Asian Journal of Research in Chemistry

M. C. Kalekar ¹, A. R. Bhat ¹, V. R. Koli ¹

Affiliations
1 Department of Pharmaceutical Chemistry, K. L.E.U’s College of Pharmacy, Belgaum, IN

Abstract

Compound (3-oxo-3, 4-dihydro-2H-1, 4-benzothiazin-2-yl) acetic acid was synthesized by reacting o-Amino thiophenol and maleic anhydride. (3-oxo-3, 4-dihydro-2H-1, 4-benzothiazin-2-yl) acetate was prepared by Esterification of (3-oxo-3, 4-dihydro-2H-1, 4-benzothiazin-2-yl) acetic acid. Further eight Mannich bases were synthesized by using substituted Aromatic amines. The structures of synthesized compounds were confirmed on basis of IR, NMR and Mass Spectra. All synthesized compounds were screened for their antibacterial activity against strains viz. E. coli, E.fecalis, Klebshilla and S. aureus and antifungal activity against strains viz. C. albican and Aspergillus Niger. [4-({[4-( N-(5-methyl-4,5-dihydroisoxazol-3-yl)-aminosulfonyl) phenyl] amino} methyl)-3-oxo-3,4-dihydro- 2H-1,4-benzothiazin-2-yl]acetic acid, Ethyl[4-({[4-(N-(5-methyl-4,5-dihydro isoxazol-3-yl)-aminosulfonyl)phenyl] amino} methyl)-3-oxo-3,4-dihydro-2H-1,4-benzo thiazin-2-yl]acetate, [4-({[4-(N-pyridin-aminosulfonyl) phenyl] amino} methyl)-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl]acetic acid and Ethyl [4-({[4-(N-pyridin-aminosulfonyl) phenyl]amino}methyl)-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl]acetate have shown significant antibacterial and antifungal activity, while other derivatives shown moderate antibacterial and antifungal activity.

Keywords

1, 4 Benzothiazine, 1, 4 Benzothiazine Ester, Antibacterial, Antifungal.

Full Text

     

M. M. Maste ¹, M. C. Kalekar ¹, N. Kadian ¹, A. R. Bhat ¹

Affiliations
1 Department of Pharmaceutical Chemistry, KLEU’s College of Pharmacy, Belgaum, IN

Abstract

Present work describes a precise, accurate and reproducible Reverse phase High Performance Liquid Chromatographic (RP-HPLC) method for simultaneous estimation of Ramipril and Amlodipine in tablet dosage form on Phenomenex C₁₈ column (245 mm × 4.5 mm, 5 μm, particle size) using acetonitrile: phosphate buffer, (60:40 v/v) as mobile phase at flow rate of 1.0 ml/min and the detection wavelength was 222 nm. The retention time for Ramipril and Amlodipine was found to be 3.41 and 6.10 min respectively. Proposed method was validated for precision, accuracy, linearity range, robustness and ruggedness.

Keywords

Amlodipine, Ramipril, RP-HPLC.

Full Text

     

M. M. Maste ¹, P. Jeyarani ¹, M. C. Kalekar ¹, A. R. Bhat ¹

Affiliations
1 Department of Pharmaceutical Chemistry, K. L.E.U’s College of Pharmacy, Belgaum, IN

Abstract

The present research work was aimed to synthesize some benzimidazole acetic acid derivatives and also the derivatives associated with 1,2,4 triazolone and was investigated for their biological activities. A two different series of compounds were synthesized, 4-[(2-aryl methyl- 1H-benzimidazol-1-yl) acetyl] 5 nitro-2,4 -dihydro-3H-1,2,4 triazol- 3-one and 4-[(2-aryl methyl-1H-benzimidazol-1-yl)methyl] 5 nitro-2,4- dihydro-3H-1,2,4 triazol-3-one. The newly synthesized compounds have been characterized by their analytical and spectral (IR and ¹H NMR, C¹³ NMR, mass spectra) properties. All the compounds have been screened for their anti tubercular and antimicrobial activities by standard methods. Results of activities reveal that compound shown promising anti tubercular activity at both the concentration compared to standard drug streptomycin, and shown good antimicrobial activities.

Keywords

1,2,4 Triazolone, Benzimidazole, Anti Tubercular, Anti Bacterial , Antifungal Activity.

Full Text