Synthesis of Novel Fused Pyrimidines and Imidazoles as Potential Analgesics from 2-Amino-4-substituted-s-triazino[1,2-a]-benzimidazoles

被引:0
|
作者
El-Feky, Said A. [1 ,2 ]
Thabet, Hamdy Kh. [3 ,4 ]
Mudawi-, Mahmoud M. E. [5 ,6 ]
机构
[1] Northern Border Univ, Fac Pharm, Dept Pharmaceut Chem, Rafha 91911, Saudi Arabia
[2] Zagazig Univ, Dept Pharmaceut Organ Chem, Fac Pharm, Zagazig 44511, Egypt
[3] Northern Border Univ, Fac Arts & Sci, Dept Chem, Rafha 91911, Saudi Arabia
[4] Al Azhar Univ, Fac Sci, Dept Chem, Cairo 11284, Egypt
[5] Northern Border Univ, Fac Pharm, Dept Pharmacol & Toxicol, Rafha 91911, Saudi Arabia
[6] Islamic Univ, Fac Pharm, Dept Pharmacol, Omdurman, Sudan
关键词
D O I
暂无
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
The synthesis of novel fused pyrimidines and imidazole derivatives from 2-amino-s-triazino[1,2a] benzimidazoles 2a-e and 3a-c was successfully carried out by a ring annelation reaction in a very good yield. Compound 3c was screened for analgesic activity against acetic acid irritation and has shown protection equal to the reference drug (diclofenac sodium). The acute toxicity study revealed that compound 3c is safe up to 300 mg/kg and there is no sign and symptoms of toxicity and mortality for 72 hours.
引用
收藏
页码:709 / 718
页数:10
相关论文
共 50 条
  • [1] Microwave-assisted synthesis of substituted 2-amino-1H-imidazoles from imidazo[1,2-a]pyrimidines
    Ermolat'ev, D. S.
    Svidritsky, E. P.
    Babaev, E. V.
    Van der Eycken, E.
    TETRAHEDRON LETTERS, 2009, 50 (37) : 5218 - 5220
  • [2] AZOLE CHEMISTRY .9. NEW SYNTHESIS OF FUSED PYRIMIDINES - TETRAHYDROPYRIMIDO(1,2-A]BENZIMIDAZOLES
    ALPER, H
    PEPPER, L
    CANADIAN JOURNAL OF CHEMISTRY-REVUE CANADIENNE DE CHIMIE, 1975, 53 (06): : 894 - 897
  • [3] Synthesis of substituted 2-amino-1-arylideneaminoimidazoles and 1-arylideneaminoimidazo[1,2-a]imidazoles
    Krimer, MZ
    Makaev, FZ
    Styngach, EP
    Koretsky, AG
    Pogrebnoy, SI
    Kochug, AI
    KHIMIYA GETEROTSIKLICHESKIKH SOEDINENII, 1996, (09): : 1209 - 1213
  • [4] CYCLIZATION REACTIONS OF 2-AMINOBENZIMIDAZOLES TO S-TRIAZINO[1,2-A]BENZIMIDAZOLES
    AUGUSTIN, M
    KUPPE, KR
    TETRAHEDRON, 1974, 30 (18) : 3533 - 3538
  • [5] Synthesis of a Novel Library of 1-Substituted Pyrido[1,2-a]benzimidazoles
    Gadde, Satyanarayana
    Leung, Yun Cheuk
    Bhadbade, Mohan
    Cheung, Belamy B.
    Black, David StC
    Kumar, Naresh
    AUSTRALIAN JOURNAL OF CHEMISTRY, 2020, 73 (12) : 1208 - 1218
  • [6] Synthesis of Novel Disubstituted Pyrazolo[1,5-a]pyrimidines, Imidazo[1,2-a]pyrimidines, and Pyrimido[1,2-a]benzimidazoles Containing Thioether and Aryl Moieties
    Li, Gang
    Zhang, Zun-Ting
    Dai, Li-Yan
    Du, Yin-Li
    Xue, Dong
    HELVETICA CHIMICA ACTA, 2012, 95 (06) : 989 - 997
  • [7] New Synthesis of peri-Fused Tetrahydro[1,3]diazepino[1,2-a]benzimidazoles from 1-Aroylmethyl-2-[(4-hydroxybutyl)amino]benzimidazoles
    Kuz'menko, T. A.
    Divaeva, L. N.
    Morkovnik, A. S.
    RUSSIAN JOURNAL OF ORGANIC CHEMISTRY, 2020, 56 (10) : 1728 - 1732
  • [8] New Synthesis of peri-Fused Tetrahydro[1,3]diazepino[1,2-a]benzimidazoles from 1-Aroylmethyl-2-[(4-hydroxybutyl)amino]benzimidazoles
    T. A. Kuzʼmenko
    L. N. Divaeva
    A. S. Morkovnik
    Russian Journal of Organic Chemistry, 2020, 56 : 1728 - 1732
  • [9] A convenient approach to the synthesis of 2-aryl-4-alkyl-1,3,5-triazino[1,2-a]benzimidazoles
    Reddy, BS
    Sambaiah, T
    Reddy, KK
    INDIAN JOURNAL OF CHEMISTRY SECTION B-ORGANIC CHEMISTRY INCLUDING MEDICINAL CHEMISTRY, 1998, 37 (12): : 1283 - 1285
  • [10] 1,2-FUSED PYRIMIDINES .6. SUBSTITUTED 2-AMINO-4H-PYRIDO[1,2-A]PYRIMIDIN-4-ONES WITH ANTIPLATELET ACTIVITY
    ROMA, G
    DIBRACCIO, M
    LEONCINI, G
    APRILE, B
    FARMACO, 1993, 48 (09): : 1225 - 1238