A new combinatorial method for synthesizing, screening, and discovering antifouling surface chemistries.

A set of diverse monomers were synthesized using combinatorial chemistry and tested using our unique high-throughput screening platform. The versatility of our platform is exemplified by possible applications in reducing biological fouling on ship hulls, filtration membranes, and surgical instruments, to name a few. To demonstrate its efficacy, the novel monomers were graft-polymerized onto light sensitive poly(ether sulfone) (PES) membranes via atmospheric-pressure plasma polymerization. A diverse library was synthesized by reacting a common vinyl ester linker with a library of maleimides containing various different functional groups. This allowed us to produce a library of many different surfaces and graft them all using the same linker chemistry. The modified surfaces were then tested and screened for the best antiprotein adsorption (nonfouling) properties. Membranes, functionalized with carboxylic acid, zwitterionic, and ester groups, had the lowest protein adhesion compared with that of an unmodified control PES membrane after a static fouling test. After dynamic fouling, these same functionalities as well as a hydroxyl group exhibited the highest permeability. These monomers performed better than our best previously synthesized amide monomers as well as our best poly(ethylene glycol) monomers, which are known to have very high protein resistance. Hansen solubility parameters qualitatively predicted which monomers performed best, indicating favorable interactions with water molecules.

A new class of antituberculosis agents.

Long-chain lipid envelopes are characteristic of mycobacteria such as those that cause tuberculosis and leprosy. Inhibition of fatty acid synthesis or elongation is a strategy demonstrated to be clinically effective against M. tuberculosis. A new class of compounds designed to inhibit the beta-ketoacyl synthase reaction of fatty acid synthesis has been developed. Of >30 compounds described, the most active were acetamides containing alkylsulfonyl substituents. Inhibitory activities were acutely sensitive to net charge, chain length, and degree of unsaturation. The most active compound 5 (alkyl = C(10)) contained a single methylene spacer between the sulfone and carboxamide and exhibited an MIC of 0.75-1.5 microg/mL, comparable to first-line antituberculosis drugs. These compounds are species-specific, exhibiting no significant activity against bacterial species other than M. tuberculosis and closely related strains. The synthesis, biological activity, and specificity of these compounds are described.

Método rápido para pesquisas de sulfonamídicos na urina

O autor propõe uma técnica rápida para a identificação de sulfonam¡dicos na urina. Trata-se da aplicação de nova reação corada descoberta por Fennell, usando-se o reagente de Ehrlich para urobilinogênio para impregnar papéis reativos. A reação é especifica para os sulfanam¡deos em geral e bastante sens¡vel para a pesquisa na urina. Descrevem-se pormenorizadamente o preparo do material, a técnica e as aplicações.

The action of diasone in the treatment of leprosy: preliminary report

The action of the oral administration of diasone has been studied in a group of advanced cases of leprosy of whom almost all had previously been treated with chaulmoogra oil. The drug was given for periods of 8 weeks with a daily dosage varying between 1 and 3 Grams according to individual tolerance; between each period or course of treatment there was a 4 weeks' interval. Anemia (82 per cent), asthenia and depression (88 per cent), headache (74 per cent) were noted as signs of intolerance. There were no grave consequences and intolerance was readily treated with liver extract, iron, and vitamin B complex. Activity of the drug was shown by softening, ulceration, and re-absorption of leprous nodules, healing of ulcers, and re-absorption of deep lepromatous infiltrations. Bacteriologically, granulation of the bacilli was observed but in no case had bacilli completely disappeared from the lesions. The improvement noted was greater the longer and more concentrated the treatment. The results found after 8 months trial were the following: in 5 cases treated for 3 periods, 100 per cent improved; in 11 cases treated for 2 periods, 63.6 per cent improved; in 26 cases after only 1 period of treatment, 50 per cent improved. Thus of 42 patients who had completed 1 to 3 periods of treatment, 59.5 per cent showed improvement. Finally it may be stated that diasone has proved to be effective in the treatment of leprosy in a series of 42 patients observed for 8 months. Further experimental treatment should be carried out so that definite conclusions based on greater experience can be obtained.