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  • Open access
  • 112 Reads
Synthesis of new pyrano[3,2-c]chromenes

The reaction of 4-hydroxy-7,7-dimethyl-7,8-dihydro-6H-chromen-2,5-dione with aldehydes and malononitrile afforded new pyrano[3,2-c]chromenes. Upon treatment of 4-hydroxy-7,7-dimethyl-7,8-dihydro-6H-chromen-2,5-dione  with anilines and triethyl orthoformate, new 3-anilinomethylidene 7,8-dihydro-2H-chromen-2,4,5(3H,6H)-triones were synthesized.

  • Open access
  • 92 Reads
Development of Triazine-4,6-diamines derivatives as potential Antimalarials: In-Silico Analysis

Development of 2, N6-disubstituted 1,2-dihydro-1,3,5-trizine-4,6-diamines derivatives were carried out by quantitative structure–activity relationship (QSAR) analyses. The nature of the substituent(s) on C-2; the nature of the substituent(s) on the distal aryl ring; as well as the nature and length of the flexible tether between the rings, to find out the structural requirements of their antimalarial activities against cycloguanil resistant (FCR-3) Plasmodium falciparum strain and sensitive to pyrimethamine. The statistically significant best 2D QSAR models for FCR-3, having correlation coefficient (r2) = 0.9821 and cross validated squared correlation coefficient (q2) = 0.6471 were developed by multiple linear regression stepwise (SW–MLR) forward algorithm. The results of the present study may be useful on the designing of more potent analogues as antimalarial agents.

  • Open access
  • 86 Reads
Preparation and Structural Assessment of Cocrystal Solvates and Cocrystal Salts of 1,3,5-Triazine-2,4,6-triamine with alpha-Hydroxycarboxylic Acids

In the present research, three cocrystals containing 1,3,5-triazine-2,4,6-triamine (melamine, me) were synthesized and characterized. The robustness of the amine-acid supramolecular synthon is discussed in the stoichiometry of the cocrystals of (me)·(H2ga)·1/2H2O (I), (me)·(Hme+)·(Hma-)·DMSO·3H2O (II) and (Hme+)·(Hma-)·diox·2H2O (III). The abbreviated designations used are glycolic acid (H2ga), mandelic acid (H2ma), dimethyl formamide (DMF), dimethyl sulfoxide (DMSO) and 1,4-Dioxane (diox). All the crystalline materials have been characterized by 1H-NMR, 13C-NMR, IR, and X-ray diffraction. The supramolecular assembly of each cocrystal is also analyzed and discussed.

  • Open access
  • 111 Reads
Forced degradation studies on Naratriptan HCL by High Performance Liquid Chromatography.

Naratriptan HCL is Anti Migraine Drug, the forced degradation studies of Naratriptan HCL were performed under acidic, basic, neutral, photolytic, and dry heat by High Performance Liquid Chromatography (HPLC). The drug was found to be unstable in alkaline medium as well as acidic medium compared to neutral conditions. The drug showed degradation in 8 hr at 60ºC when the studies were carried under 0.01N NaOH, while drug showed the degradation in 0.01N HCL when it was subjected to reflux for 2 hours at 60º C. Same retention time of degradant was also observed in neutral conditions, when drug was allowed to reflux in water for 8 hours at 100º C. Drug was found to be stable in 50% H2O2. Drug was also found to be stable in other conditions such as photolytic and dry heat. Suitable mobile phase was developed and separation of drug and degradant was achieved using isocratic elution. The method was developed on C-18 column using acetonitrile : water as a mobile phase in the ratio of 50:50, 100 µl of the sample were injected in the system for chromatographic Analysis,  the selected wavelength was 223 nm and flow rate was 1ml/min.

  • Open access
  • 121 Reads
Ultrasound assisted synthesis of 4-(benzyloxy)-N-(3-chloro-2-(substituted phenyl)-4-oxoazetidin-1-yl) benzamide

: A series of 4-(benzyloxy)-N-(3-chloro-2-(substituted phenyl)-4-oxoazetidin-1-yl) benzamide 6a-j were synthesized in good yield from Schiff bases by cyclo-condensation with chloro acetyl chloride in the presence of catalyst tri ethylamine and solvent DMF by using ultra-sonication as one of the green chemistry tool. Synthesis of these derivatives by a conventional method like stirring at room temperature required 20–28 hr and by refluxing nearly takes 8–10 hr whereas using ultra-sonication it requires only 2h for completion of reaction. The use of ultrasound to promote chemical reactions is called sono-chemistry, it is complementary technique for promoting chemical reactions by ecofriendly green synthetic protocol. Ultrasound assisted synthesis are used to reduce the amount of undesired hazardous chemicals and solvents, reduce energy consumption and increase the selectivity towards the given product. Schiff bases are the compounds carrying imine or azomethine (–C=N–) functional group in which the electrophilic carbon and nucleophilic nitrogen confers the Schiff bases possibility to interact with several biological targets and have gained importance in medicinal and pharmaceutical fields exhibiting broad spectrum of biological activities. These key compounds 4-(benzyloxy)-N'-(substituted benzylidene) benzo hydrazide i.e Schiff bases 5a-j were obtained by condensation 4-(benzyloxy)benzo hydrazide with various aromatic aldehydes. The four-membered cyclic amides commonly known as 2-azetidinones or β-lactam occupy an eminent place in organic and medicinal chemistry since the structure of penicillin showed the presence of β-lactam ring in it and various potent activities of penicillin are due to the presence of β-lactam ring.  Azetidinones are known to exhibit various biological activities like anti-tubercular, antibacterial and antifungal with β-lactam ring. Hence we are introducing the eco-friendly protocol for the synthesis of substituted azetidinone derivatives. All the synthesized compounds were characterized by FTIR, 1HNMR, 13CNMR and mass spectral analysis.

  • Open access
  • 117 Reads
Microwave-Assisted Facile Synthesis and anticonvulsant evaluation of Novel N-(3-chloro-2-oxo-4-substituted phenyl azetidin-1-yl)-2-(1, 3-dioxoisoindolin-2-yl) acetamides

Herewith, we report the design and synthesis of a series of N-(3-chloro-2-oxo-4-substituted phenyl azetidin-1-yl)-2-(1,3-dioxoisoindolin-2-yl)acetamide 7(a-l) derivatives, obtained by condensation of Schiff’s base and chloroacetyl chloride in dimethyl formamide as solvent and few drops of triethyl amine as a catalyst under microwave irradiation for about 3-4 min (700 W) at 800C based on four component pharmacophoric model to get structural prerequisite indispensable for anticonvulsant activity. The synthesized derivatives were investigated for CNS depressant, maximal electroshock seizure (MES), subcutaneous pentylenetetrazole (sc-PTZ) induced seizure and neurotoxicity screening. Most of the compounds were found to be potent in MES model. The anticonvulsant screening data shows that 65% of the compounds were found to be active against MES model when compared to 35% sc-PTZ model.

  • Open access
  • 126 Reads
Design and Characterization of Polymeric Floating Microspheres of Levofloxacin Hemihydrate.

The complex of Levofloxacin and Chitosan lead to formation of water soluble complex. This complex of Levofloxacin was then formulated into floating beads calcium alginate  with maximum entrapment of Levofloxacin found to be about 75 %( f10) and the entrapment was found to be significantly higher as compared to the other formulations ( f1 to f9). In- Vitro Release studies of the beads f10 was found to significantly improve the release of Levofloxacin as compared to other formulations.. The mean particle size of f10 microspheres and surface morphology were determined by SEM Resulting in Porous and Rough Surface of microspheres.The drug release kinetics were studied as zero order, first order , Higuchi , Koresmeyer-Peppas equations , good  linearity was found in Higuchi’s Equation (R2= 0.9310) indicating the release of the drug from Microspheres is  based on Fickian Diffusion .

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