Synthesis and preliminary in vitro evaluation of antimycobacterial activity of new pyrrolo[1,2-a]quinoxaline-carboxylic acid hydrazide derivatives

被引：38
作者：
Guillon, J
Reynolds, RC
Leger, JM
Guie, MA
Massip, S
Dallemagne, P
Jarry, C
机构：
[1] Univ Bordeaux 2, UFR Sci Pharmaceut, EA Pharmacochim 2962, F-33076 Bordeaux, France
[2] NIAID, TAACF, So Res Inst, Birmingham, AL 35255 USA
[3] Univ Caen, UFR Sci Pharmaceut, Ctr Etud & Rech Med Normandie, F-14032 Caen, France
来源：
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | 2004年 / 19卷 / 06期
关键词：
pyrrolo[1,2-a]quinoxaline-carboxylic acid hydrazide derivatives; Mycobacterium tuberculosis; antimycobacterial agents; tuberculosis;
D O I：
10.1080/14756360412331280464
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：
New pyrrolo[1,2-a]quinoxaline-2- or -4-carboxylic acid hydrazide derivatives were synthesized from nitroaniline or 1,2-phenylenediamine, and evaluated in vitro for their antimycobacterial activity as part of a TAACF TB screening program. Two compounds 7c and 13 showed an interesting activity at 6.25 mug/mL against Mycobacterium tuberculosis H(37)Rv, with a 94 and 100 percentage inhibition, respectively.
引用
收藏
页码：489 / 495
页数：7
相关论文
共 43 条
  • [1] Synthesis and antimycobacterial evaluation of new trans-cinnamic acid hydrazide derivatives
    Carvalho, Samir A.
    da Silva, Edson F.
    de Souza, Marcus V. N.
    Lourenco, Maria C. S.
    Vicente, Felipe R.
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2008, 18 (02) : 538 - 541
  • [2] Cytotoxicity and Antimycobacterial Properties of Pyrrolo[1,2-a]quinoline Derivatives: Molecular Target Identification and Molecular Docking Studies
    Venugopala, Katharigatta N.
    Uppar, Vijayakumar
    Chandrashekharappa, Sandeep
    Abdallah, Hassan H.
    Pillay, Melendhran
    Deb, Pran Kishore
    Morsy, Mohamed A.
    Aldhubiab, Bandar E.
    Attimarad, Mahesh
    Nair, Anroop B.
    Sreeharsha, Nagaraja
    Tratrat, Christophe
    Jaber, Abdulmuttaleb Yousef
    Venugopala, Rashmi
    Mailavaram, Raghu Prasad
    Al-Jaidi, Bilal A.
    Kandeel, Mahmoud
    Haroun, Michelyne
    Padmashali, Basavaraj
    ANTIBIOTICS-BASEL, 2020, 9 (05):
  • [3] Synthesis and anti-mycobacterial evaluation of some pyrazine-2-carboxylic acid hydrazide derivatives
    Abdel-Aziz, Mohamed
    Abdel-Rahman, Hamdy M.
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2010, 45 (08) : 3384 - 3388
  • [4] Novel Derivatives of Quinoxaline-2-carboxylic Acid 1,4-Dioxides as Antimycobacterial Agents: Mechanistic Studies and Therapeutic Potential
    Frolova, Svetlana G.
    Vatlin, Aleksey A.
    Maslov, Dmitry A.
    Yusuf, Buhari
    Buravchenko, Galina I.
    Bekker, Olga B.
    Klimina, Ksenia M.
    Smirnova, Svetlana V.
    Shnakhova, Lidia M.
    Malyants, Irina K.
    Lashkin, Arseniy I.
    Tian, Xirong
    Alam, Md Shah
    Zatonsky, George V.
    Zhang, Tianyu
    Shchekotikhin, Andrey E.
    Danilenko, Valery N.
    PHARMACEUTICALS, 2023, 16 (11)
  • [5] Synthesis and antimycobacterial activity of new quinoxaline-2-carboxamide 1,4-di-N-oxide derivatives
    Moreno, Elsa
    Ancizu, Saioa
    Perez-Silanes, Silvia
    Torres, Enrique
    Aldana, Ignacio
    Monge, Antonio
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2010, 45 (10) : 4418 - 4426
  • [6] Synthesis, antimycobacterial activities and phototoxic evaluation of 5H-thiazolo[3,2-a]quinoline-4-carboxylic acid derivatives
    Dinakaran, Murugesan
    Senthilkumar, Palaniappan
    Yogeeswari, Perumal
    China, Arnab
    Nagaraja, Valakunja
    Sriram, Dharmarajan
    MEDICINAL CHEMISTRY, 2008, 4 (05) : 482 - 491
  • [7] Microwave-Assisted Synthesis and Characterization of Novel 1,3,4-Oxadiazole Derivatives and Evaluation of In Vitro Antimycobacterial Activity
    Devaraji, Mahalakshmi
    Thanikachalam, Punniyakoti, V
    CUREUS JOURNAL OF MEDICAL SCIENCE, 2024, 16 (09)
  • [8] Design, Synthesis and Antimycobacterial Activity of Novel Imidazo[1,2-a]pyridine Amide-Cinnamamide Hybrids
    Li, Linhu
    Li, Zhuorong
    Liu, Mingliang
    Shen, Weiyi
    Wang, Bin
    Guo, Huiyuan
    Lu, Yu
    MOLECULES, 2016, 21 (01)
  • [9] Synthesis and biological evaluation of quinoxaline di-N-oxide derivatives with in vitro trypanocidal activity
    Perez-Silanes, Silvia
    Torres, Enrique
    Arbillaga, Leire
    Varela, Javier
    Cerecetto, Hugo
    Gonzalez, Mercedes
    Azqueta, Amaya
    Moreno-Viguri, Elsa
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2016, 26 (03) : 903 - 906
  • [10] Synthesis and in vitro evaluation of antimycobacterial and cytotoxic activity of new α,β-unsaturated amide, oxazoline and oxazole derivatives from L-serine
    Aguirre-Renteria, Saul A.
    Carrizales-Castillo, Juan J. J.
    Camacho Corona, Maria del Rayo
    Hernandez-Fernandez, Eugenio
    Garza-Gonzalez, Elvira
    Rivas-Galindo, Veronica M.
    Arredondo-Espinoza, Eder
    Avalos-Alanis, Francisco G.
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2020, 30 (09)
12345