Metronidazole hydrazone conjugates: Design, synthesis, antiamoebic and molecular docking studies

Ansari, Mohammad Fawad; Siddiqui, Shadab Miyan; Agarwal, Subhash Mohan; Vikramdeo, Kunwar Somesh; Mondal, Neelima; Azam, Amir

doi:10.1016/j.bmcl.2015.06.091

Cited by 27 publications

(6 citation statements)

References 30 publications

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“…Among the imidazole derivatives, MNZ is one compound with potent antiprotozoal activity against E. Hystolytica, T. vaginalis and giardia including periodontal pathogens [5]. Due to its short half-life, it requires frequent dosing.…”

Section: Introductionmentioning

confidence: 99%

Development of Sodium Alginate Coated Nanoparticles of Metronidazole for the Treatment of Periodontitis

Singh

Jain

2019

Int J App Pharm

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Objective: The present study was aimed to develop metronidazole (MNZ) loaded poly lactic-co-glycolic acid (PLGA) based mucoadhesive nanoparticles (NPs) in prolonged treatment in periodontitis. Methods: Nanoparticles were prepared by using single (SE) and double (DE) emulsion method to determine the suitability of methods. Prepared NPs were evaluated for surface morpholgy, mean particle size, polydispersity index, zeta potential, mucoadhesion ability and invitro-drug release, Results: SEM images confirmed that NPs were of spherical shape and smooth surface. Mean particle size, of MNZ loaded NPs were found 583.28±18.22 and 872.72±63.18 prepared by SE and DE method. Similarly, polidispersity index (0.68±0.1 and 0.83±0.06) and zeta potention (-33.29±0.7 and-31.28.0.6) was found in acceptable range. Prepared NPs were surface treated with Sodium alginate (SA) to increase mucoadhesive property. It was observe that particles remain adhere till 24 hr with biological membrane. Prepared NPs allow release of MNZ upto 24 h in sustained manner. Conclusion: This study confirms that the prepared MNZ loaded NPs may be used as an better alternate with addition application such as prolonged action thus improved patient compliance.

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Section: Introductionmentioning

confidence: 99%

Development of Sodium Alginate Coated Nanoparticles of Metronidazole for the Treatment of Periodontitis

Singh

Jain

2019

Int J App Pharm

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“…A series of chalcones were synthesized bearing N-substituted ethanamine by aldol condensation reaction and the compound ( 17 ) was found to be very potent amoebicidal indicating that such compounds can be the effective therapeutic candidates (Zaidi et al, 2015 ). Metronidazole hydrazone conjugates were synthesized and screened in vitro for antiamoebic activity, the compound ( 18 ) was found more active (Ansari et al, 2015 ). A series of chloroquinoline-acetamide hybrids were synthesized and the compound ( 19 ) inhibit the growth of E. histolytica (Inam et al, 2015 ).…”

Section: Entamoeba Histolyticamentioning

confidence: 99%

Parasitic diarrheal disease: drug development and targets

2015

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Diarrhea is the manifestation of gastrointestinal infection and is one of the major causes of mortality and morbidity specifically among the children of less than 5 years age worldwide. Moreover, in recent years there has been a rise in the number of reports of intestinal infections continuously in the industrialized world. These are largely related to waterborne and food borne outbreaks. These occur by the pathogenesis of both prokaryotic and eukaryotic organisms like bacteria and parasites. The parasitic intestinal infection has remained mostly unexplored and under assessed in terms of therapeutic development. The lack of new drugs and the risk of resistance have led us to carry out this review on drug development for parasitic diarrheal diseases. The major focus has been depicted on commercially available drugs, currently synthesized active heterocyclic compounds and unique drug targets, that are vital for the existence and growth of the parasites and can be further exploited for the search of therapeutically active anti-parasitic agents.

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“…It is the second leading cause of death from the parasitic disease worldwide, which occurs through the consumption of contaminated water or food. It results in 50 million cases and up to a million deaths per annum worldwide . The highest incidence is seen in Mexico, India, Central and South America as well as the tropical regions of Asia and Africa, where sanitary conditions are poor .…”

Section: Introductionmentioning

confidence: 99%

Insight into structural requirements of antiamoebic flavonoids: 3D‐QSAR and G‐QSAR studies

2018

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Plant-based flavonoids have been found to exhibit strong inhibitory capability against Entamoeba histolytica. So, various QSAR models have been developed to identify the critical features that are responsible for the potency of these molecules. 3D-QSAR analysis using k-nearest neighbour molecular field analysis via stepwise forward-backward variable selection method showed best results for both internal and external predictive ability of the model (i.e., q = 0.64 and pred_r = 0.56). Also, a group-based QSAR (G-QSAR) model was developed based on partial least squares regression combined with stepwise forward-backward variable selection method. It gave best parametric results (r = 0.74, q = 0.56 and pred_r = 0.54) which implied that the model is highly predictive. 3D-QSAR established that presence/absence of bulk near rings B and C is important in deciding the inhibitory potential of these molecules. Additionally, G-QSAR provided site-specific clue wherein modifications related to molecular weight, electronegativity and separation of an oxygen atom in rings A and C can result in enhanced biological activity. To the best of the author's knowledge, this is the first QSAR study of antiamoebic flavonoids, and therefore, we expect the results to be useful in the design of more potent antiamoebic inhibitors.

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Metronidazole hydrazone conjugates: Design, synthesis, antiamoebic and molecular docking studies

Cited by 27 publications

References 30 publications

Development of Sodium Alginate Coated Nanoparticles of Metronidazole for the Treatment of Periodontitis

Development of Sodium Alginate Coated Nanoparticles of Metronidazole for the Treatment of Periodontitis

Parasitic diarrheal disease: drug development and targets

Insight into structural requirements of antiamoebic flavonoids: 3D‐QSAR and G‐QSAR studies

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