International E-publication: Publish Projects, Dissertation, Theses, Books, Souvenir, Conference Proceeding with ISBN.  International E-Bulletin: Information/News regarding: Academics and Research

Antimicrobial evaluations of propionic acid of quinazolines derivatives

    ,

Author Affiliations

  • 1Synthesis Organic and Medicinal Chemistry lab, Department of Chemistry, Mewar University, Gangrar, Rajasthan-312901, India
  • 2Synthesis Organic and Medicinal Chemistry lab, Department of Chemistry, Mewar University, Gangrar, Rajasthan-312901, India

Res.J.chem.sci., Volume 8, Issue (12), Pages 24-28, December,18 (2018)

Abstract

The derivatives of Propionic Acid of Quinazoline were synthesized. It was prepped by reaction of distinct amino acids with 7-nitro-2-phenyl-4H-benzo [1,3]oxazin-4-one. Configurations of same compounds have been appraised by NMR, MASS and IR spectral analysis. Synthesized compounds were screened with against following pathogenic bacteria Staphylococcus aureus, Staphylococcus pneumoniae, Pseudomonas aeruginosa, Escherichia coli and Klebsiella pneumonia. We used 500ppm concentration in DMSO for their antibacterial activity by Kirby-Baur disk diffusion method.

References

  1. Katritzky A.R. and Pozharskii A.F. (2003)., Handbook of Heterocyclic Chemistry., Pergamon Press, Oxford.
  2. Vijaynathappa J. and Bhojraj S. (2008)., Efficient synthesis of 2-(2-hydroxyphenyl) quinazolin-4(3H)-one derivatives., Journal of Health Sciences, 54, 524-528.
  3. Alagarsamy V., Solomon V.R. and Dhanabal K. (2007)., Synthesis and pharmacological evaluation of some 3-phenyl-2-substituted-3H-quinazolin-4-one as analgesic, anti-inflammatory agents., Bioorganic and medicinal chemistry, 15(1), 235-241.
  4. Giri R.S., Thaker H.M., Giordano T., Williams J., Rogers D., Sudersanam V. and Vasu K. K. (2009)., Design, synthesis and characterization of novel 2-(2, 4-disubstituted-thiazole-5-yl)-3-aryl-3H-quinazoline-4-one derivatives as inhibitors of NF-κB and AP-1 mediated transcription activation and as potential anti-inflammatory agents., European journal of medicinal chemistry, 44(5), 2184-2189.
  5. Al-Obaid A.M., Abdel-Hamide S.G., El-Kashef H.A., Alaa A.M., El-Azab A.S., Al-Khamees H.A. and El-Subbagh H.I. (2009)., Synthesis, in vitro antitumor activity and molecular modeling study of certain 2-thieno-4(3H)-quinazolinone analogs., Eur. J. Med. Chem., 44(6), 2379-2391.
  6. Chandregowda V., Kush A.K. and Reddy G.C. (2009)., Synthesis and in vitro antitumor activities of novel 4-anilinoquinazoline derivatives., Eur. J. Med. Chem., 44(7), 3046-3055.
  7. Giri R.S., Thaker H.M. and Giordano T. (2010)., Design, synthesis and evaluation of novel 2-thiophen-5-yl-3H-quinazolin-4-one analogues as inhibitors of transcription factors NF-kappaB and AP-1 mediated transcriptional activation: Their possible utilization as anti-inflammatory and anti-cancer agents., Bioorg. Med. Chem., 18(7), 2796-2808.
  8. Vachala D. and Unnissa H. (2008)., Synthesis, Characterization and Biological Screening of Tetrahydro-Quinazoline Analogues., Indian J. Heterocycl. Chem., 17, 347-350.
  9. Jatav V., Mishra P., Kashaw S. and Stables J.P. (2008)., CNS depressant and anticonvulsant activities of some novel 3-[5-substituted 1,3,4-thiadiazole-2-yl]-2-styryl quinazoline-4(3H)-ones., Eur. J. Med. Chem., 43(9), 1945-1954. DOI: 10.1016/j.ejmech.2007.12.003, PMID: 18222569.
  10. Maddry J.A., Ananthan S., Goldman R.C., Hobrath J.V., Kwong C.D., Maddox C. and White E.L. (2009)., Antituberculosis Activity of the Molecular Libraries Screening Center Network Library., Tuberculosis, 89(5), 354-363. DOI: 10.1016/j.tube.2009.07.006, PMID: 19783214.
  11. Kabri Y., Azas N., Dumètre A., Hutter S., Laget M., Verhaeghe P. and Vanelle P. (2010)., Original quinazoline derivatives displaying antiplasmodial properties., Eur. J. Med. Chem., 45(2), 616-622.
  12. Xu G.F., Song B.A., Bhadury P.S., Yang S., Zhang P.Q., Jin L.H. and Lu P. (2007)., Synthesis and antifungal activity of novel s-substituted 6-fluoro-4-alkyl(aryl) thioquinazoline derivatives., Bioorgan. Med. Chem., 15(11), 3768-3774. DOI: 10.1016/j.bmc.2007.03.037. PMID: 17412601.
  13. Guan J., Zhang Q., O, Antimalarial activities of new pyrrolo [3, 2-f] quinazoline-1, 3-diamine derivatives., Antimicrobial agents and chemotherapy, 49(12), 4928-4933. DOI: 10.1128/AAC.49.12.4928-4933.2005, PMID: 16304154.
  14. Khalil A.A., Hamide S.G.A., Al‐Obaid A.M. and El‐Subbagh H.I. (2003)., Synthesis and in-vitro anticancer evaluation of new 2-substituted mercapto-3H-quinazoline analogs., Arch. Pharm. Med. Chem., 336(2), 95-103. DOI: 10.1002/ardp.200390011, PMID: 12761762.
  15. Jone S. and Fujita E. (1984)., Progress in the chemistry of organic natural products., The quinazoline alkaloids, Springer Publication Vienna, 159-229. ISBN-978-3-7091-8761-6.
  16. Eguchi S., Suzuki T., Okawa T., Matsushita Y., Yashima E. and Okamoto Y. (1996)., Synthesis of Optically Active Vasicinone Based on Intramolecular Aza-Wittig Reaction and Asymmetric Oxidation., J. Org. Chem., 61(21), 7316-7319.
  17. El-Hashash M.A. and Guirguis D.B. (2013)., Synthesis and reactions of 2-(4-bromophenyl)-4H-3, 1-benzoxazine-4-one., European Chemical Bulletin, 2(9), 651-656.
  18. Kacker I.K. and Zaheer S.H. (1951)., Synthesis of Substituted 4-quinazolinones., J. Indian Chem. Soc., 28, 344-346.
  19. Sharma G.V.R. and Robert A.R. (2012)., Synthetic Strategies to Quinazolinones., Int. J. Adv.Pharm. Bio and Chem., 1(3), 337-341.
  20. Rafeeq M., Chittireddy V.R.R. and Dubey P.K. (2015)., Alkylation of 2-substituted quinazolin-4(3H)-one with DMF-DMA., Der pharma chemical, 7(6), 335-357.
  21. Samira I., Patel S., Hasmin M. and Patel S. (2012)., Biological profile of Quinazoline., Int. J. Pharm. and Chem. Sc., 1(4), 1863-1872.