Arthrichitin. A New Cell Wall Active Metabolite from Arthrinium phaeospermum.

Arthrichitin (1), C(33)H(46)N(4)O(9), is a new cell wall active depsipeptide isolated from the fermentation broth of Arthrinium phaeospermum (HIL Y-903022). Its structure was elucidated on the basis of spectroscopic and chemical degradation studies. Arthrichitin consists of serine, beta-keto tryptophan, glutamic acid, and 2,4-dimethyl-3-hydroxydodecanoic acid units.

Interference in clinical laboratory tests, with special regard to the bilirubin assay: effects of a metabolite of the new prolyl 4-hydroxylase inhibitor, Lufironil.

During the toxicological examination of the fibrosuppressive agent, Lufironil (INN), in rats a dose-dependent positive reaction for urinary bilirubin was observed. This positive reaction was found in quantitative assays, and when using test strips. The positive reaction for bilirubin in these assay systems was caused by a metabolite of Lufironil.

Mersacidin, a new antibiotic from Bacillus. Fermentation, isolation, purification and chemical characterization.

Mersacidin (1) is a new peptide antibiotic containing beta-methyllanthionine. It is classified as a member of the proposed lantibiotic group of antibiotics, and is produced by a species of Bacillus. Mersacidin has a molecular weight of 1,824 (C80H120N20O21S4).

Deoxymulundocandin--a new echinocandin type antifungal antibiotic.

A new echinocandin type antifungal antibiotic, deoxymulundocandin, C48H77N7O15, was isolated from the culture filtrate and mycelia of a fungal culture, Aspergillus sydowii (Bainier and Sartory) Thom and Church var. nov. mulundensis Roy (Culture No.

Aranorosin, a novel antibiotic from Pseudoarachniotus roseus. II. Structure elucidation.

Aranorosin, a new antifungal antibiotic, has been isolated from the culture filtrate and mycelium of a strain of Pseudoarachniotus roseus Kuehn. The antibiotic, C23H33NO6, contains a novel 1-oxaspiro[4,5]decane ring system. The structure (I) has been elucidated on the basis of spectroscopic and chemical analysis.

Synthesis and structure-activity relationships in the cefpirome series. I. 7-[2-(2-Aminothiazol-4-yl)-2-(Z)-oxyiminoacetamido]-3-[(su bstituted-1-pyridinio)methyl]ceph-3-em-4-carboxylate s.

7-[2-(2-Aminothiazol-4-yl)-2-(Z)-oxyiminoacetamido]-3-[(s ubs tituted-1-pyridinio)methyl]ceph-3-em-4-carboxylates II are a group of beta-lactam antibiotics with extraordinary high antibacterial activity. The promising member of this group, cefpirome (HR 810, II-1) is a candidate for clinical use. Synthetic pathways to II starting from cefotaxime derivatives I or 7-aminocephalosporanic acid (7-ACA) are described.

Isolation, identification and in vitro synthesis of conjugates of penbutolol and its metabolites.

The metabolites of 1-tert.-butylamino-3-(2-cyclopentylphenoxy)propan-2-ol (penbutolol Betapressin) penbutolol 2-glucuronide, 4'-OH-penbutolol 2-glucuronide, 4'-OH-penbutolol 4'-sulfate and 1''-dehydropenbutolol 2-glucuronide were isolated from the urine of patients, purified by high-performance liquid chromatography and characterised by 1H-NMR and mass spectroscopy. Penbutolol 2-glucuronide and 4'-OH-penbutolol 4'-glucuronide were synthesised in vitro from penbutolol and 4'-OH-penbutolol, respectively, using glucuronyltransferase.

[Synthesis of the highly cardioselective beta-sympatholytic pacrinolol].

The synthesis is described of the enantiomerically pure (-)-3-(3,4-dimethoxyphenylethylamino)-2-hydroxypropoxy] phenyl]-cis-crotonic acid nitrile (13b) (free base) and its hydrochloride (13c) (pacrinolol, Hoe 224 A) starting from p-hydroxyacetophenone (1) and racemic epichlorohydrin (2). The p-(2,3-oxidopropoxy)acetophenone (2) resulting from this reaction is C-homologisized to (8); reactions of this with homoveratrylamine (9) leads to (10a), the racemic structural analog of (13b). Resolution of the racemate is achieved by fractional crystallisation of the diastereoisomeric mandelates (13a) and (14a) to afford the enantiomerically pure title compound (13c) and its dextrarotatory optical antipode (14c).

Swalpamycin, a new macrolide antibiotic. II. Structure elucidation.

A new antibiotic swalpamycin (1) has been isolated from the culture broth of Streptomyces sp. Y-84,30967. The antibiotic has the molecular formula of C37H56O14 and belongs to the class of 16-membered neutral macrolide antibiotics.

Mulundocandin, a new lipopeptide antibiotic. II. Structure elucidation.

The structure of a new antifungal antibiotic, mulundocandin, C48H77N7O16, was elucidated by high field NMR experiments e.g., homo- and heteronuclear correlation spectra, distortionless enhancement by polarization transfer (DEPT) spectra as well as nuclear Overhauser effect.

[Pharmacokinetics and biotransformation following topical use of the local corticoid prednicarbate].

Studies on absorption and distribution in both skin and organism, as well as on elimination and biotransformation were performed in rats, pigs, and rabbits following topical application of the corticoid prednisolone-17-ethyl carbonate-21-propionate (prednicarbate; test name: Hoe 777), which had been labeled with 14C in position 4 for this purpose. After allowing the 0.25% greasy ointment to take effect for 6 hours, about half of the dose applied to rats and three quarters of that applied to pigs could be removed from the application area (rejection rate).

[Synthesis of prednicarbate, an non-halogenated topical anti-inflammatory derivative of prednisolone-17-ethylcarbonate esters].

The synthesis of prednisolone-17-ethylcarbonate-21-propionate (5) (prednicarbate, Hoe 777) passing the intermediate products prednisolone-17,12-diethylorthocarbonate (2) and prednisolone-17-ethylcarbonate (3) as well as some physicochemical properties and spectroscopic data of (5), especially the 1H-NMR- and MS-spectrum, are reported. Prednicarbate has an optimal split of topical/systemic antiinflammatory activity.

Stereochemistry of the epoxydon group antibiotic G7063-2 isolated from a Streptomyces species HPL Y-25711.

The absolute configuration of the ring system of the antibiotic G7063-2 has been established as being the same as that reported for terreic acid, based on circular dichroism data. During structure elucidation experiments, reaction with ethereal diazomethane gave an adduct whose structure is proposed.