65414-18-8Relevant academic research and scientific papers
3-Mercapto-1,2,4-triazoles and N-acylated thiosemicarbazides as metallo-β-lactamase inhibitors
Faridoon,Hussein, Waleed M.,Vella, Peter,Islam, Nazar Ul,Ollis, David L.,Schenk, Gerhard,McGeary, Ross P.
, p. 380 - 386 (2012/02/04)
The production of β-lactamases is an effective strategy by which pathogenic bacteria can develop resistance against β-lactam antibiotics. While inhibitors of serine-β-lactamases are widely used in combination therapy with β-lactam antibiotics, there are no clinically available inhibitors of metallo-β-lactamases (MBLs), and so there is a need for the development of such inhibitors. This work describes the optimisation of a lead inhibitor previously identified by fragment screening of a compound library. We also report that thiosemicarbazide intermediates in the syntheses of these compounds are also moderately potent inhibitors of the IMP-1 MBL from Pseudomonas aeruginosa. The interactions of these inhibitors with the active site of IMP-1 were examined using in silico methods.
Laser Flash Photolysis of tert-Butyl Aroylperbenzoates: Kinetics of the Singlet and Triplet States and the Aroylphenyl Radicals
Shah, Bipin K.,Neckers, Douglas C.
, p. 1830 - 1835 (2007/10/03)
tert-Butyl aroylperbenzoates (1-4) were studied by laser flash photolysis (LFP). LFP (380 nm, pulse width ～350 fs) of 2 and 3 allowed direct observation of their singlet states, which showed broad absorption (λmax ～ 625 nm; τ ～ 20 and ～7.9 ps, respectively). The triplet state of each (λmax ～ 530-560 nm) rapidly dissociates by O-O cleavage as indicated by the short triplet lifetimes (e.g., triplet lifetime of 3 ～0.74 ns). The ～550 nm absorption obtained from the 355 nm LFP (pulse width ～7 ns) of 1, 2, and 4 has been assigned to the corresponding aroylphenyl radicals. Two representative radicals (4-benzoylphenyl 5 and 3-(4′-methylbenzoyl)phenyl 6) investigated in detail showed solvent-dependent lifetimes. Absolute bimolecular rate constants of reactions of these radicals with various quenchers including double-bond-containing monomers have been observed to range from 7.56 × 107 to 1.68 × 109 M-1 s-1 in CCl4 at room temperature. A possible structure of the aroylphenyl radicals and the transition responsible for the 550 nm absorption are discussed.
Synthesis, Crystal Structures, and Laser Flash Photolysis of tert-Butyl Aroylperbenzoates
Shah, Bipin K.,Neckers, Douglas C.
, p. 8368 - 8372 (2007/10/03)
tert-Butyl aroylperbenzoates (1-7) were synthesized. Single-crystal structures for 2 and 5 show that the perester and benzophenone carbonyl groups are almost coplanar in each. Laser flash photolysis (LFP, λex = 355 nm) of 1-5 in CCl4
