Papers by Sabarimuthu DarlinQuine
OBJECTIVE: A series of ten novel derivatives of 3-substituted-2-thioxoquinazolin-4(3H)-ones have ... more OBJECTIVE: A series of ten novel derivatives of 3-substituted-2-thioxoquinazolin-4(3H)-ones have been synthesized from anthranilic acid via Mannich reaction with various secondary amines in presence of formaldehyde in ice cold condition. MATERIALS AND METHODS: The structure of these compounds have been elucidated by spectral (FTIR, 1H-NMR and mass) analysis. The titled compounds were evaluated for antimicrobial and anticonvulsant activities. Antimicrobial activities were determined by cup plate method and MIC values using the micro dilution broth method against two Gram positive bacteria Staphylococcus aureus and Streptococcus aureus, two Gram negative bacteria Escherichia coli and Proteus vulgaris and against two fungi Candida albicans and Aspergillus niger. Amikacin and fluconazole were used as standard antibacterial and antifungal agents in the concentration of 10 µg/disc 20 µg/disc respectively. RESULTS AND CONCLUSIONS: Amongst the compounds tested, compound 2-(2,3-dimethylphenyl) (3-(4-ethoxyphenyl)-4-oxo-2thioxo-3,4-dihydroquinazolin-1-2H)-1ylmethyl amino)benzoic acid (PTQ-03) and 2-((2,3-dimethylphenyl)((3-(4-ethoxyphenyl)-4-oxo-2t h i o x o-3 , 4-d i h y d r o q u i n a z o l i n-1 (2 H)yl)methyl)amino)benzoic acid (ETQ-03) showed broad spectrum of activity against all the tested Gram positive bacteria, Gram negative bacteria and the fungi. Anti-convulsant activity of the compounds was evaluated by maximal electro shock (MES) convulsion method. The compounds sodium 2-(2-((2,6-Dichlorophenyl)(3-(4oxo-2-thioxo-3,4-dihydroquinazolin-1(2H)yl)methyl)amino) phenyl acetate (PTQ-04) and N-(4-Hydroxyphenyl)-N-((3-naphthalen-2-yl)-4-oxo-2-t h i ox o-3 , 4-d i hy d o rq u i n a z o l i n-1 (2 H)-y lmethyl)acetamide (NTQ-01) showed potent anticonvulsant activity.
Pharmaceutical Biology, Aug 13, 2012
Blepharis maderaspatensis L. Roth (BM) (Acanthaceae) and Ammannia baccifera L. (AB) (Lythraceae) ... more Blepharis maderaspatensis L. Roth (BM) (Acanthaceae) and Ammannia baccifera L. (AB) (Lythraceae) are used in folk medicine for various stomach disorders. The chloroform and ethanol extracts of both plants were evaluated for antioxidant, gastric antisecretory, and gastroprotective properties. Antioxidant properties of the extracts were evaluated using 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay and nitric oxide (NO) scavenging assay. The gastric antisecretory properties of the extracts were assessed, at a dose of 100 and 200 mg/kg, using aspirin-pylorus ligation induced gastric ulcer models and the gastroprotective activity of the extracts was assessed, at a dose of 100 and 200 mg/kg, using HCl-ethanol induced ulcer models in rats. Ethanol extract of BM (EBM) possessed good antioxidant property with IC₅₀ values of 37.4 and 44.1 µg/mL in DPPH and NO scavenging assays respectively, where 25-250 µg/mL concentration in DPPH assay and 30-300 µg/mL concentration in NO scavenging assay were used. Ethanol extract of AB (EAB) at a dose of 200 mg/kg reduced the free acidity to 142.66 mEq/L and total acidity to 451.22 mEq/L. It reduced the gastric secretion with increase in pH from 2.2 to 3.15. Possessing good antisecretory activity, it also reduced the ulcer by 92.2% in aspirin and pylorus ligation induced gastric ulcer models. EAB increased the mucus secretion and adherent mucus in the tissues with a 71.43% reduction of ulcerin HCl-ethanol induced ulcer models, at a dose of 200 mg/kg. This activity can be attributed to the various flavonoids like rutin and kaempferol-3-O-β-glucopyranoside, and the phytosterol, β-sitosterol-3-O-β-glucopyranoside, and phenolics present in the extracts. EBM possessed significant antioxidant property while EAB possessed good antisecretory and gastroprotective activity.
PubMed, 2013
Objective: A series of ten novel derivatives of 3-substituted-2-thioxoquinazolin-4(3H)-ones have ... more Objective: A series of ten novel derivatives of 3-substituted-2-thioxoquinazolin-4(3H)-ones have been synthesized from anthranilic acid via Mannich reaction with various secondary amines in presence of formaldehyde in ice cold condition. Materials and methods: The structure of these compounds have been elucidated by spectral (FTIR, 1H-NMR and mass) analysis. The titled compounds were evaluated for antimicrobial and anticonvulsant activities. Antimicrobial activities were determined by cup plate method and MIC values using the micro dilution broth method against two Gram positive bacteria Staphylococcus aureus and Streptococcus aureus, two Gram negative bacteria Escherichia coli and Proteus vulgaris and against two fungi Candida albicans and Aspergillus niger. Amikacin and fluconazole were used as standard antibacterial and antifungal agents in the concentration of 10 µg/disc 20 µg/disc respectively. Results and conclusions: Amongst the compounds tested, compound 2-(2,3-dimethylphenyl) (3-(4-ethoxyphenyl)-4-oxo-2-thioxo-3,4-dihydroquinazolin-1-2H)-1ylmethyl amino)benzoic acid (PTQ-03) and 2-((2,3-dimethylphenyl)((3-(4-ethoxyphenyl)-4-oxo-2-thioxo-3,4-dihydroquinazolin-1(2H)-yl)methyl)amino)benzoic acid (ETQ-03) showed broad spectrum of activity against all the tested Gram positive bacteria, Gram negative bacteria and the fungi. Anti-convulsant activity of the compounds was evaluated by maximal electro shock (MES) convulsion method. The compounds sodium 2-(2-((2,6-Dichlorophenyl)(3-(4-oxo-2-thioxo-3,4-dihydroquinazolin-1(2H)-yl)methyl)amino) phenyl acetate (PTQ-04) and N-(4-Hydroxyphenyl)-N-((3-naphthalen-2-yl)-4-oxo-2-thioxo-3,4-dihydorquinazolin-1(2H)-ylmethyl)acetamide (NTQ-01) showed potent anticonvulsant activity.
African Journal of Pharmacy and Pharmacology, Oct 8, 2013
The present study evaluates anti-hyperlipidaemic and anti-atherogenic activities in Triton WR-133... more The present study evaluates anti-hyperlipidaemic and anti-atherogenic activities in Triton WR-1339 and high cholesterol diet induced hyperlipidemia in rat models. Chloroform, ethyl acetate and ethanol extracts of whole plant of Blepharis maderaspatensis were evaluated for their anti-hyperlipidaemic and anti-atherogenic activities using Triton WR-1339 induced hyperlipidaemic rats (acute study) and high cholesterol diet induced (chronic study) experimental models. Hyperlipideamia was developed by intraperitonial injection of Triton WR-1339 (200 mg/kg body weight) in acute study and feeding with cholesterol rich diet in chronic study. The animals were divided into various groups and intragastric administration of various extracts of B. maderaspatensis (100 mg/kg) body weight was given in both models. After the completion of the treatment, they were evaluated for serum total cholesterol, triglycerides, high density lipoprotein (HDL), low density lipoprotein (LDL), very low density lipoprotein (VLDL), atherogenic index (AI), coronary risk index (CRI) and were compared with the rats treated with simvastatin (20 mg/kg) of the body weight. Pre-treatment of ethanol extracts of B. maderaspatensis significantly reduced the serum total cholesterol, triglycerides, LDL, VLDL, AI and CRI as comparable with simvastatin.
Journal of the Pharmaceutical Society of Japan, Jul 1, 2011
A series of 3-substituted-2-thioxoquinazolin-4(3H)-one derivatives have been synthesized and thei... more A series of 3-substituted-2-thioxoquinazolin-4(3H)-one derivatives have been synthesized and their structures have been elucidated on the basis of IR, 1 H-NMR, elemental analysis and mass spectroscopic studies. Anti-in‰ammatory and analgesic activity of the synthesized compounds was evaluated by Carrageenan induced rat paw edema method and Eddy's hot plate method respectively. Among the synthesized compounds N-(4-hydroxyphenyl)-N-(4-oxo-3-phenyl-2thioxo-3,4-dihydroquinazolin-1(2H)methyl)acetamide (PTQ01) showed excellent anti-in‰ammatory activity. N-(4ethoxyphenyl)-N-(3-(naphthalen-2yl)-4-oxo-2-thioxo-3,4-dihydroquinazolin-1(2H)-yl)methyl)acetamide (NTQ02), N-(4-Hydroxyphenyl)-N-((3-naphthalen-2-yl)-4-oxo-2-thioxo-3,4-dihydorquinazolin-1 (2H)-ylmethyl) acetamide (NTQ01), N-((3-(4-ethoxyphenyl)-4-oxo-2-thioxo-3,4-dihydoquinazolin-1(2H)-yl)methyl)-N-(4-hydroxyphenyl)acetamide (ETQ01) N-(3-(4-ethoxyphenyl)-4-oxo-2thioxo-3,4-dihydroquinazolin-1(2H)-ylmethyl)-N-(4-hydroxyphenyl) acetamide (ETQ04), N-(4-ethoxyphenyl)-N-((4-oxo-3-phenyl-2-thioxo-3,4-dihydoquinazolin-1(2H)-yl)methyl)acetamide (PTQ02) and N-(4-ethoxyphenyl)-N-(3-(4-ethoxyphenyl)-4-oxo-2-thioxo-3,4-dihydoquinazolin-1(2H)-yl) methyl)acetamide (ETQ02) at a dose of 20 mg/kg exhibited signiˆcant anti-in‰ammatory activity compared to that of standard drug diclofenac sodium. The compound 2-(2,3-dimethylphenyl)(3-(4-ethoxyphenyl)-4-oxo-2-thioxo-3,4-dihydroquinazolin-1-2H)-1ylmethylamino)benzoic acid PTQ03 and sodium 2-(2-((2,6-dichlrophenyl)(3-(4-oxo-2-thioxo-3,4-dihydroquinazolin-1(2H)-yl)methyl)amino)phenylacetate (PTQ04) showed moderate anti-in‰ammatory activity. The compounds PTQ01, PTQ02, PTQ04, ETQ01 and ETQ02 showed signiˆcant analgesic activity compared with that of standard drug pentazocin.
Revista Brasileira de Farmacognosia, 2012
Wound healing activity of the leaf extracts of Ammannia baccifera L., Lythraceae, and Blepharis m... more Wound healing activity of the leaf extracts of Ammannia baccifera L., Lythraceae, and Blepharis maderaspatensis (L.) B.Heyne ex Roth., Acanthaceae, was investigated by excision and incision wound healing models in rats. A phytochemical screening was done to determine the major constituents of the chloroform, ethyl acetate and ethanolic fractions of ethanolic leaf extracts. The excision and incision models were used to assess the effect of the plant extracts on wound healing in rats. Phytochemical screening reveals the presence of tannins, saponins, steroids, terpenoids, and flavonoids in the extract. The wound healing effect was comparatively evaluated with a standard drug Framycetin cream. Significant wound healing activity was observed for the creams prepared with 5% ethanol fraction of B. maderaspatensis and 5% chloroform fraction of A. baccifera ethanolic leaf extracts. The results of histopathological evaluation supported the outcome of both incision and excision wound models. Ethanolic fraction of B. maderaspatensis and chloroform fraction of A. baccifera exhibited marked wound healing activity. B. maderaspatensis extract displayed a remarkable wound healing activity compared to A. baccifera.
Pharmaceutical Biology, 2012
Blepharis maderaspatensis L. Roth (BM) (Acanthaceae) and Ammannia baccifera L. (AB) (Lythraceae) ... more Blepharis maderaspatensis L. Roth (BM) (Acanthaceae) and Ammannia baccifera L. (AB) (Lythraceae) are used in folk medicine for various stomach disorders. The chloroform and ethanol extracts of both plants were evaluated for antioxidant, gastric antisecretory, and gastroprotective properties. Antioxidant properties of the extracts were evaluated using 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay and nitric oxide (NO) scavenging assay. The gastric antisecretory properties of the extracts were assessed, at a dose of 100 and 200 mg/kg, using aspirin-pylorus ligation induced gastric ulcer models and the gastroprotective activity of the extracts was assessed, at a dose of 100 and 200 mg/kg, using HCl-ethanol induced ulcer models in rats. Ethanol extract of BM (EBM) possessed good antioxidant property with IC₅₀ values of 37.4 and 44.1 µg/mL in DPPH and NO scavenging assays respectively, where 25-250 µg/mL concentration in DPPH assay and 30-300 µg/mL concentration in NO scavenging assay were used. Ethanol extract of AB (EAB) at a dose of 200 mg/kg reduced the free acidity to 142.66 mEq/L and total acidity to 451.22 mEq/L. It reduced the gastric secretion with increase in pH from 2.2 to 3.15. Possessing good antisecretory activity, it also reduced the ulcer by 92.2% in aspirin and pylorus ligation induced gastric ulcer models. EAB increased the mucus secretion and adherent mucus in the tissues with a 71.43% reduction of ulcerin HCl-ethanol induced ulcer models, at a dose of 200 mg/kg. This activity can be attributed to the various flavonoids like rutin and kaempferol-3-O-β-glucopyranoside, and the phytosterol, β-sitosterol-3-O-β-glucopyranoside, and phenolics present in the extracts. EBM possessed significant antioxidant property while EAB possessed good antisecretory and gastroprotective activity.
African Journal of Pharmacy and Pharmacology, 2013
The present study evaluates anti-hyperlipidaemic and anti-atherogenic activities in Triton WR-133... more The present study evaluates anti-hyperlipidaemic and anti-atherogenic activities in Triton WR-1339 and high cholesterol diet induced hyperlipidemia in rat models. Chloroform, ethyl acetate and ethanol extracts of whole plant of Blepharis maderaspatensis were evaluated for their anti-hyperlipidaemic and anti-atherogenic activities using Triton WR-1339 induced hyperlipidaemic rats (acute study) and high cholesterol diet induced (chronic study) experimental models. Hyperlipideamia was developed by intraperitonial injection of Triton WR-1339 (200 mg/kg body weight) in acute study and feeding with cholesterol rich diet in chronic study. The animals were divided into various groups and intragastric administration of various extracts of B. maderaspatensis (100 mg/kg) body weight was given in both models. After the completion of the treatment, they were evaluated for serum total cholesterol, triglycerides, high density lipoprotein (HDL), low density lipoprotein (LDL), very low density lipoprotein (VLDL), atherogenic index (AI), coronary risk index (CRI) and were compared with the rats treated with simvastatin (20 mg/kg) of the body weight. Pre-treatment of ethanol extracts of B. maderaspatensis significantly reduced the serum total cholesterol, triglycerides, LDL, VLDL, AI and CRI as comparable with simvastatin.
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Papers by Sabarimuthu DarlinQuine