Document Type : Research Paper

Authors

1 College of Science, University of Anbar

2 University of Anbar - College of Pharmacy

3 College of Science, University of Anbar-Ramadi

Abstract

Synthesis and characterization mono imides derivatives for trimethoprim, through reaction of the later with one mole of maleic and phthalic anhydrides, using the classical reflux methods in addition to the microwave technique in the presence of glacial acetic acid. Conversion of mono imides derivatives prepared in (1) above to the Schiff`s bases by the condensation with substituted aromatic aldehydes or ketones, using conventional method and microwave technique. So that imides-imines derivatives have been prepared. All the compounds prepared above have been characterized by using the physical constant by recording the malting points and using the spectroscopic methods such as UV-Visible, FT-IR and H1NMR spectroscopy. Study the biological activity of some selected new compounds as anti-bacterial against four types of bacteria (Pseudomona aruginons , Escherichia coli , Staphylococcus aureus and Enterococcus faecalis) isolates by Biomerixe co. using the disk diffusion method. This study showed high biological activity of most prepared compound against the studying bacteria.

Main Subjects

1-    P. Bruice "Organic Chemistry",4nd (2010) 708.
2-    M. Salvati, A. Balog, W. Shan, D.D. Wei, D. Pickering, R. Attar, J. Geng, C. Rizzo,M. Gottardis, R. Weinmann, S. Krystek, J. Sack, Y. An, K. Kish, Bioorg. Med. Chem. Lett. 15(2005)271. (b) J. Kossakowski, M. Jarocka, Il Farmaco 56 (2001) 785.
3-    K. Ishizumi, A. Kojma, F. Antoku, Chem. Pharm. Bull. 39 (1991) 2288.  (d) Y. Sabata, M. Shichita, K. Sasaki, Y. Hashimoto, S. Iwasaki, Chem. Pharm. Bull. 43 (1995)177.    (e) D. Jindal, V. Bedi, B. Jit, N. Karkra, S. Guleria, R. Bansal, A. Palusczak, R. Hartmann, IlFarmaco60(2005)283.   (f) J. Wang, S. Wang, C. Lee, M. Chung,Y. Chern, Chemotherapy43 (1997) 182.
4-    A. Machado, L. Lima, J. Arau, C. Fraga,V. G.Koatz, E. Barreiro, Bioorg. Med. Chem. Lett. 15(2005)1169.                                                                                                     (h) S. Kenji, N. Hideko, U. Yoshihiro, S. Yoshikazu, N. Kazuharu, W. Motoji, W. Konstanty, T. Tadafumi, A. Tetsuji, Y. Yuji, K.  Kenji, H. Hitoshi, Bioorg. Med. Chem.,13 (2005) 4014.                              
5-     A. Mayer, S. Neuenhofer, Angew. Chem. Int. Ed.Engl.,33(1994)1044. (j) F. Miguel, D. Gema, S. Beatriz, R. Cynthia, R. Simmon, B. Teresa, Eur. J. Med. Chem., 37(2002)541.  (k) H. Miyachi, A. Azuma, A. Ogasawara, E. Uchimura, N. Watanabe, Y. Kobayashi, F. Kato, M. Kato, H. Hashimoto, J. Med. Chem., 40 (1997) 2858.
6-    D. G. Nagle, V. J. Paul, M. A. Roberts, Tetrahedron Lett,. 7 (1996) 6263.
7-    T. Iijima, Suzuki, N. Fukuda, W. Tomoi, M. Eur. J. Polym., (1995), 31  775-783.                                                                                                               
8-    S. Kohmoto, H. Masu, C. Tatsuno, K. Kishikawa, M. Yamamoto, K. Yamaguchi, J. Chem. Soc., Perkin Trans. 1 (2000) 4464.                    
9-    U. patent PCT/US97/13195, WO 98/04664, 5 February (1998).           
10- M. Sakamoto, M. Takahashi, T. Fujita, S. Watanabe, I. Iida, T. Nishio and H. Aoyama, J Org. Chem. 58 (1993) 3476.
11- G. Pettit, Y. Kamano, C. Dufresne, R. L. Cerny, C. Herald, and J. Schmidt, J. Org Chem. 54 (1989) 6005.                     
12- H. Nakamura, Y. Iitaka, H. Sakakibara, H. Umezawa and J. Antibiot. 27 (1974) 894.
13- Anshul Chawla, Ramandeep Kaur and Anju Goyal, J. Chem. Pharm. Res., (2011), 3(6):925-944.                                                                                
14- S. Shinde et al / Int. J. Ind. Chem., Vol. 2, No. 2, (2011), 112-116.
15- E. Benjamin and Y. Hijji, Molecules, (2008), 13, 157-169. 
16- D. Habibi and O. Marvi , j. ARKIVOC (2006) (xiii) 8-15.
17- M. poor-Baltork et al. J. Iran. Chem. Soc., Vol. 8, No. 2, June (2011), pp. 401-410.
18- J. March, " Advanced Organic Chemistry: Reactions, Mechanisms. And structure "(6th ed.), New York: wiely, (2007).
19- M. Kidwai, S. Saxena, S. Rastogi, and R. Venkataramanan, Current Med.Chem. Anti-infective agents, 2, 269 (2003).
20- V. Patel, and J. Patel, Ultra Scientist of Physical Sci., 16, 111 (2004).
21- W., Bauer, M. Kirby, S. Shrris and M. Turk. “Antibiotic susceptibility Testing by a Standrized Single disk Method” Am. Journal Clin. Pathol., 45, 493,(1966).
22- J. Bellamy, “The infar-reda Spectra of Complex Molecules” 2ed Richard Clay and Co. Ltd., Bungay, Suffolk., 132 (1964).
23- H.W. Seely, Jr.,P.J. Vandamark, MICROBES IN ACTION,3rd ed. 178,W.H. Freedman & Comp.1981.
24- لجنة من تدریسی قسم علوم الحیاة, علم الاحیاء المجهریة, 305317,59, جامعة بغداد 1991.
25- زلزلة, قاسم علی "موجز فی علم الاحیاء الدقیقة" بغداد 1982.