Novel 2-pyrazoline derivatives as potential antibacterial and antifungal agents

Kini, Suvarna G.; Gandhi, AM

doi:10.4103/0250-474x.40344

Cited by 40 publications

(28 citation statements)

References 5 publications

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“…The sterilized media was poured into Petri-plates 43,44 of 100 mm size. For each formulation, three plates were prepared and kept for solidifying.…”

Section: Ntifungal Activity In Vitro Cup Plate Methodsmentioning

confidence: 99%

Design Development and Evaluation of Topical Microemulsion

Muzaffar¹,

Singh²

2017

Int. Res. J. Pharm.

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A microemulsion based gel was designed for the topical and targeted delivery of sertaconazole nitrate for the treatment of su perficial fungal infection. The microemulsion region was obtained using a ternary diagram, different ratio of oil and Smix were used. The microemulsion of sertaconazole containing 2% (w/w) of sertaconazole, 6.67% (w/w) of oil phase (Eugenol+Oleic acid 1:1), 60.18% (w/w) of surfactant mixture 2:1 ratio (Tween-80 and Transcutol-P) and 33.15% (w/w) with distilled water. The prepared microemulsion gel and commercial cream of sertaconazole were evaluated for in-vitro and ex-vivo studies. The highest drug retention was achieved with Tween 80 and Transcutol P (T80TC45) when the optimized formulation was converted to a gel. The designed formulation MG2 was safe to be used over the skin as the PDI=0 when compared with commercial cream and MG1. The optimized formulation also posse's anti-inflammatory activity. The average zone of inhibition of MG2 was (23.19 ± 0.478) which was more than the commercial cream (15.34 ± 0.382) or MG1 (17.78 ± 0.715). Candida albicans which may be due to better permeation and retention effect of microemulsion gel 2. The MG2 was found to be stable after six month. The results obtained in this research from in vitro and in vivo data it can be concluded that the developed microemulsions have great potential for topical drug delivery in the treatment of inflammation and fungal infection.

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“…The sterilized media was poured into Petri-plates 43,44 of 100 mm size. For each formulation, three plates were prepared and kept for solidifying.…”

Section: Ntifungal Activity In Vitro Cup Plate Methodsmentioning

confidence: 99%

Design Development and Evaluation of Topical Microemulsion

Muzaffar¹,

Singh²

2017

Int. Res. J. Pharm.

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“…inflammatory 11,12 , anti-coagulant 13 , anti-amoebic 14 , antimalerial 15,16 , antibacterial 17 , anti-microbial 10,18 , analgesic 19 , cytotoxic 20 -21 , pesticide 22 and pesticidal and fungicidal activities 23 . Pyrimidine derivatives exhibited various biological activities such as anti-proliferative 24 , anticancer 25,26 , antihypertensive 27 , antioxidant 28,29 , antiviral 30 , antiinflammatory and analgesic activities 31,32 .…”

Section: Ijpsr (2018) Volume 9 Issue 2 (Research Article)mentioning

confidence: 99%

Untitled

2018

IJPSR

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ABSTRACT:In the present study eight novel 2-pyrazoline -amino pyrimidine hybrids have been synthesized in order to search new chemical entities with increased pharmacological properties. The targeted analogues were synthesized in four steps; Claisen-schmidt condensation of 4-nitro acetophenone with different benzaldehydes in basic medium to yield precursor chalcone which was cyclised using hydrazine hydrates and acetic acid to form 1-acetyl-2-pyrazoline. These were condensed with substituted benzaldehydes to give corresponding pyrazolyl chalcones, which were cyclised using guanidine carbonate to obtain 2-pyrazolineamino pyrimidine hybrids. All the synthesized compounds were characterized by elemental and spectral ( 1 H and 13 C NMR, FTIR and Mass) analysis. All the compounds have been screened for their antibacterial activity against gram positive bacteria (Bacillus substilis, Streptococcus aureus), gram negative bacteria (Pseudomonas aeruginosa, Escherichia coli) and antifungal activity against Aspergillus niger comparable to reference standard ciprofloxacin and fluconazole by agarwell diffusion method. All compounds 4(a-h) exhibited moderate to high activity and showed more pronounced antibacterial activity than antifungal activity. 4h showed dual effect antibacterial as well as antifungal agent.

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“…Moreover, pyrazolines and pyrazoles play a crucial role in the development of theory in heterocyclic chemistry and also are extensively used as useful synthons in organic synthesis [6]. 2-Pyrazolines and the corresponding pyrazoles have been shown to possess antitumor, anesthetic, analgesic, tranquilizer, muscle relaxant, antidepressant, neuroleptic, hypnotic, anticonvulsant, anti-inflammatory, antipyretic, antidiabetic, antiarrhythmic, antibacterial, antifungal, antiparasitic, antituberculosis, and insecticidal activities [7][8][9].…”

Section: Introductionmentioning

confidence: 99%