Design, synthesis and biological evaluation of new 5-nitro benzimidazole derivatives as AT1 antagonists with anti-hypertension activities

Zhu, Weibo; Da, Yajing; Wu, Dan; Zheng, Hongchen; Zhu, Linfeng; Wang, Li; Yan, Yuan; Chen, Zhilong

doi:10.1016/j.bmc.2014.02.008

Cited by 44 publications

(23 citation statements)

References 8 publications

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“…Benzimidazole is a popular nucleus in structural manipulation in medicinal chemistry and has been intensively discussed in the literature [ 19 , 21 , 22 , 23 , 24 ] and many benzimidazoles are reported to show anthelmintic [ 25 , 26 ], antimicrobial [ 27 , 28 , 29 , 30 , 31 , 32 ], anti-HIV [ 33 , 34 , 35 ], antiviral [ 36 , 37 ], anti-inflammatory [ 38 , 39 ], anticancer [ 40 , 41 , 42 , 43 , 44 ], anticonvulsant [ 45 ], antidiabetic [ 45 , 46 ], antihypertensive [ 47 ], anti-tuberculosis [ 48 , 49 ], antimalarial [ 50 , 51 ] and antioxidant [ 52 , 53 ] activities.…”

Section: Benzazolesmentioning

confidence: 99%

Importance of Fluorine in Benzazole Compounds

2020

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Fluorine-containing heterocycles continue to receive considerable attention due to their unique properties. In medicinal chemistry, the incorporation of fluorine in small molecules imparts a significant enhancement their biological activities compared to non-fluorinated molecules. In this short review, we will highlight the importance of incorporating fluorine as a basic appendage in benzothiazole and benzimidazole skeletons. The chemistry and pharmacological activities of heterocycles containing fluorine during the past years are compiled and discussed.

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Section: Benzazolesmentioning

confidence: 99%

Importance of Fluorine in Benzazole Compounds

2020

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“…Benzimidazole is a well-known pharmacophore which has played a crucial role in the theoretical development of heterocyclic chemistry and organic synthesis. It possess multifarious bioactivities as antimicrobial 11 , antitubercular 12 , anticancer 13 , proton pump inhibitors 14 , antiviral 15 , antioxidant 16 , antiparasitic 17 , antihelmintics 18 , anti-HIV 19 , anticonvulsant 20 , anti-inflammatory 21 , antihypertensive 22 . It is also an important constituent of Vitamin-B 12 23 .…”

Section: Variousmentioning

confidence: 99%

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2018

IJPSR

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A series of (Z)-3-((1H-benzo[d]imidazol-2-yl)methyl)substituted thiazolidine-2,4-dione (9a-n) have been synthesized and evaluated for their mycobacterium inhibitory activity against Mycobacterium tuberculosis H37Rv strain. The structures of the newly synthesized compounds were characterized by FTIR and NMR spectral analysis. Most of the synthesized compounds showed moderate to good anti-tubercular activity. Among these compounds 9a, 9d, 9f and 9g have displayed good anti-tubercular activity (MIC 6.25 μg/ml). Further, the molecular docking studies were carried out in order to rationalze the biological activity.

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“…7) exerts high nanomolar and durable activity (IC 50 = 1.03 ± 0.26nM) in vascular smooth muscle cells. This compound bears an indole benzoic ring instead of the biphenyl scaffold with an acidic segment attached at the ortho-position, (a common feature to commercial drugs except eprosartan that contains only one phenyl ring) 18 . (Fig.…”

Section: Fig 5: Chemical Structure Of Bv6mentioning

confidence: 99%

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2017

IJPSR

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ABSTRACT:The renin-angiotensin system (RAS) plays an important role in pathogenesis of hypertension, congestive heart failure, and chronic renal failure. In addition to a discussion of the current understanding of the chemical structures and the modes of action of angiotensin converting enzyme (ACE) inhibitors and angiotensin receptor (ATR) antagonists, review includes their SAR analysis and chemical modification for improving their activity. Nowadays different modeling strategies are underway to develop tailor made molecules with the best of properties among nonpeptide renin inhibitors, dual action receptor antagonists (e.g. angiotensin and endothelin antagonists, ACE/NEP inhibitors, AT 1 /TxA 2 antagonists, balanced AT 1 /AT 2 antagonists), triple inhibitors. In the first part is given an overview of various ACE inhibitors. The second part is devoted to overview of angiotensin receptor antagonists. The advances that have been made, new opportunities, and future directions of design and development of these classes have been discussed.

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Design, synthesis and biological evaluation of new 5-nitro benzimidazole derivatives as AT1 antagonists with anti-hypertension activities

Cited by 44 publications

References 8 publications

Importance of Fluorine in Benzazole Compounds

Importance of Fluorine in Benzazole Compounds

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