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Synthesis and enzymatic evaluation of the guanosine analogue 2-amino-6-mercapto...
Neto,Brenno A. D.; Lapis,Alexandre A. M.; Netz,Paulo A.; Spencer,John; Dias,Silvio L. P.; Tamborim,Silvia M.; Basso,Luiz A.; Santos,Diógenes S.A modified experimental procedure for the synthesis of MESG (2-amino-6-mercapto-7-methylpurine ribonucleoside) 1 has been successfully performed and its full characterization is presented. High resolution ESI(+)-MSMS indicates both the nucleoside bond cleavage as the main fragmentation in the gas phase and a possible S N1 mechanism. Ab initio transition state calculations based on the blue print transition stat...
An inorganic complex that inhibits Mycobacterium tuberculosis enoyl reductase a...
Basso,Luiz A.; Schneider,Cristopher Z.; Santos,Anderson J. A. B. dos; Santos Jr,André A. dos; Campos,Maria M.; Souto,André A.; Santos,Diógenes S.Here we describe the inhibitory activity of IQG607, pentacyano(isoniazid)ferrate(II), on isoniazid-sensitive and isoniazid-resistant strains of Mycobacterium tuberculosis, its oral toxicity, and efforts to adapt IQG607 synthesis to large chemical reactors. IQG607 represents a promising chemotherapeutic agent aiming at the inhibition of a validated and druggable molecular target.
Kinetic and equilibrium mechanisms of substrate binding to Mycobacterium tuberc...
Vasconcelos,Igor B.; Basso,Luiz A.; Santos,Diógenes S.Tuberculosis (TB) remains the leading cause of mortality due to a single bacterial pathogen, Mycobacterium tuberculosis. There is a need for the development of new antimycobacterial agents. M. tuberculosis 2-trans-enoyl-ACP(CoA) reductase (InhA) is the main target of isoniazid, the most prescribed anti-TB agent. Here we present pre-steady state kinetics and equilibrium data of 2-trans-dodecenoyl-CoA substrate b...