NISCAIR Online Periodicals Repository Collection: IJC-B Vol.51B(11) [November 2012]

Design, synthesis, biological evaluation of thiazolyl schiff base derivatives as novel anti-inflammatory agents

Title: Design, synthesis, biological evaluation of thiazolyl schiff base derivatives as novel anti-inflammatory agents

Authors: Bhosale, P P; Chavan, R S; Bhosale, A V

Abstract: A series of new 4-(4-substitutedphenyl)-N-(4-substitutedbenzylidene)-thiazol-2-amine derivatives 5a-l has been synthesized and evaluated for their anti-inflammatory and analgesic activities at a dose of 50 mg/kg p.o. The most active compounds 5a, 5j have been subjected to acute ulcerogenesis study at a dose of 150 mg/kg. The structure of all these compounds have been established on the basis of spectral (IR, ¹H NMR data) studies.

Page(s): 1649-1654

Synthesis, characterization and antimicrobial screening of some novel chalcones and their derivatives

Title: Synthesis, characterization and antimicrobial screening of some novel chalcones and their derivatives

Authors: Chate, Asha V; Joshi, Ratnadeep S; Mandhane, Priyanka G; Gill, Charansingh H

Abstract: Synthesis of some novel 2-(4-(allyloxy)-3-methoxyphenyl)-4H-chromen-4-ones 5a-f and 2-(4-(allyloxy)-3-methoxyphenyl)-3-chloro-4H-chromen-4-ones 6a-f by oxidative cyclisation of (E)-3-(4-allyloxy)-3-methoxyphenyl)-1-(2-hydroxyphenyl)prop-2-en-1-ones using DMSO/I₂ and DMSO/CuCl₂ at reflux condition has been carried out. A useful and efficient synthetic strategy for the synthesis of 4-allyloxy-3-methoxyphenyl chromones has been reported. The synthesized compounds have been characterized by melting point, FT-IR, NMR and EI-MS spectral data. The synthesized compounds have been evaluated for their antibacterial and antifungal activities. Most of the compounds are found to be of comparable potency when compared with the reference standard drugs.

Page(s): 1642-1648

Synthesis and antimicrobial activity studies of certain pyrimidinyl oxadiazolo azetidinones

Title: Synthesis and antimicrobial activity studies of certain pyrimidinyl oxadiazolo azetidinones

Authors: George, Sonia; Sabitha, R; Govindhammal, V; Ravi, T K

Abstract: Aryl substituted pyrimidinyl oxadiazolo azetidinones have been synthesized from ethyl 6-methyl-2-oxo-4-phenyl-1,2,3,4-tetrahydropyrimidine-5-carboxylate 1 which on reaction with semicarbazide hydrochloride in ethanol yields 2-[(6-methyl-2-oxo-4-phenyl-1,2,3,4-tetrahydropyrimidin-5-yl)carbonyl]hydrazinecarboxamide 2. Compound 2, on reaction with concentrated sulphuric acid, undergo cyclization to yield 5-(5-amino-1,3,4-oxadiazol-2-yl)-6-methyl-4-phenyl-3,4-dihydropyrimidin-2(1H)-one 3. Further, compound 3, on treatment with appropriate aldehydes, in ethanol give 6-methyl-4-phenyl-5-(5-{[(1E)-arylmethylidene]amino}-1,3,4-oxadiazol-2-yl)-3,4-dihydropyrimidin-2(1H)-ones 4a-e. Finally, the title compounds 5-[5-(3-chloro-2-oxo-4-arylazetidin-1-yl)-1,3,4-oxadiazol-2-yl]-6-methyl-4-phenyl-3,4-dihydropyrimidin-2(1H)-ones 5a-e have been obtained by ring closure of the compounds 4a-e with monochloroacetyl chloride in dioxane in the presence of triethylamine. The structures of the novel compounds are assigned based on IR, ¹H NMR, mass spectral data and elemental analysis data. All the compounds have been screened for their antimicrobial activity using bacterial and fungal strains.

Page(s): 1637-1641

Development of HPLC method for simultaneous estimation of ambroxol, guaifenesin and salbutamol in single dose form

Title: Development of HPLC method for simultaneous estimation of ambroxol, guaifenesin and salbutamol in single dose form

Authors: Dubey, Nidhi; Sahu, Sandeep; Singh, G N

Abstract: A simple, accurate and precise High Performance Liquid Chromatographic (HPLC) method has been developed for simultaneous determination of ambroxol, guaifenesin and salbutamol in single dosage form. The method has been validated as per the guidelines of ICH and FDA. The finalized Reverse Phase–HPLC method is revealed with significant shorter retention time of 15 min with simple isocratic program. The separation is achieved on C- 8, 5μm; 250 mm × 4.6 mm column with flow rate 1.0 mL per minute in isocratic mode using disodium hydrogen-ortho-phosphate buffer (pH 4.5) and methanol as mobile phase. Column oven temperature is maintained at 25°C and observations are recorded at 220 nm. The method is simple, accurate, reproducible and short and can be used for simultaneous analysis of ambroxol, guaifenesin and salbutamol in several single dose form formulation available in the market.

Page(s): 1633-1636