Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Frederic Douelle"'
Autor:
Diego Gonzàlez Cabrera, Frederic Douelle, David Waterson, Jeremy N. Burrows, Yassir Younis, Quoc Wu, Susan A. Charman, Michael J Witty, Karen L. White, Tzu-Shean Feng, Kelly Chibale, Sergio Wittlin, Aloysius T. Nchinda, Eileen Ryan
Publikováno v:
Journal of Medicinal Chemistry. 54:7713-7719
An aminomethylthiazole pyrazole carboxamide lead 3 with good in vitro antiplasmodial activity [IC(50): 0.08 μM (K1, chloroquine and multidrug resistant strain) and 0.07 μM (NF54, chloroquine sensitive strain)] and microsomal metabolic stability was
Publikováno v:
Organic Letters. 9:1931-1934
The intramolecular iodo-aldol cyclization of alpha-substituted enoate aldehydes and ketones is described. Using prochiral starting materials, the reaction produces hetero- and carbocycles containing quaternary centers adjacent to secondary or tertiar
Publikováno v:
Tetrahedron Letters. 43:5361-5365
Very efficient, simple, and high yield procedures for the transformation of heterocyclic aldehydes into heterocyclic methylidene-p-hydroxyanilines, heterocyclic α-iminonitriles, and finally into heterocyclic α-oxoacetic acids were described. Consid
Autor:
Claire Le Manach, Diego Gonzàlez Cabrera, Frederic Douelle, Sandra Duffy, Leslie J. Street, Dale Taylor, Michael J Witty, Kelly Chibale, Yassir Younis, Sergio Wittlin, Corinne March, Susan A. Charman, David Waterson, Vicky M. Avery, Aloysius T. Nchinda, Karen L. White, Eileen Ryan, Lubbe Wiesner
Publikováno v:
Journal of medicinal chemistry. 57(6)
A novel class of imidazopyridazines identified from whole cell screening of a SoftFocus kinase library was synthesized and evaluated for antiplasmodial activity against K1 (multidrug resistant strain) and NF54 (sensitive strain). Structure-activity r
Autor:
Leslie J. Street, Claire Le Manach, Karen L. White, Sergio Wittlin, Sandra Duffy, Frederic Douelle, Aloysius T. Nchinda, Diego Gonzàlez Cabrera, Dale Taylor, Lubbe Wiesner, Vicky M. Avery, Sridevi Bashyam, Tzu-Shean Feng, Tanya Paquet, Yassir Younis, Kelly Chibale, Yuvaraj Sambandan, Susan A. Charman, Michael J Witty, Carmen de Kock, David Waterson, Mohammed K Zabiulla
Publikováno v:
Journal of medicinal chemistry. 57(3)
A novel series of 2,4-diaminothienopyrimidines with potential as antimalarials was identified from whole-cell high-throughput screening of a SoftFocus ion channel library. Synthesis and structure-activity relationship studies identified compounds wit
Autor:
Tanya Paquet, Leslie J. Street, Karen L. White, Sridevi Bashyam, Mohammed K Zabiulla, Yassir Younis, Claire Le Manach, Diego Gonzàlez Cabrera, David Waterson, Frederic Douelle, Michael J Witty, Sergio Wittlin, Aloysius T. Nchinda, Jayan T. Joseph, Susan A. Charman, Kelly Chibale
Publikováno v:
Journal of medicinal chemistry. 56(21)
Replacement of the pyridine core of antimalarial 3,5-diaryl-2-aminopyridines led to the identification of a novel series of pyrazine analogues with potent oral antimalarial activity. However, other changes to the pyridine core and replacement or subs
Autor:
Eileen Ryan, Karen L. White, Mohammed K Zabiulla, Leslie J. Street, Diego Gonzàlez Cabrera, Sridevi Bashyam, Kasiram Katneni, Michael J Witty, David Waterson, Tzu-Shean Feng, Jolanda Kamber, Claire Le Manach, Yassir Younis, Oliver D. Montagnat, Frederic Douelle, Christian Scheurer, Kelly Chibale, Jayan T. Joseph, Susan A. Charman, Sergio Wittlin, Aloysius T. Nchinda
Publikováno v:
Journal of medicinal chemistry. 55(24)
In an effort to address potential cardiotoxicity liabilities identified with earlier frontrunner compounds, a number of new 3,5-diaryl-2-aminopyridine derivatives were synthesized. Several compounds exhibited potent antiplasmodial activity against bo
Autor:
Karen L. White, David M. Shackleford, Sergio Wittlin, Mohammed K Zabiulla, Jayan T. Joseph, Aloysius T. Nchinda, Sridevi Bashyam, Claire Le Manach, David J. Hardick, Susan A. Charman, Vicky M. Avery, Yassir Younis, Ravi K. Bhamidipati, Frederic Douelle, Michael J Witty, Tzu-Shean Feng, Kelly Chibale, Diego Gonzàlez Cabrera, David Waterson, Kasiram Katneni, Julia Morizzi, Janne Mannila, Sandra Duffy
Publikováno v:
Journal of medicinal chemistry. 55(7)
A novel class of orally active antimalarial 3,5-diaryl-2-aminopyridines has been identified from phenotypic whole cell high-throughput screening of a commercially available SoftFocus kinase library. The compounds were evaluated in vitro for their ant
Publikováno v:
ChemInform. 33
Autor:
Diego Gonzàlez Cabrera, Frederic Douelle, Claire Le Manach, Ze Han, Tanya Paquet, Dale Taylor, Mathew Njoroge, Nina Lawrence, Lubbe Wiesner, David Waterson, MichaelJ. Witty, Sergio Wittlin, LeslieJ. Street, Kelly Chibale
Publikováno v:
Journal of Medicinal Chemistry; Sep2015, Vol. 58 Issue 18, p7572-7579, 8p