Synthesis of novel α-pyranochalcones and pyrazoline derivatives as Plasmodium falciparum growth inhibitors

Wanare, Gajanan; Aher, Rahul Balasaheb; Kawathekar, N.; Ranjan, Ravi; Kaushik, Neeraj; Sahal, Dinkar

doi:10.1016/j.bmcl.2010.05.069

Cited by 80 publications

(32 citation statements)

References 27 publications

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“…Le profil hybride de la chalcone serait favorable à une meilleure activité sur les isolats de P. falciparum chloroquinorésistants. Une telle inversion d'efficacité antiplasmodiale a également été observée par Wanare et al (2010) au cours de leur étude sur d'autres hybrides de chalcone. Un début d'explication pourrait venir de leur possible spécificité d'action vis-à-vis des facteurs de résistances plutôt que ceux à l'origine de la sensibilité des plasmodies aux médicaments antipaludiques.…”

Section: Niveau D'activité Antiplasmodiale Des Benzimidazolyl-chalconesunclassified

Synthèse et criblage antiplasmodial de quelques benzimidazolyl-chalcones

Ouattara¹,

Sissouma²,

Yavo³

et al. 2015

Int. J. Bio. Chem. Sci

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Section: Niveau D'activité Antiplasmodiale Des Benzimidazolyl-chalconesunclassified

Synthèse et criblage antiplasmodial de quelques benzimidazolyl-chalcones

Ouattara¹,

Sissouma²,

Yavo³

et al. 2015

Int. J. Bio. Chem. Sci

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“…α-pyranopyrazoline analogues were synthesized and evaluated for antimalarial activity, compound 21 turned to be the most potent analog of the series having IC 50 3.1 µg/mL against chloroquine-sensitive strain 3D7 and IC 50 of 1.1 µg/mL against chloroquine-resistant strain RKL9. To support the data further docking was done into the active site of falciparum enzyme which showed good interaction with the active site residue [35]. 2-pyrazoline and pyrazoles synthesized as celecoxib analogues and evaluated for in vitro COX-1/COX-2 inhibitory activity compound 22 was most selective COX-2 inhibitor [36].…”

Section: Analogues Of Chalcones Pyrazoline Analogues With Various Phamentioning

confidence: 99%

Chalconoid Derived Heterocycles as Potent Bioactive Molecules: A Review

Sapra¹,

Sharma²

2016

Chem Sci J

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Although chalcones symbolize an important pharmacophore for variety of biological actions, however their analogues are also reported to be equally important for plethora of biological actions. In the present review, a comprehensive study of chalcones derived molecules (like pyrazoles, isoxazoles, pyridine, pyrimidine) their pharmacological actions, mechanism of action, structure activity relationship studies have been described. which includes anti-proliferative, anti-inflammatory, antioxidant, proapoptotic, anti-bacterial and anti-adhesive effects [18]. Analogues of chalcones Pyrazoline analogues with various pharmacological activities:Pyrazole nucleus present in compounds exhibit wide range of biological activity. Introduction of a pyrazole ring in the chalcones between the two aryl rings increase the cytotoxic activity against a series of human cancer cell lines. Dhar et al. [19] synthesized a series of 1-acetyl-3,5-diaryl-4,5-dihydro-(H)-pyrazoles and assayed for in vitro cytotoxicity against PC-3, OVCAR, IMR-32, HEP-2 human cancer cell lines, compound 1 showed broad spectrum cytotoxic activity against all the four cell lines. The activity shown by the compounds conclude that (i) Substitution on phenyl ring showed marked effect on cytotoxic activity, (ii) Presence of electron donating groups on phenyl ring led to enhanced activity whereas electron withdrawing group except NO 2 reduces the cytotoxic activity, (iii) Replacement of phenyl ring with heterocyclic ring also reduces the cytotoxic potential and napthyl ring on both sides are more beneficial for cytotoxic potential Chemical Sciences JournalChem ic a l S cience s J o u rnal

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“…The antibacterial activity 18 of the five copolyesters PSGH, PSOH, PSIH, PSOM and PSGM were assayed against (Staphylococcus aureus, Bacillus subtillus, Klebsilla pnemoniae, Pseudomonas aeruginosa & amp; Escherichia coli by disc diffusion method 19 . Streptomycin inhibited the escalation of Staphylococcus aureus by 20mm, Enterrococcus faecalis.…”

Section: Bactericidal Studymentioning

confidence: 99%

Untitled

2016

IJPSR

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Two chalcone diols (2E)-1-(4-hydroxyphenyl)-3(4-hydroxy, 3-ethoxy phenyl) prop-en-1-one and (2E)-1-(4-hydroxy-3-methoxy phenyl)-3(4-hydroxy, 3-ethoxy phenyl) prop-en-1-one were synthesized by acid catalyzed ClaisenSchmidt reaction. The synthesized chalcones were made to undergo polymerization using three aliphatic dichlorides namely glutaryl, succinyl and oxalyl chlorides. The polymers were random copolyesters and characterized by solubility and viscosity measurement. The structure of the copolyester was established by FTIR,

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Synthesis of novel α-pyranochalcones and pyrazoline derivatives as Plasmodium falciparum growth inhibitors

Cited by 80 publications

References 27 publications

Synthèse et criblage antiplasmodial de quelques benzimidazolyl-chalcones

Synthèse et criblage antiplasmodial de quelques benzimidazolyl-chalcones

Chalconoid Derived Heterocycles as Potent Bioactive Molecules: A Review

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