A Chiral Benzoquinolizine-2-carboxylic Acid Arginine Salt Active against
Vancomycin-Resistant <i>Staphylococcus </i><i>a</i><i>ureus</i>
Noel J. de Souza
Shrikant V. Gupte
Prasad K. Deshpande
Vijaya N. Desai
Satish B. Bhawsar
Ravindra D. Yeole
Milind C. Shukla
Jacob Strahilevitz
David C. Hooper
Bülent Bozdogan
Peter C. Appelbaum
Michael R. Jacobs
Nitin Shetty
Mahesh V. Patel
Rasendrakumar Jha
Habil F. Khorakiwala
10.1021/jm050035f.s001
https://acs.figshare.com/articles/journal_contribution/A_Chiral_Benzoquinolizine_2_carboxylic_Acid_Arginine_Salt_Active_against_Vancomycin_Resistant_i_Staphylococcus_i_i_a_i_i_ureus_i_/3273289
There is an urgent medical need for novel antibacterial agents to treat hospital infections,
specially those caused by multidrug-resistant Gram-positive pathogens. The need may also be
fulfilled by either exploring antibacterial agents having new mechanism of action or expanding
known classes of antibacterial drugs. The paper describes a new chemical entity, compound
<b>21</b>, derived from hitherto little known “floxacin”. The choice of the entity was made from a
series of synthesized prodrugs and salts of the active chiral benzoquinolizine carboxylic acid,
<i>S</i>-(−)-nadifloxacin. The chemistry, physicochemical characteristics, and essential bioprofile of
<b>21</b> qualifies it for serious consideration as a novel drug entity against hospital infections of
multi-drug-resistant <i>Staphylococcus aureus</i>, and its progress up to clinical phase I trials in
humans is described.
2005-08-11 00:00:00
Staphylococcu
hospital infections
agent
novel drug entity
chiral benzoquinolizine carboxylic acid