DPPH radical scavenging activity. They exerted varying degree of scavenging activity toward DPPH radical with IC 50 values between 25.6-190 µM. Compounds 1, 4, 2, 3, 7, and 6 have IC 50 values of 25.6, 28.1, 29.3, 29.8, 30.0 and 30.1 µM respectively, showing better activity than an n-propyl gallate standard (IC 50 value = 30.30 µM). For super oxide anion scavenging activity compounds 1, 2 and 3 with IC 50 values of 98.3, 102.6, and 105.6, respectively, also showed better activity than the n-propyl gallate standard (IC 50 value = 106.34 µM).

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Synthesis, Characterization of Some New Five Membered Heterocycles Based on Imidazole Moiety and their Applications on Therapeutics

Cited by 8 publications

References 22 publications

Comprehensive Review in Current Developments of Imidazole-Based Medicinal Chemistry

Comprehensive Review in Current Developments of Imidazole-Based Medicinal Chemistry

Synthesis, Crystal Structure, DFT Studies and Evaluation of the Antioxidant Activity of 3,4-Dimethoxybenzenamine Schiff Bases

Synthesis, Evaluation of Antioxidant Activity and Crystal Structure of 2,4-Dimethylbenzoylhydrazones

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