TY - JOUR
T1 - Anti-microbial studies on novel 1,3-oxazolidine analogs
AU - Vachala, D.
AU - Mathew, J.E.
AU - Panneerselvam, P.
AU - Nagarethinam, Sivagurunathan
N1 - Export Date: 10 November 2017
Correspondence Address: Dinakaran, V.; Department of Pharmaceutical Chemistry, Manipal College of Pharmaceutical Sciences, Manipal 576 104 Karnataka, India; email: [email protected]
Chemicals/CAS: ciprofloxacin, 85721-33-1; ketoconazole, 65277-42-1
References: Kamlesh, S., Kishwar, S., Anwar, S., Stereo selective formation of steroidal (6R)-spiro oxazolidines (2003) Indian J Chem, 42 B, pp. 2866-2868; Adnan A.Bekhit, Hesham T.Y.Fahmy. Design and synthesis of some substituted 1H-pyrazolyl-oxazolidines or 1H-pyrazolylthiazolidines as Anti-inflammatory- Antimicrobial Agents. Archiv der Pharmazie 2003; 336:111-118; James, R.G., William, R.P., Toni-Jo, P., Richard, C.T., Stereo divergent synthesis of sulfoxide containing antibiotics (2000) Tetrahedron Lett, 41, pp. 4301-4305; Neha, G., Brijesh, K.S., Vidya, B.L., Braj, B.L., Oxazolidines-2-thiones: A molecular modelling study (2004) Tetrahedron Lett, 45, pp. 6269-6272; Heong, S.O., Hoh-Gyu, H., Seung, H.C., Deok-Chan, H., Solid phase synthesis of 1,3-oxazolidine derivatives (2000) Tetrahedron Lett, 41, pp. 5069-5072; (1989) The Merck Index: An encyclopedia of chemical drugs and biologicals, 2342, p. 3204. , Susan B, editor, 11th ed. Merck and co Inc, USA; Caroon J.M, Clark R.D, Kluge A.F, Lee H.C, Strosberg A.M. Synthesis and antihypertensive activity of a series of spiro [1,3,4,6,7b-hexahydro-2H-benzo [a] quinoline-2,5′-oxazolidin-2′-ones]. J Med Chem 1993; 26:1426-1433; Ebner, D.C., Culhane, J.C., Winkelman, T.N., Haustein, M.D., Ditty, J.L., J.Thomas Ippoloti. Synthesis of novel oxazolidinone.antimicrobail agents (2008) Bioorg.Med.Chem, 16 (5), pp. 2651-2656; Indian Pharmacopoeia, 2nd ed. II. Controller of Publication, New Delhi (1996) 100; Hawkey, P.M., Lewis, D.A., (1994) Medical Bacteriology-A Practical Approach, p. 181. , Oxford University, UK
PY - 2008
Y1 - 2008
N2 - In present study several substituted 1, 3-oxazolidines were synthesized by condensation of reduced Schiff base of phenylglycinol with different aldehydes. All the synthesized compounds showed good to moderate antimicrobial activity. The antimicrobial activites were performed by disc diffusion method and minimum inhibitory concentration determination by serial agar dilution method. Thus among the ten compounds, 3-[3-2-furyl methyl)-4-phenyl- 1,3-Oxazolidin-2-yl]-1H-indole (4a), 2-(2-furyl)-3-(2-furyl methyl)-4-phenyl-1,3-Oxazolidine (4b) and 4-[3-(2-furylmethyl)-4-phenyl-1,3- oxazolidin-2-yl]-2-methoxy phenol (4h) were found to have a moderate to significant antimicrobial activity against all the strains used. Compound 2-(4-chlorophenyl)-3-(2- furylmethyl)-4-phenyl-1, 3-oxazolidine (4j) showed very good antifungal activity than- the other compounds tested. Further more, compounds containing -Cl-, -OCH3, -OH groups as substituents were found to be potent antimicrobial agents. Moreover the heteroaromatic substitutions also showed very good antimicrobial activities.
AB - In present study several substituted 1, 3-oxazolidines were synthesized by condensation of reduced Schiff base of phenylglycinol with different aldehydes. All the synthesized compounds showed good to moderate antimicrobial activity. The antimicrobial activites were performed by disc diffusion method and minimum inhibitory concentration determination by serial agar dilution method. Thus among the ten compounds, 3-[3-2-furyl methyl)-4-phenyl- 1,3-Oxazolidin-2-yl]-1H-indole (4a), 2-(2-furyl)-3-(2-furyl methyl)-4-phenyl-1,3-Oxazolidine (4b) and 4-[3-(2-furylmethyl)-4-phenyl-1,3- oxazolidin-2-yl]-2-methoxy phenol (4h) were found to have a moderate to significant antimicrobial activity against all the strains used. Compound 2-(4-chlorophenyl)-3-(2- furylmethyl)-4-phenyl-1, 3-oxazolidine (4j) showed very good antifungal activity than- the other compounds tested. Further more, compounds containing -Cl-, -OCH3, -OH groups as substituents were found to be potent antimicrobial agents. Moreover the heteroaromatic substitutions also showed very good antimicrobial activities.
M3 - Article
SN - 1827-8620
VL - 2
SP - 192
EP - 197
JO - Pharmacologyonline
JF - Pharmacologyonline
ER -