Both the instrumentation required for two photon excitation (TPE) and tissue damage possibility by high intensity laser lights could impede TPE-induced CO delivery in hospital settings. Herein we report two Mn(i)-based photoCORMs with a fac-{Mn(CO)} moiety that exhibit facile CO release upon simple exposure to light within the phototherapeutic region (no TPE required).
View Article and Find Full Text PDFFollowing the success of Auranofin as an anti-arthritic drug, search for novel gold drugs has afforded a large number of [L-Au(PPh )] complexes that exhibit notable salutary effects. Unlike Au(III)-containing species, these gold complexes with {Au(PPh )} moiety are stable in biological media and readily exchange L with S- and Se-containing enzymes or proteins. Such exchange leads to rapid reduction of microbial loads or induction of apoptotic cell death at malignant sites.
View Article and Find Full Text PDFAs part of the quest for new gold drugs, we have explored the efficacy of three gold complexes derived from the tuberculosis drug pyrazinamide (PZA), namely, the gold(I) complex [Au(PPh)(PZA)]OTf (, OTf = trifluoromethanesulfonate) and two gold(III) complexes [Au(PZA)Cl] () and [Au(PZO)Cl] (, PZO = pyrazinoic acid, the metabolic product of PZA) against two mycobacteria, and . Only complex with the {Au(PPh)} moiety exhibits significant bactericidal activity against both strains. In the presence of thiols, gives rise to free PZA and {Au(PPh)}-thiol polymeric species.
View Article and Find Full Text PDFTwo cationic Au(I) complexes derived from aryl-benzothiazoles, namely [(PPh)Au(pbt)](OTf) (1) and [(PPh)Au(qbt)](OTf) (2) (where pbt = 2‑(pyridyl)benzothiazole and qbt = (quinolyl)benzothiazole, and OTf = trifluoromethanesulfonate anion), have been synthesized and structurally characterized by X-ray crystallography. Both complexes exhibit strong antibacterial effects against Gram-negative bacteria such as Acinetobacter baumannii and Pseudomonas Aeruginosa. Results of examination of the reactions of 1 and 2 indicate that these cationic Au(I) complexes rapidly cross the bacterial membrane and exert drug action by disrupting cellular function(s) through binding of cytosolic thiol-containing peptides (such as glutathione) and proteins to the highly reactive (PPh)Au intermediate formed upon in situ dissociation of pbt or qbt.
View Article and Find Full Text PDFPhotoCORMs (photo-active CO-releasing molecules) have emerged as a class of CO donors where the CO release process can be triggered upon illumination with light of appropriate wavelength. We have recently reported an Mn-based photoCORM, namely [MnBr(pbt)(CO)] [pbt is 2-(pyridin-2-yl)-1,3-benzothiazole], where the CO release event can be tracked within cellular milieu by virtue of the emergence of strong blue fluorescence. In pursuit of developing more such trackable photoCORMs, we report herein the syntheses and structural characterization of two Mn-carbonyl complexes, namely fac-tricarbonylchlorido[2-(pyridin-2-yl)-1,3-benzothiazole-κN,N']manganese(I), [MnCl(CHNS)(CO)], (1), and fac-tricarbonylchlorido[2-(quinolin-2-yl)-1,3-benzothiazole-κN,N']manganese(I), [MnCl(CHNS)(CO)], (2).
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