RESUMO
This article elaborates on the important recent developments in the enzymatic transformation of penicillins to 6-aminopenicillanic acid (6-APA), which is the basic raw material for the industrial production of semisynthetic penicillins such as amoxycillin and ampicillin. Particular emphasis is placed on the improvements in purification, stability, and immobilization of the enzymes, (i.e. penicillin acylases) used for these transformations.
RESUMO
Organomercury(II)-purine derivatives of the type, p-MeOC(6)H(4)HgL(1) (I), p-NO(2)C(6)H(4)HgCl(L(2))(II), p-MeC(6)H(4)HgCl(L(3))(III) and p-NO(2)C(6)H(4)HgCl(L(3))(IV) [ HL(1) = theophylline, L(2) = theobromine, L(3) = caffeine] have been synthesised and characterised on the basis of spectral studies (IR, UV, (1)H & (13)C NMR). The complexes have been screened for anti-inflammatory activity.
RESUMO
A few organomercury (II) complexes involving anti-carcinogenic ligands have been synthesized. The compounds are of the type p-MeOC6H4HgL1 (I), p-NO2C6H4HgL2 (II), p-MeOC4H4HgL3 (III) and p-MeC6H4HgL4 (IV) (HL1-6-mercaptopurine, HL2-6-thioguanine, HL3-5-fluorouracil, L4-phenyldithiocarbazate). Their composition has been determined from elemental analysis. Thin layer chromatography (TLC) studies demonstrate that the compounds are pure. Conductance measurement reveal that these derivatives are non-electrolytes. From IR and UV spectral studies the bonding modes of the ligands to the mercury (II) ion have been elucidated. The stoichiometry of the compounds has been confirmed on the basis of 1H and 13C NMR spectra. Some preliminary results of anti-neoplastic activity are reported.
Assuntos
Antineoplásicos/síntese química , Compostos Organomercúricos/síntese química , Antineoplásicos/química , Ensaios de Seleção de Medicamentos Antitumorais , Fluoruracila/análogos & derivados , Espectroscopia de Ressonância Magnética , Mercaptopurina/análogos & derivados , Compostos Organomercúricos/química , Espectrofotometria Infravermelho , Espectrofotometria Ultravioleta , Tioguanina/análogos & derivados , Células Tumorais CultivadasRESUMO
Organomercury(II) complexes of the type, p-MeOC6H4HgL1 (I), p-NO2C6H4HgL2 (II), p-MeOC6H4HgL3 (III) and p-MeC6H4HgL4 (IV) (HL1-6-mercaptopurine, HL2-6-thioguanine, HL3-5-fluorouracil, L4-phenyldithiocarbazate) have been screened against the following cell panels: leukemia, non-small cell lung cancer, small cell lung cancer, brain cancer, melanoma, ovarian cancer and renal cancer. The variation in anti-neoplastic activity has been correlated with the structural parameters of the complexes.
Assuntos
Antineoplásicos/farmacologia , Compostos Organomercúricos/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Fluoruracila/análogos & derivados , Humanos , Hidrazinas , Mercaptopurina/análogos & derivados , Tioguanina/análogos & derivados , Células Tumorais CultivadasRESUMO
A number of organomercury(II) complexes of kojic acid (HL1, I) and maltol (HL2, II) of the type p-XC6H4HgL1 (III) and p-XC6H4HgL2 (IV) [X = Me, MeO, NO2] have been synthesized and characterized. [formula: see text] Conductance measurements indicate the nonelectrolyte behavior of the complexes. From IR and UV studies, the bonding modes of the ligands to the organomercury(II) moieties have been elucidated. The 1H and 13C NMR spectra support the stoichiometry of the complexes. The fragmentation pattern has been analyzed on the basis of mass spectra. From thermal studies (TG and DTA), various kinetic and thermodynamic parameters for thermal degradation have been enumerated. The complexes have been screened against some pathogenic bacterial strains. The bactericidal activity has been correlated with the thermal data.
