SYNTHESIS AND IN VITRO ANTIBACTERIAL ACTIVITY OF N-[5-(5-NITROARYL)-1, 3, 4-THIADIAZOL-2-YL] PIPERAZINYL QUINOLONES

Q: How can I download an article?

To download an article from SID, first log in to the site, search for the article title, and click on the 'Download Article' option.

Q: How can I download an ISI article?

To download an ISI article on SID, enter the keyword or article title in the search bar, view the relevant results, click on the desired article, and select the 'Download Article' option.

Q: How can I access the SID database?

To access the SID database, visit SID.ir, create an account, and log in to access scientific resources.

Q: Is downloading articles from SID free?

Some articles on SID are available for free, while others require payment. Details are specified on the article's page.

MOSHEFI M.H.; SAFAVI SEYEDEH MALIHE; FOROUMARDI A.R.

مرکز اطلاعات علمی Scientific Information Database (SID) - Trusted Source for Research and Academic Resources

Journal Paper

Paper Information

Journal: JOURNAL OF RAFSANJAN UNIVERSITY OF MEDICAL SCIENCES AND HEALTH SERVICES Year:2010 | Volume:8 | Issue:4 (33) Page(s): 253-262

Download Full-Text

Persian Verion

View:

1,018

Download:

Cites:

Information Journal Paper

Title

SYNTHESIS AND IN VITRO ANTIBACTERIAL ACTIVITY OF N-[5-(5-NITROARYL)-1, 3, 4-THIADIAZOL-2-YL] PIPERAZINYL QUINOLONES

Author(s)

MOSHEFI M.H. | SAFAVI SEYEDEH MALIHE | FOROUMARDI A.R. | Issue Writer Certificate

Keywords

QUINOLONESQ2

NITROAROMATIC COMPOUNDSQ3

1Q1

3Q1

4-THIADIAZOLEQ3

ANTIBACTERIAL ACTIVITYQ3

Abstract

Background and Objectives: Because resistance to antimicrobial drugs is widespread, recognition of new antimicrobial and understanding of their mechanisms are vital. The QUINOLONES have a broad antibacterial spectrum of activity against Gram-positive, Gram-negative and mycobacterial pathogens such as anaerobes. In the present study, the synthesis and ANTIBACTERIAL ACTIVITY of a new series of N-piperazinyl QUINOLONES containing 5-(nitroaryl)-1, 3, 4-THIADIAZOLE-2-yl moiety have been studied. Materials and Methods: In this laboratory study, the reaction of 1-cyclopropyl-6 fluoro-8 methoxy-4-oxo-7- (piperazin-1-yl)-1, 4- dihydroquinoline-3- carboxylic acid (compound 3), with 2-chloro-5-(nitroaryl)-1,3,4-thiadiazol (compounds 9a-f), in DMF in the presence of NaHCO3 at 85-90oC, gave final compounds 1- cyclopropyl- 6fluoro-7-[4-[5-(nitroaryl)-1,3, 4-thiadiazol-2yl], piperazin-1-yl] -8- methoxy-4-oxo-quinoline-3- carboxylic acid (8a-f). compounds 8a-f, were tested in vitro by the conventional agar dilution method against a panel of microorganisms including stophylococcus aureus, Escherichia coli, salmonella typhi, shigella flexneri, klebsiella pneumonia, serratia marcescens and pseudomonas aeruginosa. Results: Among synthesized compound, nitrofuran analog 8b exhibited more potent inhibitory activity against Gram-positive bacteria including B. subtilis, S. epidermidis, E. feacalis, M. luteus, in respect to other synthesized compounds and reference drug gatifloxacin. Conclusion: Introduction of the bulky group of [5-(5-nitroaryl)-1, 3, 4-thiadiazol-2-yl] could dramatically impact the ANTIBACTERIAL ACTIVITY of the parent quinolone, and among the nitroaryl groups, 5-nitrofuryl analogue showed the most potent ANTIBACTERIAL ACTIVITY against the tested microorganisms .

Cites

No record.

References

No record.

Cite

APA: Copy

MOSHEFI, M.H., SAFAVI, SEYEDEH MALIHE, & FOROUMARDI, A.R.. (2010). SYNTHESIS AND IN VITRO ANTIBACTERIAL ACTIVITY OF N-[5-(5-NITROARYL)-1, 3, 4-THIADIAZOL-2-YL] PIPERAZINYL QUINOLONES. JOURNAL OF RAFSANJAN UNIVERSITY OF MEDICAL SCIENCES AND HEALTH SERVICES, 8(4 (33)), 253-262. SID. https://sid.ir/paper/71077/en

Vancouver: Copy

MOSHEFI M.H., SAFAVI SEYEDEH MALIHE, FOROUMARDI A.R.. SYNTHESIS AND IN VITRO ANTIBACTERIAL ACTIVITY OF N-[5-(5-NITROARYL)-1, 3, 4-THIADIAZOL-2-YL] PIPERAZINYL QUINOLONES. JOURNAL OF RAFSANJAN UNIVERSITY OF MEDICAL SCIENCES AND HEALTH SERVICES[Internet]. 2010;8(4 (33)):253-262. Available from: https://sid.ir/paper/71077/en

IEEE: Copy

M.H. MOSHEFI, SEYEDEH MALIHE SAFAVI, and A.R. FOROUMARDI, “SYNTHESIS AND IN VITRO ANTIBACTERIAL ACTIVITY OF N-[5-(5-NITROARYL)-1, 3, 4-THIADIAZOL-2-YL] PIPERAZINYL QUINOLONES,” JOURNAL OF RAFSANJAN UNIVERSITY OF MEDICAL SCIENCES AND HEALTH SERVICES, vol. 8, no. 4 (33), pp. 253–262, 2010, [Online]. Available: https://sid.ir/paper/71077/en

Related Journal Papers