New heterocyclic hybrids of pyrazole and its bioisosteres: Design, synthesis and biological evaluation as dual acting antimalarial-antileishmanial agents

“…7,8 Pyrazole 1 is known to be one of the most potential families of nitrogen-containing compounds. Pyrazole derivatives exhibit a broad spectrum of biological profiles, for instance, anti-tubercular, 9 anti-AIDS, 10 anti-malarial, 8 * For correspondence anti-microbial, 11 antitumor, 12,13 anticancer 14 and antifungal. 6 In addition, pyrazoles have also been found as promising anti-hyperglycemic, 15 anti-depressant, 16 anti-convulsant, 17 anti-pyretic, 18 anti-anxiety 19,20 and insecticidal agents.…”

Section: Introductionmentioning

confidence: 99%

Recent developments in synthetic chemistry and biological activities of pyrazole derivatives

et al. 2019

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Pyrazole, a five-membered heterocycle containing two nitrogen atoms, is extensively found as a core framework in a huge library of heterocyclic compounds that envelops promising agro-chemical, fluorescent and biological potencies. Attributed to its several potential applications, there is a rise in the significance of designing novel pyrazoles, disclosing innovative routes for synthesizing pyrazoles, examining different potencies of pyrazoles, and seeking for potential applications of pyrazoles. This review consists of two parts. The first part provides an overview on the recent developments in synthetic approaches to pyrazoles, which is related to the new or advanced catalysts and other 'environment-friendly' procedures, including heterogeneous catalytic systems, ligand-free systems, ultrasound and microwave-assisted reactions. The second part focuses on the recently reported novel biological affinities of pyrazoles. This systematic review covers the published studies from 1990 to date. It is expected that this review will be helpful in future research and for new thoughts in the quest for rational designs for developing more promising pyrazoles.

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“…[26] To synthesize functionalized Michael adducts a simple and novel route was established by Michael addition of dimedone with chalcones. [27] Michael addition of chalcones with pyrazolin-5-one, for the synthesis of 4-alkyl-1H-pyrazoles have attracted attention due to their biological activities like, antioxidant, [28] antimicrobial, [29] analgesic, [30] anticancer, [31] antimalarial, [32] anti-inflammatory [33] and antiallergic [34] properties. Further, 4-alkyl-1H-pyrazoles act as potential inhibitors of hepatitis C virus (HCV) replication, [35] selective inhibitory activity against COX-2 enzyme, [36] partial antagonists for the nicotinic acid receptor, [37] anti-HIV agents, [38] and p38 kinase inhibitors.…”

Section: Introductionmentioning

confidence: 99%

l‐Proline Catalyzed Synthesis of Highly Functionalized 4‐Hydroxy‐4H‐chromene‐pyrazoles and 4‐Hydroxy‐4H‐chromene‐barbiturates in Aqueous Medium

Reddy

Sumathi

2020

ChemistrySelect

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A simple and efficient method for the synthesis of novel 4‐hydroxy‐4H‐chromene‐pyrazoles and 4‐hydroxy‐4H‐chromene‐barbiturates was developed from the reaction of 2‐ethoxy‐2H‐chromene chalcones with pyrazolin‐5‐one and barbituric acid catalyzed by l‐proline in water. The developed protocol is applicable for the construction of biologically important 4H‐chromenes from easily accessible chalcones having various substituents. This reaction proceeds through Aldol condensation, Michael addition and hydrolysis reactions followed by the elimination of ethoxy group. This methodology offers cleaner conversion, a shorter reaction time and high yields. For the first time, we report the synthesis of novel 4‐hydroxy‐4H‐chromenes from 2‐ethoxy‐2H‐chromene chalcones and pyrazolin‐5‐one/barbituric acid using l‐proline (72–86 % yield in 6 h). Water was used as the solvent for all the compounds it represents a green synthetic protocol.

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New heterocyclic hybrids of pyrazole and its bioisosteres: Design, synthesis and biological evaluation as dual acting antimalarial-antileishmanial agents

Cited by 119 publications

References 51 publications

Synthesis and Antiproliferative Activity of Thiadiazole Peptidomimetic Derivatives

Synthesis and Antiproliferative Activity of Thiadiazole Peptidomimetic Derivatives

Recent developments in synthetic chemistry and biological activities of pyrazole derivatives

l‐Proline Catalyzed Synthesis of Highly Functionalized 4‐Hydroxy‐4H‐chromene‐pyrazoles and 4‐Hydroxy‐4H‐chromene‐barbiturates in Aqueous Medium

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