Green synthesis, antileishmanial activity evaluation, and in silico studies of new amino acid-coupled 1,2,4-triazoles

El‐Saghier, Ahmed M. M.; Mohamed, Mounier A.; Abd-Allah, Omyma A; Kadry, Asmaa M.; Ibrahim, Tamer M.; Bekhit, Adnan A.

doi:10.1007/s00044-018-2274-x

Cited by 36 publications

(19 citation statements)

References 49 publications

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“…45 ) were evaluated for their in vitro antileishmanial activity on L. major promastigotes by El-Saghier et al. [ 9 ]. Among them, compounds 236a-d (IC 50 : 0.0312–0.0866 μg/mL) were 36–100 folds more potent than the reference miltefosine (IC 50 : 3.1924 μg/mL) and comparable to amphotericin B deoxycholate (IC 50 : 0.0472 μg/mL).…”

Section: Biological Activities Of 124-triazole Derivativesmentioning

confidence: 99%

“…1,2,4-Triazoles and their fused heterocyclic derivatives have been reported to possess a wide range of bioactivities such as neuroprotectant [ 6 ], antioxidant [ 7 ], antimalarial [ 8 ], antileishmanial [ 9 ], anti-urease [ 10 ], antiviral [ 11 , 12 ], anticonvulsant [ 13 ], cannabinoid CB1 receptor antagonists [ 14 ], PDE4A inhibitors [ 15 ] and γ-aminobutyric acid-A (GABA-A) α-2, α-3 and α-5 containing receptor antagonists [ 16 ]. Moreover, they have applications in ionic liquids, corrosion inhibitors, agrochemicals, polymers, supramolecular and material science [ [17] , [18] , [19] , [20] , [21] ].…”

Section: Introductionmentioning

confidence: 99%

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An insight on medicinal attributes of 1,2,4-triazoles

Aggarwal

Sumran²

2020

European Journal of Medicinal Chemistry

197

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The present review aims to summarize the pharmacological profile of 1,2,4-triazole, one of the emerging privileged scaffold, as antifungal, antibacterial, anticancer, anticonvulsant, antituberculosis, antiviral, antiparasitic, analgesic and anti-inflammatory agents, etc. along with structure-activity relationship. The comprehensive compilation of work carried out in the last decade on 1,2,4-triazole nucleus will provide inevitable scope for researchers for the advancement of novel potential drug candidates having better efficacy and selectivity.

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Section: Biological Activities Of 124-triazole Derivativesmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

An insight on medicinal attributes of 1,2,4-triazoles

Aggarwal

Sumran²

2020

European Journal of Medicinal Chemistry

197

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“…In this direction a new class of GSK-3 inhibitors containing the triazole scaffold with favorable water solubility 46-48 ( Figure 12) were synthesized by treatment of 3-azido-2-amino-1,2,5-oxadiazole with ethyl chloroacetacetic acid, giving access to the key functionalized [1-3]-triazoles moieties [43]. Furthermore, a series of triazole-containing amino acid derivatives 52 ( Figure 13) was prepared under green chemistry conditions via MCRs using lemon juice as an acidic catalyst [44]. Moreover, in silico predictions revealed that these compounds exhibited promising drug-likeness and pharmacokinetics profile.…”

Section: A Safer Approach To Ndd Drug Discovery: Green Chemistry Techmentioning

confidence: 99%

“…Their results showed an excellent free radical scavenging ability against different free radicals ( • OH, CH3 • CHOH, SO3 •-), and showed good neuroprotective activity without producing cell damage or cytotoxicity [48]. Furthermore, a series of triazole-containing amino acid derivatives 52 ( Figure 13) was prepared under green chemistry conditions via MCRs using lemon juice as an acidic catalyst [44]. Moreover, in silico predictions revealed that these compounds exhibited promising drug-likeness and pharmacokinetics profile.…”

Section: A Safer Approach To Ndd Drug Discovery: Green Chemistry Techmentioning

confidence: 99%

“…Moreover, in silico predictions revealed that these compounds exhibited promising drug-likeness and pharmacokinetics profile. Furthermore, a series of triazole-containing amino acid derivatives 52 ( Figure 13) was prepared under green chemistry conditions via MCRs using lemon juice as an acidic catalyst [44]. Moreover, in silico predictions revealed that these compounds exhibited promising drug-likeness and pharmacokinetics profile.…”

Section: A Safer Approach To Ndd Drug Discovery: Green Chemistry Techmentioning

confidence: 99%

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Theoretical and Experimental Approaches Aimed at Drug Design Targeting Neurodegenerative Diseases

et al. 2019

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In recent years, green chemistry has been strengthening, showing how basic and applied sciences advance globally, protecting the environment and human health. A clear example of this evolution is the synergy that now exists between theoretical and computational methods to design new drugs in the most efficient possible way, using the minimum of reagents and obtaining the maximum yield. The development of compounds with potential therapeutic activity against multiple targets associated with neurodegenerative diseases/disorders (NDD) such as Alzheimer’s disease is a hot topic in medical chemistry, where different scientists from various disciplines collaborate to find safe, active, and effective drugs. NDD are a public health problem, affecting mainly the population over 60 years old. To generate significant progress in the pharmacological treatment of NDD, it is necessary to employ different experimental strategies of green chemistry, medical chemistry, and molecular biology, coupled with computational and theoretical approaches such as molecular simulations and chemoinformatics, all framed in the rational drug design targeting NDD. Here, we review how green chemistry and computational approaches have been used to develop new compounds with the potential application against NDD, as well as the challenges and new directions of the drug development multidisciplinary process.

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Synthesis and antidiabetic activity of novel triazole derivatives containing amino acids

Mohamed

Allah

Bekhit

et al. 2020

Journal of Heterocyclic Chem

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New series of triazole derivatives coupled with amino acids 1a‐h were obtained via multicomponent reaction of 2‐hydroxy benzaldehyde or 2‐hydroxy acetophenone with thiosemicarbazide and different amino acids. The obtained compounds were reacted with p‐toluinesulfonyl chloride 2 to give the corresponding sulfonamides 3a‐h. Compound 1b was allowed to react with different aromatic aldehydes or cyclic ketone under alkaline conditions to afford the expected imino compounds 4a‐d and 6a‐c, respectively. These compounds were allowed to react with ethyl glycolate to yield the expected thiazolidinone derivatives 5a‐d or 7a‐c, respectively. Structures of the newly synthesized compounds were found to be in accordance with their elemental analyses and spectral data. The obtained compounds exhibited very prominent in vitro and in vivo antihyperglycemic effect at a dose of 40 mg/kg body weight compared to the standard drug gliclazide and control. The antidiabetic effect was investigated using oral glucose tolerance test in normal and non‐insulin‐dependent diabetes mellitus (NIDDM) in STZ‐rat model. Compounds 3a‐h, 5b, 5c, 5d, 7a, 7b, and 7c showed significant activity in lowering blood glucose (more than 80%) compared to the NIDDM control.

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Green synthesis, antileishmanial activity evaluation, and in silico studies of new amino acid-coupled 1,2,4-triazoles

Cited by 36 publications

References 49 publications

An insight on medicinal attributes of 1,2,4-triazoles

An insight on medicinal attributes of 1,2,4-triazoles

Theoretical and Experimental Approaches Aimed at Drug Design Targeting Neurodegenerative Diseases

Synthesis and antidiabetic activity of novel triazole derivatives containing amino acids

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