Synthesis and <i>in‐vitro</i> Anti‐hepatitis B Virus Activity of Ethyl 6‐Bromo‐8‐hydroxyimidazo[1,2‐<i>a</i>]pyridine‐3‐carboxylates

Chen, Dong; Liu, Yajing; Zhang, Shulan; Guo, Dexiang; Liu, Chunhong; Li, Sai; Gong, Ping

doi:10.1002/ardp.201000045

Cited by 7 publications

(2 citation statements)

References 16 publications

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“…Phenolic Mannich bases 233 (R 1 ¼ H, 4-F, 4-Cl, 4-Br, 4-CH 3 , 3-OCH 3 ) derived from 6bromo-8-hydroxyimidazo[1,2-a]pyridine-3-carboxylates ( Fig. 42), especially those having 4-morpholinyl or 4-methylpiperazin-1-yl moieties in the aminomethyl function, inhibited the replication of HBV DNA, but had no inhibitory effect on secretion of HBsAg or HBeAg [354]. The nature of substituents in the arylmercapto residue modulates the anti-HBV activity, as the decrease of bulkiness of the substituents (from bromine to fluorine, for example) and the presence of lipophilic substituents (e.g., a methyl group) enhance the inhibition of replication of HBV DNA, whereas the presence of a 3-methoxy group further increases the activity.…”

Section: Antiviral Activitymentioning

confidence: 99%

Mannich bases in medicinal chemistry and drug design

Roman¹

2015

European Journal of Medicinal Chemistry

271

110

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The biological activity of Mannich bases, a structurally heterogeneous class of chemical compounds that are generated from various substrates through the introduction of an aminomethyl function by means of the Mannich reaction, is surveyed, with emphasis on the relationship between structure and biological activity. The review covers extensively the literature reports that have disclosed Mannich bases as anticancer and cytotoxic agents, or compounds with potential antibacterial and antifungal activity in the last decade. The most relevant studies on the activity of Mannich bases as antimycobacterial agents, antimalarials, or antiviral candidates have been included as well. The review contains also a thorough coverage of anticonvulsant, anti-inflammatory, analgesic and antioxidant activities of Mannich bases. In addition, several minor biological activities of Mannich bases, such as their ability to regulate blood pressure or inhibit platelet aggregation, their antiparasitic and anti-ulcer effects, as well as their use as agents for the treatment of mental disorders have been presented. The review gives in the end a brief overview of the potential of Mannich bases as inhibitors of various enzymes or ligands for several receptors.

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Section: Antiviral Activitymentioning

confidence: 99%

Mannich bases in medicinal chemistry and drug design

Roman¹

2015

European Journal of Medicinal Chemistry

271

110

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“…Furthermore, pyridine is an important class of heterocyclic ring, which have attracted attention in past few years. The pyridine nucleus exists in numerous natural products and is extremely important in the chemistry of biological systems, such as antioxidant activity [ 27 ], antimicrobial activity [ 28 ], acetylcholinesterase inhibitors [ 29 ], antibacterial activity [ 30 , 31 ], anticancer activity [ 32 , 33 ], anti-HBV activity [ 34 ], and so on. In the fungicidal activity area, some pyridine derivatives can prevent Ralstonia solanacearum [ 35 ], Cerospora beticola sacc.…”

Section: Introductionmentioning

confidence: 99%

Microwave Assistant Synthesis, Antifungal Activity and DFT Theoretical Study of Some Novel 1,2,4-Triazole Derivatives Containing Pyridine Moiety

Sun

Yang

Shi

et al. 2014

IJMS

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In order to investigate the biological activity of novel 1,2,4-triazole compounds, seventeen novel 1,2,4-triazole derivatives containing pyridine moiety were synthesized under microwave assistant condition by multi-step reactions. The structures were characterized by 1H NMR, MS and elemental analyses. The target compounds were evaluated for their fungicidal activities against Stemphylium lycopersici (Enjoji) Yamamoto, Fusarium oxysporum. sp. cucumebrium, and Botrytis cinerea in vivo, and the results indicated that some of the title compounds displayed excellent fungicidal activities. Theoretical calculation of the title compound was carried out with B3LYP/6-31G (d,p). The full geometry optimization was carried out using 6-31G (d,p) basis set, and the frontier orbital energy, atomic net charges were discussed, and the structure-activity relationship was also studied.

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ChemInform Abstract: Synthesis and in vitro Antihepatitis B Virus Activity of Ethyl 6‐Bromo‐8‐hydroxyimidazo[1,2‐a]pyridine‐3‐carboxylates.

et al. 2011

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Synthesis and in vitro Antihepatitis B Virus Activity of Ethyl 6-Bromo-8-hydroxyimidazo[1,2-a]pyridine-3-carboxylates. -19 Title compounds of type (VIII) are prepared and tested for their in-vitro anti-hepatitis B virus activities. Nearly half of the compounds are highly effective in inhibiting the replication of HBV DNA with (VIIId) and (VIIIe) being the most promising compounds. -(CHEN, D.; LIU, Y.; ZHANG, S.; GUO, D.; LIU, C.; LI, S.; GONG*, P.; Arch. Pharm. (Weinheim, Ger.) 344 (2011) 3, 158-164, http://dx.doi.org/10.1002/ardp.201000045 ; Sch. Pharm. Eng., Shenyang Pharm. Univ., Shenyang 110016, Peop. Rep. China; Eng.) -M. Bohle 27-165

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Synthesis and in‐vitro Anti‐hepatitis B Virus Activity of Ethyl 6‐Bromo‐8‐hydroxyimidazo[1,2‐a]pyridine‐3‐carboxylates

Cited by 7 publications

References 16 publications

Mannich bases in medicinal chemistry and drug design

Mannich bases in medicinal chemistry and drug design

Microwave Assistant Synthesis, Antifungal Activity and DFT Theoretical Study of Some Novel 1,2,4-Triazole Derivatives Containing Pyridine Moiety

ChemInform Abstract: Synthesis and in vitro Antihepatitis B Virus Activity of Ethyl 6‐Bromo‐8‐hydroxyimidazo[1,2‐a]pyridine‐3‐carboxylates.

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