N-((1,3-Diphenyl-1H-pyrazol-4-yl)methyl)anilines: A novel class of anti-RSV agents.

作者: Rossella Fioravanti , Nicoletta Desideri , Mariangela Biava , Paolo Droghini , Elena Maria Atzori

DOI: 10.1016/J.BMCL.2015.04.006

关键词:

摘要: Abstract A series of N-((1,3-diphenyl-1H-pyrazol-4-yl)methyl)anilines were synthesized and evaluated in vitro for cytotoxicity antiviral activity against a large panel viruses. Most the tested compounds interfered with RSV replication micromolar concentrations (EC50s ranging from 5 μM to 28 μM). SAR studies suggested that presence trifluoromethyl group R1 abolished anti-RSV enhanced while best results term both selectivity obtained by introduction chlorine or bromine atom.

参考文章(17)
Gregory A Prince, An update on respiratory syncytial virus antiviral agents. Expert Opinion on Investigational Drugs. ,vol. 10, pp. 297- 308 ,(2001) , 10.1517/13543784.10.2.297
Y. AUJARD, B. FAUROUX, Risk factors for severe respiratory syncytial virus infection in infants Respiratory Medicine. ,vol. 96, ,(2002) , 10.1053/RMED.2002.1295
Cinzia Conti, Luca Proietti Monaco, Nicoletta Desideri, Synthesis and anti-rhinovirus activity of novel 3-[2-(pyridinyl)vinyl]substituted -2H-chromenes and -4H-chromen-4-ones. Bioorganic & Medicinal Chemistry. ,vol. 22, pp. 1201- 1207 ,(2014) , 10.1016/J.BMC.2013.11.054
Michael Eisenhut, Extrapulmonary manifestations of severe RSV bronchiolitis The Lancet. ,vol. 368, pp. 988- 988 ,(2006) , 10.1016/S0140-6736(06)69409-9
Shinichiro Morichi, Hisashi Kawashima, Hiroaki Ioi, Gaku Yamanaka, Yasuyo Kashiwagi, Akinori Hoshika, Tetsuo Nakayama, Yasuo Watanabe, Classification of acute encephalopathy in respiratory syncytial virus infection Journal of Infection and Chemotherapy. ,vol. 17, pp. 776- 781 ,(2011) , 10.1007/S10156-011-0259-5
M.A. Kira, M.O. Abdel-Rahman, K.Z. Gadalla, The vilsmeier-haack reaction - III Cyclization of hydrazones to pyrazoles Tetrahedron Letters. ,vol. 10, pp. 109- 110 ,(1969) , 10.1016/S0040-4039(01)88217-4
Fabio Sparatore, Giuseppe Paglietti, Sabrina Pricl, Gabriele Giliberti, Sylvain Blois, Cristina Ibba, Giuseppina Sanna, Roberta Loddo, Paolo La Colla, Michele Tonelli, Matteo Simone, Bruno Tasso, Federica Novelli, Vito Boido, Antiviral activity of benzimidazole derivatives. II. Antiviral activity of 2-phenylbenzimidazole derivatives. Bioorganic & Medicinal Chemistry. ,vol. 18, pp. 2937- 2953 ,(2010) , 10.1016/J.BMC.2010.02.037
Harish Nair, D James Nokes, Bradford D Gessner, Mukesh Dherani, Shabir A Madhi, Rosalyn J Singleton, Katherine L O'Brien, Anna Roca, Peter F Wright, Nigel Bruce, Aruna Chandran, Evropi Theodoratou, Agustinus Sutanto, Endang R Sedyaningsih, Mwanajuma Ngama, Patrick K Munywoki, Cissy Kartasasmita, Eric AF Simões, Igor Rudan, Martin W Weber, Harry Campbell, Global burden of acute lower respiratory infections due to respiratory syncytial virus in young children: a systematic review and meta-analysis The Lancet. ,vol. 375, pp. 1545- 1555 ,(2010) , 10.1016/S0140-6736(10)60206-1
William W. Thompson, David K. Shay, Eric Weintraub, Lynnette Brammer, Nancy Cox, Larry J. Anderson, Keiji Fukuda, Mortality Associated With Influenza and Respiratory Syncytial Virus in the United States JAMA. ,vol. 289, pp. 179- 186 ,(2003) , 10.1001/JAMA.289.2.179