Jennifer Fernandes

SYNTHESIS AND BIOLOGICAL EVALUATION OF SOME NOVEL PYRAZOLINE DERIVATIVES DERIVED FROM N - SUBSTITUTED QUINOLINYL CHALCONES

A series of novel substituted 1 - amino - 3 - (5 - phenyl - 4, 5 - dihydro - 1 H - pyrazol - 3 - yl) quinolin - 2(1 H ) - one (AJP1 - AJP8) have been synthesized upon reaction with 1 amino - 3 - cinnamoyl - quinolin - 2(1 H ) - one by using hydrazine hydrate as cyclising medium in alcohol medium. 1 - amino - 3 - cinnamoyl - quinolin - 2(1 H ) - one were synthesized by condensing 3 - acetyl - 1 - amino - quinolin - 2 - one with different substituted benzaldehyde in presence of ethanolic KOH. The structures of the final synthesized compounds were con firmed by IR, 1 H NMR a nd mass spectra. The synthesized compounds were screened for their antibacterial and antifungal activity against Bacillus subtilis , Staphylococcus aureus , Escherichia coli , Pseudomonas aeruginosa and Candida albicans , Aspergillus nige r respectively by cup plate method. Compounds AJ P1 , AJ P3 , AJ P4 , AJ P5, AJP6 and AJ P7 showed good antibacterial activity compared to the standard drug amoxicillin. Compounds AJ P 1, AJ P 3, AJ P5 and AJ P 7 showed moderate antifungal activity compared to the standa rd drug fluconazole. The synthesized compounds were screened for their anti inflammatory activity by Carrageenan induced paw edema method. Compounds AJP1 and AJP7 showed significant anti - inflammatory activity compared to the standard drug diclofenac sodium .

Antihyperlipidemic activity of Achyranthes aspera Linn leaves on cholesterol induced hyperlipidemia in rats

Plants have been one of the important sources of medicines since the beginning of human civilization. Achyranthes aspera Linn. (A.aspera) belonging to family Amaranthaceae, commonly found in India. The plant is used as antiarthritic, purgative, diuretic and antimalarial etc. The antihyperlipidemic activity of alcoholic and aqueous extracts of leaves of A.aspera was evaluated using cholesterol induced hyperlipidemia in albino wistar rats. In this model, 8 groups consist of 6 animals per group. Group I and II were considered as saline and hyperlipidemic controls respectively, and groups III-VIII received respective treatment (ethanolic extract 250 mg, 500 mg, aqueous extract 250mg, 500 mg, Ayurvedic preparation and atorvastatin). All the groups received cholesterol (400 mg/kg b.w. p.o) except saline control for 4 weeks. The serum HDL, LDL, TG, and TC levels were analyzed in cholesterol induced hyperlipidemia where both the extracts of ethanolic and aqueous extract were shown antihyperlipidemic activity compared to hyperlipidemic control.

Synthesis and Antimicrobial Evaluation of Substituted Oxazolidinones Moieties

In order to develop relatively small molecules as pharmacologically active molecules, a series of oxazolidinones having benzo thiazinen moieties and their derivatives were synthesized, and characterized by IR, 1H NMR and Mass spectral studies. Oxazolidinones were prepared from R-glycidylbutarate and Para bromo aniline. Various substituted oxazolidinones benzo thiazinen were prepared by simple reflux in the presence of acetonitrile. Treatment of these oxazolidinones benzo thiazinen deravatives with methanesulfonyl gives its sulphonates derivatives on further treatment with sodium azide and tri phenyl phosphine in acetic anhydride to give its acetamide derivatives. All the newly synthesized compounds were evaluated for antibacterial activity against Bacillus subtilis, Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa.

Synthesis and in-Vitro Anti-Inflammatory Activity of Novel Pyrazoline Derivatives

A new series of Chalcones (2a-j) were prepared by reacting 2-acetyl Pyrrole and substituted ketones in alcohol medium in presence of NaOH. The Chalcones undergoes selective cyclization with phenoxy acetic acid hydrazide (1) in glacial acetic acid medium to yield the title compounds 1,3,5-trisubstituted Pyrazolines (3a-j). The newly synthesized compounds were evaluated for their In-vitro anti-inflammatory activity by egg albumin denaturation and protein denaturation method. All the new compounds were established on the basis of 1H-NMR, IR and Mass spectral data. Some of the tested compounds 3a, 3f showed good anti-inflammatory activity when compared to the standard drug diclofenac sodium.

Synthesis and Biological Evaluation of Some Novel Pyrazoline incorporated 2-Quinolones

A series of novel substituted 1-amino-3-(5-phenyl-4,5-dihydro-1H-pyrazol-3-yl)quinolin-2(1H)-one (AJP1-AJP8) have been synthesized upon reaction with 1-amino-3-cinnamoyl-quinolin-2(1H)-one using hydrazine hydrate as cyclising agent in alcohol medium. 1-amino-3-cinnamoyl-quinolin-2(1H)-one were synthesized by condensing 3-acetyl-1-amino-quinolin-2-one with different substituted benzaldehyde in presence of ethanolic KOH. The structures of the final synthesized compounds were characterized by IR, 1H NMR and mass spectra. The final synthesized compounds were screened for their antioxidant activity by DPPH radical scavenging method and in vitro cytotoxic activity against Ehrlich Ascites Carcinoma cells (EAC) by Trypan blue exclusion method.

SYNTHESIS AND EVALUATION OF OXAZOLIDINONES HAVING BENZO THIAZINEN MOIETI ES AS ANTIMICROBIAL AND ANTI - INFLAMMATORY AGENTS

Phenyl oxazolidinones were prepared from R - glycidyl butarate and Para bromo aniline, further (3 - (4 - bromophenyl) methylene oxazolidine - 5yl) and substituted benzothiazinen was refluxed resulted in oxazoli dinones benzothiazinen moieties. Treatment of these oxazolidinones benzo thiazinen moieties with methane sulfonyl gives its sulphonates on further treatment with sodium azide and tri phenyl phosphine in acetic anhydride gives acetamide derivatives . Further synthesized compounds were characterized by IR, H NMR 1 and Mass spectral studies. T he synthesized compounds were evaluated for antibacterial activity against Bacillus subtilis , Staphylococcus aureus , Escherichia coli , Pseudomonas aeruginosa and antifungal activity against , Candida albicans and Aspergillus