Synthesis, antimicrobial testing and QSAR study of new 2-phenylethenylbenzothiazolium salts substituted by cyclic amines.

A series of new 2-phenylethenylbenzothiazolium salts substituted by cyclic amines has been prepared by the condensation of 2-methyl benzothiazolium bromide with substituted benzaldehydes. The nucleophilic substitution of 4-fluorobenzaldehyde with appropriate cyclic amines has been used to obtain the starting benzaldehydes. The compounds with saturated cycloamino substituents have shown enhanced activity against Euglena and some derivatives with piperazine substituent were active against Gram positive bacteria.

Synthesis and antimicrobial activity of new 2-phenylethynylbenzothiazoles and related salts.

New 2-phenylethynylbenzothiazoles were synthesized by coupling reaction between 2-iodobenzothiazole and substituted phenylacetylenes under palladium catalysis. The modified Wittig reaction was used to prepare the substituted phenylacetylenes from corresponding benzaldehydes. 2-Phenylethynylbenzothiazoles were next quarternized with trimethyloxonium tetrafluoroborate to 3-methylbenzothiazolium salts. Antimicrobial in vitro activities were determined for all new compounds.

Evidence for the involvement of a 66 kDa membrane protein in the synthesis of sterolglucoside in Saccharomyces cerevisiae.

The membrane-bound sterolglucoside synthase from the yeast Saccharomyces cerevisiae has been solubilized by nonionic detergent, Nonidet P-40, Triton X-100, and partially purified by DEAE-cellulose column chromatography and ammonium sulfate fractionation. SDS/PAGE of the purified fraction revealed the presence of two protein bands of molecular mass 66 kDa and 54 kDa. In an attempt to identify further the polypeptide chain of sterolglucoside synthase, the partially purified enzyme was treated with [di-125I]-5-[3-(p-azidosalicylamide)]allyl-UDPglucose, a photoactive analogue of UDP glucose, which is a substrate for this enzyme. Upon photolysis the 125I-labeled probe was shown to link covalently to the 66 kDa protein. The photoinsertion was competed out by the presence of unlabeled UDPglucose thus suggesting that this protein contains substrate binding site for UDPglucose. Since photoinsertion of the probe to protein of 66 kDa correlates with the molecular mass of the protein visualized upon enzyme purification we postulate that the 66 kDa protein is involved in sterolglucoside synthesis in yeast.

[Rapid prenatal diagnosis of cystic fibrosis using the polymerase chain reaction: results of the first 5 cases]. / Rýchla prenatálna diagnostika cystickej fibrózy metódou polymerázovej ret'azovej reakcie (PCR): výsledky prvých piatich vysetrení.

Cystic fibrosis (CF) is an autosomal recessive lethal disease with an incidence in Slovakia of 1 affected in 1800 newborns. Within a year the incidence amounts to about 50 cases. Though the responsible gene has already been cloned, the only effective approach to prevention is prenatal diagnosis in the first and second trimester of pregnancy. The paper presents the results of the first five cases of prenatal diagnosis of CF established by the new rapid method of DNA analysis, polymerase chain reaction (PCR). Delta F508 deletion mutation and closely linked DNA polymorphism KM19/PstI were assessed. In two of the five cases studied the fetuses were found to be affected and pregnancy termination was indicated. To exclude the possibility of fetal DNA contamination with maternal DNA, the hypervariable DNA polymorphism VNTR apoB was determined simultaneously. The advantages of this approach are demonstrated on cases of prenatal diagnosis performed in two families where contamination of fetal DNA could be excluded. The value of the PCR method is being compared with that of Southern's hybridization method. (Tab. 2, Fig. 4, Ref. 27.).