Cefdinir: A comparative study of anhydrous vs. monohydrate form. Microstructure and tabletting behaviour.

Anhydrous cefdinir (AC) vs. monohydrated cefdinir (MHC) was compared in order to be used as antimicrobial in therapeutics. Different techniques have been used to characterize physically AC and MHC, and also a complete microstructural analysis of raw materials was carried out.

Cephem sulfones as inactivators of human leukocyte elastase. 5. 7 alpha-Methoxy- and 7 alpha-chloro-1,1-dioxocephem 4-ketones.

Studies on cephem sulfones as inhibitors of human leukocyte elastase (HLE) have been extended to the new class of cephem 4-ketones. tert-Butyl and phenyl ketones were prepared from 4-carboxycephem derivatives, at either the sulfide or sulfone oxidation level, by chemoselective Grignard reaction. Obtained products were functionalized with heterocyclothio and acyloxy substituents at C-3', C-2, or both positions.

Synthesis and antimicrobial spectrum of FCE 22101 and its orally available ester FCE 22891.

The most efficient routes for the synthesis of FCE 22101, a penem antibiotic characterized by a carbamoyloxymethyl sidechain at C-2 identical to that of cefuroxime and cefotaxime, and of FCE 22891, its orally absorbed pro-drug, are described. On the basis of in-vitro antimicrobial profile and other characteristics the compounds have been considered worthy of further development.