Literature DB >> 20548968

Synthesis and Antimicrobial Activity of N,N'-Bis(2-hydroxylbenzyl)-1,2-ethanediamine Derivatives.

Musiliyu A Musa1, M Omar F Khan, Arden Aspedon, John S Cooperwood.   

Abstract

A series of N,N'-Bis(2-hydroxylbenzyl)-1,2-ethanediamine derivatives and its schiff bases were synthesized, characterized and screened for in vitro antimicrobial activity against Staphylococcus aureus, Pseudomonas aeruginosa and Salmonella enterica. Result indicated that the ethylenediamine derivatives, N,N'-Bis(2-hydroxy-5-bromobenzyl)-1,2-ethanediamine (21), and N,N'-Bis(2-hydroxy-5-chlorobenzyl)-1,2-ethanediamine (22) showed the most favorable antimicrobial activity exhibiting LC(50) of 11.6 and 8.79 muM against S.enterica, 86 and 138 muM against P. aeruginosa, and 140 and 287 muM against S. aureus, respectively. These compounds displayed highest level of resistance with S. aureus. Thus, the high level of activity seen with the compounds (21, 22) suggests that these compounds could serve as the leads for development of novel synthetic compounds with enhanced antimicrobial activity.

Entities:  

Year:  2010        PMID: 20548968      PMCID: PMC2884154          DOI: 10.2174/157018010790596678

Source DB:  PubMed          Journal:  Lett Drug Des Discov        ISSN: 1570-1808            Impact factor:   1.150


  28 in total

1.  Synthesis, antibacterial, antifungal and anti-HIV activities of Schiff and Mannich bases derived from isatin derivatives and N-[4-(4'-chlorophenyl)thiazol-2-yl] thiosemicarbazide.

Authors:  S N Pandeya; D Sriram; G Nath; E DeClercq
Journal:  Eur J Pharm Sci       Date:  1999-10       Impact factor: 4.384

Review 2.  Two-component signal transduction as a target for microbial anti-infective therapy.

Authors:  J F Barrett; J A Hoch
Journal:  Antimicrob Agents Chemother       Date:  1998-07       Impact factor: 5.191

3.  Combinatorial lead optimization of [1,2]-diamines based on ethambutol as potential antituberculosis preclinical candidates.

Authors:  Richard E Lee; Marina Protopopova; Emma Crooks; Richard A Slayden; Marianne Terrot; Clifton E Barry
Journal:  J Comb Chem       Date:  2003 Mar-Apr

4.  Identification of a new antitubercular drug candidate, SQ109, from a combinatorial library of 1,2-ethylenediamines.

Authors:  Marina Protopopova; Colleen Hanrahan; Boris Nikonenko; Rowena Samala; Ping Chen; Jackie Gearhart; Leo Einck; Carol A Nacy
Journal:  J Antimicrob Chemother       Date:  2005-09-19       Impact factor: 5.790

5.  Presence of new mecA and mph(C) variants conferring antibiotic resistance in Staphylococcus spp. isolated from the skin of horses before and after clinic admission.

Authors:  Christina Schnellmann; Vinzenz Gerber; Alexandra Rossano; Valentine Jaquier; Yann Panchaud; Marcus G Doherr; Andreas Thomann; Reto Straub; Vincent Perreten
Journal:  J Clin Microbiol       Date:  2006-09-27       Impact factor: 5.948

6.  Synthesis of Schiff bases of 4-(4-aminophenyl)-morpholine as potential antimicrobial agents.

Authors:  Perumal Panneerselvam; Rajasree R Nair; Gudaparthi Vijayalakshmi; Ekambaram Harihara Subramanian; Seshaiah Krishnan Sridhar
Journal:  Eur J Med Chem       Date:  2005-02       Impact factor: 6.514

7.  Biological characterization of cyclothialidine, a new DNA gyrase inhibitor.

Authors:  N Nakada; H Shimada; T Hirata; Y Aoki; T Kamiyama; J Watanabe; M Arisawa
Journal:  Antimicrob Agents Chemother       Date:  1993-12       Impact factor: 5.191

8.  Synthesis and structure-activity relationships of 5-substituted 6,8-difluoroquinolones, including sparfloxacin, a new quinolone antibacterial agent with improved potency.

Authors:  T Miyamoto; J Matsumoto; K Chiba; H Egawa; K Shibamori; A Minamida; Y Nishimura; H Okada; M Kataoka; M Fujita
Journal:  J Med Chem       Date:  1990-06       Impact factor: 7.446

9.  Synthesis and antibacterial activity of novel and potent DNA gyrase inhibitors with azole ring.

Authors:  Akihiko Tanitame; Yoshihiro Oyamada; Keiko Ofuji; Mika Fujimoto; Kenji Suzuki; Tomohiko Ueda; Hideo Terauchi; Motoji Kawasaki; Kazuo Nagai; Masaaki Wachi; Jun-ichi Yamagishi
Journal:  Bioorg Med Chem       Date:  2004-11-01       Impact factor: 3.641

10.  Synthesis and antitumor activity of amino derivatives of pyridine-2-carboxaldehyde thiosemicarbazone.

Authors:  M C Liu; T S Lin; A C Sartorelli
Journal:  J Med Chem       Date:  1992-10-02       Impact factor: 7.446

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  2 in total

1.  N-Polybenzylated alicyclic 1,2-diamines: cytotoxicity and G1 phase arrest in cancer cell line.

Authors:  Antonio Caldarelli; Valeria De Biasio; Giovanni B Giovenzana; Gianpiero Mastronardo; Roberto Negri
Journal:  Mol Divers       Date:  2014-06-28       Impact factor: 2.943

2.  Cu(II), Ni(II), and Zn(II) Complexes of Salan-Type Ligand Containing Ester Groups: Synthesis, Characterization, Electrochemical Properties, and In Vitro Biological Activities.

Authors:  P Jeslin Kanaga Inba; B Annaraj; S Thalamuthu; M A Neelakantan
Journal:  Bioinorg Chem Appl       Date:  2013-07-25       Impact factor: 7.778

  2 in total

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