SAR study of clubbed [1,2,4]-triazolyl with fluorobenzimidazoles as antimicrobial and antituberculosis agents

Jadhav, Ganesh R.; Shaikh, Mohammad Usman; Kale, Rajesh P.; Shiradkar, Mahendra; Gill, Charansingh H.

doi:10.1016/j.ejmech.2008.12.001

Cited by 69 publications

(23 citation statements)

References 31 publications

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“…The antibacterial data suggested that the analogues with electronegative substituents emerged as the most promising antimicrobials. A few of the selected analogues are under further evaluation for secondary antitubercular screening, as they have shown better activity when compared to rifampin [101]. …”

Section: Antitubercular Activitymentioning

confidence: 99%

Pharmacological significance of triazole scaffold

Kharb

Sharma

Yar

2010

Journal of Enzyme Inhibition and Medicinal Chemistry

453

236

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Section: Antitubercular Activitymentioning

confidence: 99%

Pharmacological significance of triazole scaffold

Kharb

Sharma

Yar

2010

Journal of Enzyme Inhibition and Medicinal Chemistry

453

236

View full text Add to dashboard Cite

“…After the antibacterial evaluation, it was found that the compounds having electronegative substituents possess promising antimicrobials. It was also observed that the compounds with good antimicrobials activities can possess better antimycobacterials activity as well (Jadhav et al, 2009). Marrapu et al synthesized some chalcone substituted imidazole and found active against the virulent M. tuberculosis (Marrapu et al, 2011).…”

Section: Antitubercularmentioning

confidence: 99%

Imidazole and its derivatives as potential candidates for drug development

Mumtaz

Saeed

Fatima

et al. 2016

Bangladesh J Pharmacol

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Imidazole and its derivatives are the pharmacological significant scaffolds with the broad spectrum of activities can be synthesized in the laboratory in the single step by the action of the catalyst. The current review summarizes the role of the imidazole and its derivatives during the last decade (2005)(2006)(2007)(2008)(2009)(2010)(2011)(2012)(2013)(2014) for the treatment of many diseases. Review highlights their significant contribution towards the drug development for the treatment of some fatal diseases like HIV, cancer, tuberculosis and hepatitis C. As imidazole and its derivatives continue to play an important role for the treatment of many diseases so there is a need to trigger research in this field. Article InfoReceived:26 Mini-reviewThis article was downloaded by you on: Oct 01, 2016 2009), anti-oxidant (Sorrenti et al., 2006) and antidepressant (Dostert et al., 1990) are the known examples.Synthesis of imidazole ring and its derivatives is carried out by using one-step condensation of diketone with aldehyde, ammonium acetate and primary aromatic amine in the presence of nanocrystalline magnesium aluminate (Safari et al., 2013), supported ionic liquidlike phase (Saffari Jourshari et al., 2013), SiO2-Pr-SO3H (Ziarani et al., 2013, clay supported titanium catalyst (Kannan and Sreekumar, 2013), brønsted acidic ionic liquid,(4-sulfobutyl)tris(4-sulfophenyl)phosphonium hydrogen sulfate (Banothu et al., 2013), nano-TiCl4.SiO2 (Mirjalili et al., 2012) I2/Cs2CO3 (Xue et al., 2014 and sulfonic acid functionalized SBA-15 nanoporous material (SBA-Pr-SO3H) catalyst .As imidazole and its derivatives are associated with a number of biological significances so the current review will emphasized on the role of imidazole and its derivative as potential candidate for the development of drugs to treat some fatal diseases including HIV-AIDS (de Walque, 2014), cancer (Fraser et al., 2014), hepatitis-C (Linas et al., 2014) and tuberculosis (Zoraghi and Reiner, 2013), etc. Pharmacological SignificancesFrom the literature, it is found that imidazole and their derivatives they possess potent activities against fetal diseases and playing a significant role in a fight against them. Anti-HIV activityAcquired immunodeficiency syndrome (AIDS) is a viral disease caused due to the special virus Human Immunodeficiency Virus type 1 (HIV-1) (Basu et al., 2009). The HIV-1 type virus destroys the lymphocytes the 'helper cell' which fight against the infections (Roy and Leonard, 2005). According to World Health Organization report, three million people were suffering from AIDS and more than five million people acquire the AIDS in the single year (AIDS, 2003). As the HIV-AIDS is increasing globally and there is a need to introduce some new drugs to help in a fight against this fatal disease. In this regard imidazole and their derivatives are playing a significant role in the treatment of disease. During the course of drugs for the treatment of HIV-AIDS, the activity is mainly focused on the interaction of the compound with t...

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“…A new strategy of hybridization between benzimidazole and a 1,2,4-triazole ring has obtained a series of compounds (34, figure 9). Using a SAR study, it was determined that these compounds enhance biological activity by increasing electronegativity of the molecule, but surprisingly when a trifluoromethyl group (high electronegativity) was introduced, it produced a substantial loss of activity, which could be due to a delay in intracellular transport (Jadhav et al, 2009). Following with the use of a benzimidazole ring as a drug design, Klimešova and cols replaced a nitrogen atom with a corresponding oxygen atom (isosteric) (35, figure 9) to obtain a series of benzylsulfanyl benzoxazole derivatives.…”

Section: Azoles Derivativesmentioning

confidence: 99%