Synthesis, analgesic and anti-inflammatory activities of substituted benzoylthioureas

Tutuk Budiati, Suzana ., Siti Surdijati

Abstract


Three compounds (i.e.  benzoylthiourea,  4-nitrobenzoylthiourea,  and  4-chlorobenzoylthiourea) have  been  synthesized  from  ammonium  thiocyanate, substituted benzoyl chlorides, and ammonia as starting materials. The structures of  sythesized  compounds  were  confirmed  by  means  of  ultra-violet,  infrared, magnetic resonance, and mass spectroscopy. All compounds were evaluated for their  analgesic  and  anti-inflamatory  activities  by  tail-flick  technique  and carragenan-induced  paw  oedema  test  respectively.  Substitution of p-NO2 and p-Cl  group  to  benzoylthiourea  increased  the  analgesic  and  anti-inflamatory activities.  The  two  compounds,  4-nitrobenzoylthiourea  and  4-chlorobenzoylthiourea,  were  significantly  more  potent  as  analgesic  but  their  antiinflamatory actvity was weaker than Na-diclofenac.

Keywords: benzoylthioureas, p-Cl dan p-NO2substituents, analgesic and anti-inflamator activities

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References


Alagarsamy V, Murugananthan G., and Venkateshperumal R., 2003., Synthesis, analgesic, antiinflamatory and antibacterial activities of some novel 2-methyl-3-substituted quinazolin-4-(3H)-ones. Bio Pharm Bull. 26, 12, 1711-1714.

Alagarsamy V, Rajesh R, Ramaseshu M, Vijaykumar S, Ramaseshu K. V., and Duraianandakumar T., 2004, Synthesis, analgesic, anti-inflamatory and antibacterial activities of some novel 2-methylthio-3-substituted quinazolin-4(3H)-ones. Bio Pharm Bull. 27, 652-656.

Kachhadia V. V., Patel M. R., and Joshi H. S., 2004., Heterocyclic system containing S/N regioselective nukleophilic competition: facile synthesis, antitubercular and antimicrobial activity of thiohydantoins and iminothiazolidinones containing the benzo[b]thiophene moiety. J Serb Chem Soc. 70, 2, 153-161.

Katzung B. G., 2002., Farmakologi Dasar dan Klinik. Buku 2, edisi 8 (penerjemah : Bagian Farmakologi Fakultas Kedokteran Universitas Airlangga). Salemba .Medika Jakarta, : 291-323.

Kossakowski J., and Struga M. Synthesis of thiourea derivates of 1H-Isoindol-1,3(2H)-dione as potential antiviral agents. Ann Univ Mariae Currie-Sklodowska Lublin-Polonia.,2006; 111, 186-191.

Limban, C., Chifriuc, M. C. B, Missir, A. V, Chirita I. C, and Bleotu C., 2008. Antimicrobial activity of some new thioureides devided from 2-(4-chlorophenoxymethyl)benzoic acids, part 13, [Online] http://www.mdpi.org /moleculas.com. [2008, March 4]

Siswandono., 1999., Modifikasi struktur dan hubungan struktur-aktivitas senyawa-senyawa baru

turunan benzoilurea. Disertasi. Program Pasca Sarjana Universitas Airlangga, Surabaya.

Suzana, Budiati T, dan Ekowati J., 2004., Sintesis senyawa benzoiltiourea dan uji aktivitas sebagai penekan saraf pusat pada mencit (Mus musculus). Laporan Penelitian. Fakultas Farmasi Universitas Airlangga, Surabaya.

Thomas G., 2000., Medicinal Chemistry : an Introduction. John Wiley and Sons, Ltd. Chichester, England. : 42-67.

Thompson, E. B., 1990., Drug bioscreening: Drug evaluatio n techniques in pharmacology. VCH Publisher Inc. New York.: 53-78

Xu, X., Qian, X., Li, Z., Huang, Q., and Chen G., 2003., Synthesis and insecticidal activity of new substituted N-aryl-N’-benzoylthiourea compounds, J. of Fluorine Chem. 121, 51-54.




DOI: http://dx.doi.org/10.14499/indonesianjpharm0iss0pp68-76

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