Development of drugs based on imidazole and benzimidazole bioactive heterocycles: recent advances and future directions

Gaba, Monika; Mohan, Chander

doi:10.1007/s00044-015-1495-5

Cited by 251 publications

(128 citation statements)

References 144 publications

Supporting

Mentioning

125

Contrasting

Unclassified

Order By: Relevance

“…Some of the imidazole based drugs viz., ketoconazole, econazole, tinidazole, metronidazole etc., are used in the market as antimicrobial agents. [6] Besides, 1,2,3-triazole containing compounds possess antifungal, [7] antibacterial, [8] antimalarial, [9] antiviral [10] and antimycobacterial activities. [11] Clinically, tazobactam, cefatrizine, fluconazole and voriconazole [12] are widely used to treat Invasive Fungal Infections (IFIs; Figure 1).…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Molecular Properties Prediction and Antimicrobial Activity of Imidazolyl Schiff Bases, Triazoles and Azetidinones

Rekha

Ummadi

Padmaja

et al. 2019

Chemistry & Biodiversity

View full text Add to dashboard Cite

Benzylidenehydrazinyl imidazoles (3) are prepared from 2‐hydrazinyl imidazoles (2) on treatment with hydrazine. The imine functionality in 3 is utilized to develop 5′‐aryl‐N‐(4‐aryl‐1H‐imidazol‐2‐yl)‐1H‐1,2,3‐triazol‐1‐amines (5) by 1,3‐dipolar cycloaddition of diazomethane followed by aromatization with I2 in DMSO. Compounds 3 are also explored to prepare 4′‐aryl‐1‐(4‐aryl‐1H‐imidazol‐2‐ylamino)‐3‐chloroazetidin‐2‐ones (6) on treatment with chloroacetyl chloride. The Molinspiration calculations predicted that 3, 5 and 6 have molecular hydrophobicity, conformational flexibility, good intestinal absorption and bioactivity scores. The chloro, bromo and nitro substituted imidazolyl azetidinones (6c, 6d, 6f) and nitro substituted imidazolyl triazole (5f) exhibited excellent antibacterial activity on B. subtilis, whereas chloro and nitro substituted imidazolyl triazoles (5c, 5f) showed prominent antifungal activity on A. niger.

show abstract

Section: Introductionmentioning

confidence: 99%

Synthesis, Molecular Properties Prediction and Antimicrobial Activity of Imidazolyl Schiff Bases, Triazoles and Azetidinones

Rekha

Ummadi

Padmaja

et al. 2019

Chemistry & Biodiversity

View full text Add to dashboard Cite

show abstract

“…Fur ther more, benzimidazole moiety is a crucial template in medicinal chemistry because of its wide variety of reported biological and pharmacological activities, some of which include anticancer 11 , antimicrobial 12 , antitumor 13 , antimalarial 14 ,anti-HIV 15 , anti-inflammatory 16 , antitubercular 17 , anthelmintic 18 , anticonvulsant 19 , antioxidant 20 , anti-ulcer 21 , anti-HBV 22 , among others. The pharmacological investigation showed that the antagonism of Ang II-induced pressure response by oral administration of a series of benzimidazole hybrid was obviously superior to that of clinical drug standard used.…”

Section: -9mentioning

confidence: 99%

Facile Synthesis, Characterization and Antimicrobial Activity of 2-Alkanamino Benzimidazole Derivatives

Ajani¹,

Aderohunmu²,

Olorunshola³

et al. 2016

Orient. J. Chem

View full text Add to dashboard Cite

Benzimidazole derivatives are known to represent a class of medicinally important compounds which are extensively used in drug design and catalysis. A series of 2-substituted benzimidazole derivatives 10a-i was herein synthesized from the reaction of o-phenylenediamine with some amino acids using ameliorable pathway. The chemical structures of the synthesized compounds were confirmed by IR, UV, 1 H-NMR, 13 C-NMR, Mass spectral and analytical data. The compounds were investigated for their antimicrobial activity alongside gentamicin clinical standard. The results showed that this skeletal framework exhibited marked potency as antimicrobial agents. The most active compound was 1H-benzo[d]imidazol-2-yl)methanamine, 10a.

show abstract

“…The synthesis of substituted benzimidazole derivatives is of considerable importance, because most of these compounds have a promising biological activity [1][2][3][4][5][6][7][8][9][10]. Also, the compounds whose molecules possess an azole ring, such as pyrrole [11][12][13], 1,3,4-oxadiazole [14][15][16][17][18][19] and 1,2,4-triazole [19][20][21][22][23], are often characterized as good antimicrobial agents.…”

Section: Introductionmentioning

confidence: 99%

Nucleophilic ring opening of 1,4-disubstituted 2-pyrrolidones with hydrazine. Synthesis of azoles with a high antibacterial activity

Peleckis¹,

Anusevičius²,

Šiugždaitė³

et al. 2018

chemija

View full text Add to dashboard Cite

3-(1H-Benzimidazol-2-yl)-4-[(phenyl and 4-substituted phenyl)amino]butanohydrazides were synthesized in good yields by treating the corresponding 4-(1H-benzimidazol-2-yl)-1-phenyl(substituted phenyl)-2-pyrrolidinones with the excess of hydrazine monohydrate. The utility of the newly synthesized hydrazides in the preparation of pyrroles, pyrazoles, oxadiazoles and triazoles has been demonstrated. All compounds were screened for their antibacterial activity. A significant antibacterial activity was found.

show abstract

Development of drugs based on imidazole and benzimidazole bioactive heterocycles: recent advances and future directions

Cited by 251 publications

References 144 publications

Synthesis, Molecular Properties Prediction and Antimicrobial Activity of Imidazolyl Schiff Bases, Triazoles and Azetidinones

Synthesis, Molecular Properties Prediction and Antimicrobial Activity of Imidazolyl Schiff Bases, Triazoles and Azetidinones

Facile Synthesis, Characterization and Antimicrobial Activity of 2-Alkanamino Benzimidazole Derivatives

Nucleophilic ring opening of 1,4-disubstituted 2-pyrrolidones with hydrazine. Synthesis of azoles with a high antibacterial activity

Contact Info

Product

Resources

About