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Novel 3,4-Methylenedioxybenzene Scaffold Incorporated 1,3,5-Trisubstituted-2-pyrazolines: Synthesis, Characterization and Evaluation for Chemotherapeutic Activity.

Deshpande SR, Nagrale SN, Patil MV, Chavan PS - Indian J Pharm Sci (2015 Jan-Feb)

Bottom Line: A series of novel 3, 4-methylenedioxybenzene scaffold incorporated 1,3,5-trisubstituted-2-pyrazoline derivatives was synthesised as potent antitubercular agents via chalcone intermediates by reaction with hydrazines.The structures of the compounds were confirmed by IR, 1HNMR, 13CNMR and mass spectral data.All the compounds exhibited excellent activity that could be due to the presence of 3,4-methylenedioxybenzene frame work in the molecules.

View Article: PubMed Central - PubMed

Affiliation: Department of Medicinal and Pharmaceutical Chemistry, H. S. K. College of Pharmacy, BVVS Campus, Bagalkote-587 101, India.

ABSTRACT
A series of novel 3, 4-methylenedioxybenzene scaffold incorporated 1,3,5-trisubstituted-2-pyrazoline derivatives was synthesised as potent antitubercular agents via chalcone intermediates by reaction with hydrazines. The structures of the compounds were confirmed by IR, 1HNMR, 13CNMR and mass spectral data. The novel pyrazolines were screened for in vitro antitubercular activity by almar blue dye method against M. tuberculosis H37Rv. All the compounds exhibited excellent activity that could be due to the presence of 3,4-methylenedioxybenzene frame work in the molecules. Some of the compounds also showed in vitro cytotoxicity on EAC cell lines in tryphan blue exclusion assay suggesting their safety.

No MeSH data available.


Related in: MedlinePlus

Chemical structures of some antitubercular pyrazolines.
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Figure 1: Chemical structures of some antitubercular pyrazolines.

Mentions: The exploration of new heterocyclics that can accommodate potency to multiple biological targets remains a continuous intriguing scientific endeavor. Pyrazolines have been known to play an important role in medicinal chemistry. Diversely substituted pyrazoline derivatives embedded with variety of functional group are important biological agents[9] and have been found to exhibit diverse biological and pharmacological activities such as antibacterial[1011], antiamoebic[12], antidepressant[1314], antioxidant[1516], antiinflammatory[17], analgesic[18], hypotensive[19], anticoagulant[20], fungicidal and insecticidal[21] actions. Some pyrazoline derivatives possessing thiourea, 3-chloro-4-fluoro aniline[22] and quinoline moieties[23] (fig. 1) were also reported for good antitubercular activity.


Novel 3,4-Methylenedioxybenzene Scaffold Incorporated 1,3,5-Trisubstituted-2-pyrazolines: Synthesis, Characterization and Evaluation for Chemotherapeutic Activity.

Deshpande SR, Nagrale SN, Patil MV, Chavan PS - Indian J Pharm Sci (2015 Jan-Feb)

Chemical structures of some antitubercular pyrazolines.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4355879&req=5

Figure 1: Chemical structures of some antitubercular pyrazolines.
Mentions: The exploration of new heterocyclics that can accommodate potency to multiple biological targets remains a continuous intriguing scientific endeavor. Pyrazolines have been known to play an important role in medicinal chemistry. Diversely substituted pyrazoline derivatives embedded with variety of functional group are important biological agents[9] and have been found to exhibit diverse biological and pharmacological activities such as antibacterial[1011], antiamoebic[12], antidepressant[1314], antioxidant[1516], antiinflammatory[17], analgesic[18], hypotensive[19], anticoagulant[20], fungicidal and insecticidal[21] actions. Some pyrazoline derivatives possessing thiourea, 3-chloro-4-fluoro aniline[22] and quinoline moieties[23] (fig. 1) were also reported for good antitubercular activity.

Bottom Line: A series of novel 3, 4-methylenedioxybenzene scaffold incorporated 1,3,5-trisubstituted-2-pyrazoline derivatives was synthesised as potent antitubercular agents via chalcone intermediates by reaction with hydrazines.The structures of the compounds were confirmed by IR, 1HNMR, 13CNMR and mass spectral data.All the compounds exhibited excellent activity that could be due to the presence of 3,4-methylenedioxybenzene frame work in the molecules.

View Article: PubMed Central - PubMed

Affiliation: Department of Medicinal and Pharmaceutical Chemistry, H. S. K. College of Pharmacy, BVVS Campus, Bagalkote-587 101, India.

ABSTRACT
A series of novel 3, 4-methylenedioxybenzene scaffold incorporated 1,3,5-trisubstituted-2-pyrazoline derivatives was synthesised as potent antitubercular agents via chalcone intermediates by reaction with hydrazines. The structures of the compounds were confirmed by IR, 1HNMR, 13CNMR and mass spectral data. The novel pyrazolines were screened for in vitro antitubercular activity by almar blue dye method against M. tuberculosis H37Rv. All the compounds exhibited excellent activity that could be due to the presence of 3,4-methylenedioxybenzene frame work in the molecules. Some of the compounds also showed in vitro cytotoxicity on EAC cell lines in tryphan blue exclusion assay suggesting their safety.

No MeSH data available.


Related in: MedlinePlus