139244-46-5Relevant academic research and scientific papers
Regioselective enzymatic acylation as a tool for producing solution- phase combinatorial libraries
Mozhaev, Vadim V.,Budde, Cheryl L.,Rich, Joseph O.,Usyatinsky, Alexander Ya.,Michels, Peter C.,Khmelnitsky, Yuri L.,Clark, Douglas S.,Dordick, Jonathan S.
, p. 3971 - 3982 (1998)
A simple combinatorial strategy for sequential regioselective enzymatic acylation of multifunctional lead compounds has been developed and demonstrated using a polyhydroxylated flavonoid, bergenin, as a model. The approach is based on the ability of different enzymes to regioselectively acylate different sizes on a lead molecule without affecting other similar functional groups. In sharp contrast to enzymatic acylation, conventional chemical acylation methods showed almost complete lack of regioselectivity. The enzymatic strategy was applied successfully to produce a solution phase combinatorial library of 167 distinct selectively acylated derivatives of bergenin on a robotic workstation in a 96-well plate format. General applicability of the automated combinatorial biocatalysis strategy is discussed.
Antimycobacterial Activity of a Series of Pyrazinoic Acid Esters
Cynamon, Michael H.,Klemens, Sally P.,Chou, Tso-Sheng,Gimi, Rayomand H.,Welch, John T.
, p. 1212 - 1215 (2007/10/02)
A series of pyrazinoic acid esters has been prepared and evaluated for in vitro antimycobacterial activity.Several of the pyrazinoate esters have substantially better activity than the first-line antituberculous agent pyrazinamide against susceptible isolates of Mycobacterium tuberculosis as well as activity against pyrazinamide-resistant isolates.The minimal inhibitory concentrations (MICs) were lower for each organism and at each pH than the MICs for pyrazinamide.The esters have activity against Mycobacterium bovis and Mycobacterium kansasii, two species resistant to pyrazinamide, but not against Mycobacterium avium complex.
