Abstract
A series of novel substituted 2-[4-(2,4-dimethoxy-benzoyl)-phenoxy]-1-[4-(3-piperidin-4-yl-propyl)-piperidin- 1-yl]-ethanone sulfonamide (9a-h) benzamides (10a-h) were synthesized in order to determine their antibacterial activities and possible structure- activity relationships to improve therapeutic efficacy. The synthesized compounds were characterized by 1H-NMR, FTIR and elemental analysis. All the synthesized compounds were evaluated in vitro for their efficacy as antibacterial agents by agar well diffusion and micro dilution method against standard strains of Gram-positive (staphylococcus aureus ATCC 29737, Bacillus substilis NCIM 2010, Streptococcus pyognes NCIM 2608) and Gram-negative (Pseudomonas aeruginosa ATCC 20852, Klebsiella pneumoniae MTCC 618, Escherichia coli ATCC 25922) bacteria. Among the synthesized new compounds (9c), (9d), (9e), (9f), (10a), (10c), (10d), (10e) and (10g) showed potent antibacterial activities compared to the standard drug. In particular, all the tested compounds had potent inhibitory activity against B. subtilis and E. coli.
Keywords: (4-hydroxyphenyl)(2,4-dimethoxyphenyl)methanone, 1,3-Dimethoxy benzene, N-Methyl morpholine, Sulfonyl chlorides, Acid chlorides, Antibacterial activity
Letters in Drug Design & Discovery
Title: Synthesis of Medicinally Important N-Trimethylene Dipiperidine Sulfonamides and Carboxamides Containing a Substituted Benzophenone Moiety - An Antibacterial Agents
Volume: 5 Issue: 4
Author(s): Mallappanahally Kambappa Vinaya, Hanuma Naika Raja Naika, Channapille Koppal Siddegowda Ananda Kumar, Salekoppal Boregowda Benaka Prasad, Siddappa Chandrappa, Somasagara Ramanna Ranganatha, Venkatarangaiah Krishna and Kanchugarakoppal Subbegowda Rangappa
Affiliation:
Keywords: (4-hydroxyphenyl)(2,4-dimethoxyphenyl)methanone, 1,3-Dimethoxy benzene, N-Methyl morpholine, Sulfonyl chlorides, Acid chlorides, Antibacterial activity
Abstract: A series of novel substituted 2-[4-(2,4-dimethoxy-benzoyl)-phenoxy]-1-[4-(3-piperidin-4-yl-propyl)-piperidin- 1-yl]-ethanone sulfonamide (9a-h) benzamides (10a-h) were synthesized in order to determine their antibacterial activities and possible structure- activity relationships to improve therapeutic efficacy. The synthesized compounds were characterized by 1H-NMR, FTIR and elemental analysis. All the synthesized compounds were evaluated in vitro for their efficacy as antibacterial agents by agar well diffusion and micro dilution method against standard strains of Gram-positive (staphylococcus aureus ATCC 29737, Bacillus substilis NCIM 2010, Streptococcus pyognes NCIM 2608) and Gram-negative (Pseudomonas aeruginosa ATCC 20852, Klebsiella pneumoniae MTCC 618, Escherichia coli ATCC 25922) bacteria. Among the synthesized new compounds (9c), (9d), (9e), (9f), (10a), (10c), (10d), (10e) and (10g) showed potent antibacterial activities compared to the standard drug. In particular, all the tested compounds had potent inhibitory activity against B. subtilis and E. coli.
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Vinaya Kambappa Mallappanahally, Raja Naika Naika Hanuma, Ananda Kumar Koppal Siddegowda Channapille, Benaka Prasad Boregowda Salekoppal, Chandrappa Siddappa, Ranganatha Ramanna Somasagara, Krishna Venkatarangaiah and Rangappa Subbegowda Kanchugarakoppal, Synthesis of Medicinally Important N-Trimethylene Dipiperidine Sulfonamides and Carboxamides Containing a Substituted Benzophenone Moiety - An Antibacterial Agents, Letters in Drug Design & Discovery 2008; 5 (4) . https://dx.doi.org/10.2174/157018008784619951
DOI https://dx.doi.org/10.2174/157018008784619951 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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