Browse > Article

Synthesis and Antitubercular Activity of 6-Chloro (Unsubstituted)- 2-Methoxy-9-Substituted Acridine Derivatives  

Aly, Enayat I. (Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University)
Abadi, Ashraf H. (Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University)
Publication Information
Archives of Pharmacal Research / v.27, no.7, 2004 , pp. 713-719 More about this Journal
Abstract
Several analogues of the general formulae 2-methoxy-9-substituted acridine and 6-chloro-2-methoxy-9-substituted acridine were synthesized and evaluated in vitro at 6.25 $\mu\textrm{g}$/mL against M. tuberculosis $H_{37}Rv$. Compounds 15 and 17 showed potential antitubercular activity with 100% inhibition to the virulent mycobacterium.
Keywords
Acridine; Tuberculosis;
Citations & Related Records

Times Cited By Web Of Science : 1  (Related Records In Web of Science)
Times Cited By SCOPUS : 2
연도 인용수 순위
1 Alberghina, M. and Palermo, F., Mutational studies of the drugr-resistance of M. tuberculosis with special reference to ${\rho}$-aminosalicylic acid, ethambutol, isoniazid and rifampicin. Boll. 1st. Sieroter. Milan, 54, 437-444 (1975)   PUBMED
2 ChemSketch 5.0 freeware, Advanced Chemistry Development Inc. 90 Adelaide Street West, Suite 600 Toronto, Ontario M5H 3V9, Canada.
3 HyperChem 6.0, Hypercube Inc., 1115 N. W. 4th street, Gainesville, FI 32601, USA.
4 Zachariah, R., Spielmann, M. P, Harries, A. D., and Salaniponi, F. L., Voluntary counselling, HIV testing and sexual behaviour among patients with tuberculosis in a rural district of Malawi. Int. J. Tuberc. Lung Dis., 7, 65-71 (2003)
5 Yamada, H., Nakahara, Y., Aoki, Y., Katoh, O., Hiura, K., Kuori, S., and Yamaguchi, M., Hospital-onset tuberculosis in compromised host. Intern. Med., 31, 740-745 (1992)   DOI   ScienceOn
6 Mir, I., Siddiqui, M. T., and Cormie, A. M., Antituberculosis agents. V: Alpha-[5-(5-nitro-2-furyl)-1,3,4-oxadiazol-2-ylthio] acethydrazide and related compounds. J. Pharm. Sci., 80, 548-550 (1991)   DOI   PUBMED
7 Ellner, J. J., Goldberger, M. J., and Parenti, D. M., Myco-bacterium avium infection and AIDS: a therapeutic dilemma in rapid evolution. J. Infect. Dis.,163, 1326-1335 (1991)   DOI   PUBMED   ScienceOn
8 EPI Suite v. 3.11, freeware developed by the Environmental Protection Agency EPA and Syracuse Research corporation.
9 O'Brien, R. J. and Nunn, P. P., The need for new drugs against tuberculosis. Obstacles, opportunities and next steps. Am. J. Respir. Crit. Care Med., 163, 1055-1058 (2001)   DOI   PUBMED
10 lIseman, M. D., Treatment of multidrug-resistant tuberculosis. N. Engl. J. Med., 329, 784-791 (1993)   DOI   PUBMED   ScienceOn
11 Farmer, P. and kim, J. Y, Community based approaches to the control of multidrug-resistant tuberculosis 'DOTS-plus', BMJ, 317, 671-674 (1998)   DOI   ScienceOn
12 Evans, K. D., Nakasone, A. S., Sutherland, P.A, de la Maza, L. M., and Peterson, E. M., Identification of Mycobacterium tuberculosis and Mycobacterium avium- M. intracellulare directly from primary BACTEC cultures by using acridiniumester- labeled DNA probes. J. Clin. Microbiol., 30, 2427-2431 (1992)   PUBMED
13 Dye, C., Scheele, S., Dolin, P., Pathania, V., and Raviglione, M. C., Consensus statement. Global burden of tuberculosis: estimated incidence, prevalence and mortality by country. WHO global surveillance and monitoring project. JAMA, 282, 677-686 (1999)   DOI   ScienceOn
14 Suling, W. J., Seitz, L. E., Pathak, V., Westbrook, L., Barrow, E. W., Zywno-Van-Ginkel, S., Reynolds, R. C., piper, J. R., and Barrow, W. W., Antimycobacterial activities of 2,4-diamino-5-deazapteridine derivatives and effects on mycobacterial dihydrofolate reductase. Antirnicrob. Ag. Chemother., 44, 2784-2793 (2000)   DOI   ScienceOn
15 Ismail, K. A. and Koreish, E. A., Synthesis of 9-{4-[2-(substituted amino)ethoxy]phenoxy}2-methoxyacridines as potential antimicrobial and antitumor agents. Alex. J. Pharm. Sci., 14, 161-166 (2000)
16 Thiim, M. and Friedman, L. S., Hepatotoxicity of antibiotics and antifungals. Clin. Liver Dis., 7, 381-399 (2003)   DOI   ScienceOn
17 Kimura, M., Okabayashi, I., and Kato, A., Acridine derivatives. III. Preparation and antitumor activity of the novel acridinyl-substituted uracils. Chem. Pharm. Bull.,37, 697-701 (1989)   DOI   PUBMED   ScienceOn
18 Omar, M. T. and Hamouly, W. S., Synthesis and antimicrobial evaluation of some new acridine derivatives. Al-Azhar Bull. Sci., 7, 153-159 (1996)
19 Collins, L. A. and Franzblau, S. G., Microplate alamar blue assay versus BACTEC 460 system for high-throughput screening of compounds against Mycobacterium tuberculosis and Mycobacterium avium. Antimicrob. Agents Chemother., 41, 1004-1009 (1997)   PUBMED
20 Baca, A. M., Sirawarapom, R., Turley, S., Sirawarapom, W., and Hoi, W. G., Crystal structure of Mycobacterium tuberculosis 7,8-dihydropteroate synthase in complex with pterin monophosphate: new insight into the enzymatic mechanism and sulfa-drug action. J. Mol. Biol., 302, 1193-1212 (2000)   DOI   ScienceOn