Synthesis and In Vitro Evaluation of Novel 1, 2, 4-Triazole Derivatives as Antifungal Agents

Kokil, Ganesh R.; Rewatkar, Prarthana; Gosain, Sandeep; Aggarwal, Saurabh; Verma, Ankita; Kalra, Atin; Thareja, Suresh

doi:10.2174/157018010789869415

Cited by 30 publications

(13 citation statements)

References 15 publications

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“…The ether‐linked coumarin–1,2,4‐triazole hybrids 7 (Fig. ) were examined for their in vitro antifungal activities against Candida albicans , and almost all hybrids displayed promising potency . It is worth mentioning that hybrids 7b–e (MIC: 12.5–75 μg/mL) with substituents regardless of electron‐withdrawing or electron‐donating groups at phenyl ring were far more active than the unsubstituted 7a (MIC: >200 μg/mL).…”

Section: Antibacterial and Antifungal Activitiesmentioning

confidence: 99%

Coumarin–triazole Hybrids and Their Biological Activities

Fan

Xing

Liu

2018

Journal of Heterocyclic Chem

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Hybridization is emerged as a promising strategy in the discovery of new drugs, especially these with complimentary activities and multiple pharmacological targets that are the potential weapons to prevent the drug resistance. Currently, several hybrids are under different stages of clinical trial, and may be introduced into clinical practice to treat various diseases in the near future. Triazoles including 1,2,3‐triazole and 1,2,4‐triazole as well as coumarins occupy an important position in medicinal chemistry attribute to their various biological activities, and some of them have been used in clinical practice. Obviously, hybridization of these two pharmacophores may lead to novel candidates with broader spectrum, more effective, lower toxicity, and multiple mechanisms of action. This review aims to outline the biological activities of coumarin–triazole hybrids, and discuss their structure–activity relationship to pave the way for the further rational development of this kind of hybrids.

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Section: Antibacterial and Antifungal Activitiesmentioning

confidence: 99%

Coumarin–triazole Hybrids and Their Biological Activities

Fan

Xing

Liu

2018

Journal of Heterocyclic Chem

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“…Certain triazoles undergo cleavage very easily due to socalled ring-chain tautomerism such as in the Dimroth rearrangement. 1,2,3triazole is considered to be the most useful component, widely used in research purpose as a building block for complex chemical compounds such as pharmaceutical drugs like tazobactam (Kaplancikli et al, 2005;Karakurt et al, 2006;Karthikeyan, 2009;Kharb et al, 2012;Kokil, 2010;Lin et al, 2005;Mohamed et al, 2006;Pachuta-Stec et al, 2009). 1, 2, 4-Triazole is a basic aromatic heterocycle and its derivatives possess a wide variety of pharmacological activity such as antifungal, anticancer, anticonvulsant, antimicrobial, anti-inflammatory, antioxidant, anti-tubercular, anti-malarial, anti-nociceptive (Ali et al, 2015, Asif et al, 2015aHavaldar and Patil, 2008;Ibrahim, 2009;Jadhav et al, 2009;Jordao et al, 2009.…”

Section: Introductionmentioning

confidence: 99%

Anti-neuropathic and anticonvulsant activities of various substituted triazoles analogues

Asif¹

2019

Preprint

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Various heterocyclic compounds along their derivatives were evaluated for their biological activities as antiviral, antitumor, anticonvulsant, antibacterial, antifungal, antituberculosis, analgesic, anti-inflammatory, antidiabetic, antihistamine and other biological activities. The triazole moiety seems to be very small, but in the biological profile has attracted the attention of many researchers to explore this skeleton to its multiple potential against several activities. The triazole derivatives possess a great importance in medicinal chemistry and can be used for the synthesis of numerous heterocyclic compounds with different biological activities. This review article covers the information of triazoles derivatives having different psychopharmacological actions. Thus triazole acts as a promising medicinal agent for the scientists working over this field. This review can be helpful to develop various more new compounds possessing triazoles moiety that could be better in terms of efficacy and lesser toxicity.

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“…1,2,4‐Triazole is an important template that is connected with several biological activities as antibacterial, anticholinergic, analgesic, and antiasthmatic . Likewise, triazoles are utilized in several antifungal medicines as well as fungicides . There is considerable interest in the chemistry of heterocyclic thiones, because they are ambidextrous or multifunctional donors with sulfur or nitrogen atom.…”

Section: Introductionmentioning

confidence: 99%

Synthetic Approach to Some New Annulated 1,2,4‐Triazine Skeletons with Antimicrobial and Cytotoxic Activities

Hamama

El‐Bana

Shaaban

et al. 2018

Journal of Heterocyclic Chem

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in Wiley Online Library (wileyonlinelibrary.com).The synthesis of some triazolotriazine, tetrazolotriazine, triazinotetrazine, and triazinotetrazepinoindole by the reaction of 4-amino-6-benzyl-3-hydrazinyl-1,2,4-triazin-5(4H)-one (2) with different reagents is described. The synthesized compounds were screened for their antimicrobial activity using the minimum inhibition concentration method by serial dilution technique. Two of these compounds showed higher activity than that of standard drug, and they were further evaluated for their cytotoxic activities against human cancer cells (MCF-7, HCT116, and HepG2), which indicate strong effect on these cancer cell lines. J. Heterocyclic Chem., 55, 971 (2018). and the carbonyl group of acid to form hydrazone intermediate, which underwent a cyclization reaction between the secondary amine and the hydroxyl group of the acid function affording 3, following pathway A. The constitution of 3 was deduced from its spectral data. Its 1 H NMR spectrum showed a singlet signal at δ = 2.49 and 6.05 ppm corresponding to CH 3 and NH 2 , Scheme 2. Action of 1,2-diketonic compounds on the triazino hydrazine derivative 2 to form the corresponding hydrazones 7, 8, 9, and 11. Scheme 1. Heterocyclization reaction of 2 with various reagents. Scheme 3. Alkylation of hydrazine derivative 2 with halo compounds. 972W.

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Synthesis and In Vitro Evaluation of Novel 1, 2, 4-Triazole Derivatives as Antifungal Agents

Cited by 30 publications

References 15 publications

Coumarin–triazole Hybrids and Their Biological Activities

Coumarin–triazole Hybrids and Their Biological Activities

Anti-neuropathic and anticonvulsant activities of various substituted triazoles analogues

Synthetic Approach to Some New Annulated 1,2,4‐Triazine Skeletons with Antimicrobial and Cytotoxic Activities

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