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Selvam: Synthesis, Anti-mycobacterial and Cytotoxicity Studies of Novel …
International Journal of Drug Design and Discovery
Volume 3 Issue 3 July – September 2012. 837-839
Synthesis, Anti-mycobacterial and Cytotoxicity Studies of Novel
[(Sulphamoylphenyl)amino]methylpiperazinyl fluroquinolones

P. Selvam
Devaki Amma Memorial College of Pharmacy, Chelembra, Malapuram- 673634, Kerala. ABSTRACT: A series of novel [(Sulphamoylphenyl)amino]methyl piperazinyl fluroquinolones were synthesized through
modifying the N4-hydrogen of piperazine in fluoroquinolones with formaldehyde and sulphanomides by mannich reactions.
Synthesized compounds were screened for anti-mycobacterial activity against TB H37Rv strain. Cytotoxicity of the
synthesized compounds was also tested in mock-infected Vero cells. All the compounds exhibited significant anti-tubercular
activity. Among the synthesized compounds, compounds GF-SA, GF-SD and CF-SD were found to exhibit the most potent
in vitro anti-mycobacterial activity with a EC90 value of less than 0.195 µg/ml, and a selectivity index of more than 153 while
not being cytotoxic to the Vero cell line up to 30 µg/ml.
KEYWORDS: Fluoroquinolone; Mannich reaction; Mycobacterium tuberculosis; Vero cells.
Quinolone is a versatile lead molecule for designing from DMF with ethanol. The IR spectra of all the potential bioactive agents and its derivatives are reported to compounds showed intense peak at 1707-1773 cm-1 for possess a broad spectrum of antimicrobial activity. aromatic carbonyl (C=O), 1618-1628 (C=N), 1440 (SO2), Recently, newer synthesized aryl piperazinyl fluoro- 3347-3527 (NH), 2359-2723 (C-Alkyl), 659-673 cm-1 for quinolones were studied for anti-tubercular activity, some fluorine (C-F). The formation of the product is indicated by of their derivatives were found to possess significant anti- the disappearance of peaks due to C-NH2 of the starting mycobacterium activity1-11. But anti-TB activity of material at 3425 cm-1. 1H-NMR spectra of all the [(Sulphamoylphenyl)amino]methyl piperazinyl fluroquinolones compounds showed signals at 7.1-7.3 δ ppm (m, Ar-H) and is relatively less explored. In view of this, we have 8.7-9.1 δ ppm (s, 1H, COOH). All these compounds did synthesized novel N-Sulphonamidomethyl piperzinyl not contain that the primary amine of sulphonamide reacted fluoroquinolones by Mannich reactions (Scheme 1) and with fluoroquinolones. All these compounds do not contain tested for anti-mycobacterial activity. Cytotoxicity of the broad singlet at 6.1 ppm indicate that the primary amino of test compounds was tested in mock-infected Vero cells. sulphonamide react with fluoroquinolones. Melting points were determined in open capillary tubes The synthesized compounds were evaluated for their on a Thomas-Hoover melting point apparatus and are inhibitory effect on the Mycobacterium tuberculosis H37Rv uncorrected. IR spectra were recorded for KBr pellets on a ATCC 2729413 and their EC90 (effective concentration of Jasco-410 infrared spectrophotometer, 1H-NMR spectra compound achieving 90% protection against M. were determined BRUKER AMX 400 MHZ with tuberculosis H37Rv) and CC50 (cytotoxic concentration of tetramethylsilane as an internal standard. The sample was compound required to reduce the viability of mock infected dissolved in DMSO-d6 and the value was measured in δ Vero cells), are reported in Table 1. The results revealed that all the compounds exhibited excellent anti-TB activity. Compound GF-SA, GF-SD and CF-SD inhibited the Synthesis of N-sulphonamidomethyl fluoroquinolones Mycobacterium tuberculosis. Their inhibitory derivatives12 was achieved by stirring on equimolar (0.01 mole) mixture of sulphonamides (sulphonamide, sulphadiazine and sulphadimidine), formaldehyde (37% v/v, 30 µg/ml. The compound NF-SA, NF-SD and NF-SDM ml) and fluoroquinolone (norfloxacin NF, ciprofloxacin CF inhibited the Mycobacterium tuberculosis with the EC and gatifloxacin GF) with ethanol using a magnetic stirrer for 3 hours. The mixture allowed to cool over night in a These compounds also inhibited significant activity against refrigerator. The solid thus obtained was recrystallized Mycobacterium tuberculosis with the SI values of more than 153 and 18. All the compounds exhibited cytotoxic concentration of more than 30 µg/ml in uninfected Vero 838 International Journal of Drug Design and Discovery Volume 3 Issue 3 July – September 2012
Compound Code
Scheme 1 Synthesis of N-sulphonamidomethyl fluoroquinolones.
Selvam: Synthesis, Anti-mycobacterial and Cytotoxicity Studies of Novel …
Table 1 Cytotoxicity and Anti-TB Activity of Fluoroquinone Derivatives.
Compound
Selectivity indexc
50 (µg/ml)
(µg/ml)
EC90/CC50
a90% Effective concentration of compound, achieving 90% protection against the MTB. b50% Cytotoxic concentration of compound, required to reduce the viability of mock-infected Vero cells by 50%. ND-not determined References
[7] Sriram D, Bal TR, Yogeeswari P, Nagaraja V. Evaluation of antimycobacterial and DNA gyrase inhibition of [1] Sriram, D, Bal TR, Yogeeswari P. Microwave-assisted fluoroquinolone derivatives. J Gen App Microbiol 2006; synthesis, and anti-YFV activity of 2, 3-diaryl-1, 3- 52:195-200,
thiazolidin-4-ones. J Pharm Pharm Sci 2005; 8: 429-66.
[8] Sriram D, Aubry A, Yogeeswari P. Gatifloxacin [2] Sriram D, Bal TR, Yogeeswari P. Design, synthesis and derivatives: Synthesis, antimycobacterial activities, and biological evaluation of novel non-nucleoside HIV-1 inhibition of Mycobacterium tuberculosis DNA gyrase. reverse transcriptase inhibitors with broad-spectrum Bioorg Med Chem. Lett 2006; 16: 2982-85.
chemotherapeutic properties. Bioorg Med Chem 2004; 12:
[9] Sriram D, Yogeeswari P, Basha JS, Nagaraja V. Synthesis and Antimycobacterial evaluation of various 7- [3] Sriram D, Bal TR, Yogeeswari P. Newer Substituted Ciprofloxacin Derivatives. Bioorg Med Chem aminopyrimidinimino isatin analogues as non-nucleoside 2005; 13: 5774-78.
HIV-1 reverse transcriptase inhibitors for HIV and other [10] Pandeya SN, Sriram D, Yogeeswari P, Ananthan S. opportunistic infections of AIDS: Synthesis and biological Antituberculous activity of Norfloxacin Mannich bases evaluation. Farmaco 2005; 60: 377-84.
with Isatin derivatives. Chemotherapy, 2001;47: 266-69.
[4] Murugesan D, Palaniappan S, Perumal Y, Valakunja N, [11] Pandeya SN, Sriram D, Nath G, De Clercq E. Synthesis, Sriram D. Antimycobacterial and phototoxic evaluation of antibacterial, antifungal and anti-HIV activities of 6-fluoro/nitro-4-oxo-7-(sub)-4H- [1,3] thiazeto[3,2-a] norfloxacin Mannich bases. J Med Chem 2000; 35: 249-
quinoline-3-carboxylic acid. Int J Antimicrob Agents 2008; 31; 337-44,.
[12] Selvam P, Rathore P, Karthikumar S, Velkumar K, [5] Dinakaran M, Senthilkumar P, Yogeeswari P, China A, Palanisamy P, Vijayalakhsmi S, Witvrouw M. Synthesis Sriram D. Antimycobacterial activities of novel 2-(sub)- and Antiviral Studies of Novel N-Sulphonamidomethyl 3-fluoro/nitro-5,12-dihydro-5-oxo benzo- thiazolo[3,2- piperazinyl Fluoroquinolones. Indian J Pharm Sci 2009; a] quinoline-6-carboxylic acid. Bioorg Med Chem 2008; 71: 432-6.
16: 3408-18,.
[13] Collins L, Franzblau SG. Microplate alamar blue assay [6] Senthilkumar P, Dinakaran M, Yogeeswari P. Sriram D. versus BACTEC 460 system for high- throughput Synthesis and antitubercular activities of 1-(cyclopropyl/t- screening of compounds against Mycobacterium butyl/4-fluorophenyl)-1,4-dihydro-6-nitro-4-oxo-7- tuberculosis and Mycobacterium avium. Antimicrob (substituted secondary amines)-1,8-naphthyridine-3- Agents Chemother 1997; 41: 1004-9.
carboxylic acid. Med Chem Res 2007; 15:281-82,

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