Lapachol was chemically modified to obtain its thiosemicarbazone and semicarbazone derivatives. These compounds were tested for antimicrobial activity against several bacteria and fungi by the broth microdilution method. The thiosemicarbazone and semicarbazone derivatives of lapachol exhibited antimicrobial activity against the bacteria Enterococcus faecalis and Staphylococcus aureus with minim...

Isatin (1H-indole-2,3-dione) and its derivatives are responsible for a broad spectrum of biological activities. Among these the cytotoxic and antineoplastic properties have been the most widely reported. The synthetic versatility of the isatin, due to its privileged scaffold, has led to the generation of a large number of structurally diverse derivatives which include analogues derived from eit...

An isocratic analytical method based on liquid chromatographic determination with UV detection is described for the determination of isatin in spiked plasma and in its synthetic mixture. The separation of the isatin was achieved on a betasil C-8 column using a mobile phase consisting of a binary mixture of acetonitrile and buffer (Na2CO3 + NaHCO3). The linearity, accuracy and precision were fou...

Isatin is an endogenous indole in mammalian tissues and fluids that is expected to have antitumor effects in human breast cancer cells. Human breast cancer cells (MCF-7) were exposed to isatin at various concentrations (0, 50, 100, 200 µmol/l) for 48 h. Apoptotic features were demonstrated by nuclei staining with Hoechst 33258 and flow cytometry. Bcl-2 and Bax mRNA were analyzed via reverse tra...

BINAM-prolinamides are very efficient catalyst for the synthesis of non-protected and N-benzyl isatin derivatives by using an aldol reaction between ketones and isatins under solvent-free conditions. The results in terms of diastereo- and enantioselectivities are good, up to 99% de and 97% ee, and higher to those previously reported in the literature under similar reaction conditions. A high va...

In screening for anonymous mycobacteria the use of thiosemicarbazone (10mug./ml.) may give rise to false positive results. Although these can usually be overcome by further tests, additional time and effort is required, which seriously limits the value of thiosemicarbazone as a true screening agent. Para-nitrobenzoic acid (500 mug./ml.) has proved more satisfactory in our hands; no false positi...

Isatin and its metabolites are constituents of many natural substances. They are also components of many synthetic compounds exhibiting a wide range of effects, including antiviral activity, antitumor and antiangiogenic activity, antibacterial, antitubercular, antifungal, antiaptotic, anticonvulsant and anxyolytic activities. Isatin itself is an endogenous oxidized indole with a wide spectrum o...

BACKGROUND & OBJECTIVES Derivatives of isatin are known to have cytotoxicity against human carcinoma cell lines. This compound therefore, has a potential to be used as a chemotherapeutic agent against cancer. This study was done to investigate the antioxidant and anticancer activities of isatin, extracted from flower of a folklore medicinal plant Couroupita guianensis against human promylocytic...

Five isatin anions were prepared by deprotonation of initial isatins in aprotic solvents using basic fluoride and acetate anions (F- and CH₃COO-). The F- basicity is sufficient to deprotonate isatin NH hydrogen from all the studied compounds. This process is reversible. In the presence of proton donor solvents, the anions form the corresponding isatins. The isatin hydrogen acidity depends on th...

We present herein the results of microwave promoted N-alkylations of isatin (1)with different alkyl, benzyl and functionalized alkyl halides. Reactions were carried out under different conditions, always employing methodologies compatible with MW assisted chemistry. Generation of isatin anion employing diverse bases and solvents or using the preformed isatin sodium salt was tested. The best res...