Synthesis and cytostatic properties of monoterpene derivatives of cyanuric and isocyanuric acids.

Symmetric, trisubstituted derivatives of cyanuric and isocyanuric acid 3a-e and 4a-e, respectively have been prepared by treatment of cyanuric chloride 1 with appropriate terpenic alcohols 2a-e. Under less basic conditions involving treatment of appropriate alcohols 2a-e with metallic sodium, less polar cyanuric acid derivatives 3a-e were obtained in 74-85 yield. Under more basic conditions, in the presence of sodium hydride, isocyanuric acid derivatives 4a-e were prepared in 71-88 yield. Cytostatic activity of (IR,2S,5R)-menthol derivative (3a) has been evaluated on 9 cancer subtypes including 62 tumor cell lines. The studies have shown that contrary to expectations, 2,4,6-trimentoloxy-1,3,5-triazine revealed a weak or moderate activity against most of the cell lines.

Track counting and the blots.

Track detectors are very useful devices for alpha particle dosimetry. Alpha particle tracks are registered on the detector's surface. The registered track density is proportional to the dose. When the dose is low the greatest effect on the total error of dose assessment has a Poisson distribution (random error). When the dose is high, the greatest contribution to the total error is the effect of track overlapping (systemic error). This paper describes how to solve the problem of overlapping tracks when a computer aided image analyser is used. The formulae presented in this paper were proven in the international calibration programme run by NRPB and EU.

A novel generation of coupling reagents. Enantiodifferentiating coupling reagents prepared in situ from 2-chloro-4,6-dimethoxy-1,3,5-triazine (CDMT) and chiral tertiary amines.

Coupling of racemic N-protected amino acids with amino components by means of 2-chloro-4,6-dimethoxy-1,3,5-triazine (CDMT) in the presence of chiral tertiary amines such as strychnine, brucine, and sparteine proceeds enantioselectively, affording appropriate amides or dipeptides in 69-85% yield. The configuration of the preferred enantiomer and enantiomeric enrichment depend on the structures of the amine and carboxylic acid. Calculated Kagan enantioselectivity parameters (s) are in the range 1.6-195. Chiral triazinylammonium chlorides formed in situ from CDMT and chiral tertiary amines are postulated as reactive intermediates involved in the process of enantioselective activation of N-protected amino acids.

Various opportunistic infections and neoplasms in patients dying of AIDS in the last 12 years--report based on pathomorphological investigations.

BACKGROUND: The aim of the study was microscopic diagnostics of infections and neoplasms in patients who died of AIDS. MATERIAL AND METHODS: Post-mortem analyses were performed in the Hospital for Infectious Diseases in Warsaw. In total, 200 patients with AIDS who were treated and subsequently died were included in the analysis. The study group consisted of 175 men and 25 women. Patients' age ranged between 11 months and 64 years (mean age 43 years). RESULTS: The most frequent infection diagnosed in these subjects was cytomegalovirus, followed by bacterial, mycotic, tuberculotic infections and toxoplasmosis. As far as neoplasms are concerned, patients with AIDS suffered most frequently from malignant lymphoma, Kaposi's sarcoma and finally, from Hodgkin's disease. In most cases, many types of infections coexisted with one another or there was a co-occurrence of the infection and neoplasm. CONCLUSIONS: The author suggests that the material presented in this paper is representative for Polish population. Pulmonary changes is the most often cause of the death of the patients with AIDS.

Synthesis and application of chiral triazine condensing reagents prepared from esters of amino acids.

Treatment of cyanuric chloride with chiral amines or esters of chiral amino acids gave chiral 2,4-dichloro-6-alkylamino-1,3,5-triazines (2-5) in 49-69% yield, which were found useful as coupling reagents. Enantioselective activation and enantioselective aminolysis in the presence of 2-5 was observed.

Novel side reactions accompanying activation and aminolysis of N-benzoyl-2-alkylserines.

2-Phenyl-4-alkyl-4-hydroxymethyl-1,3-oxazolones (2a-d) have been identified as side products accompanying activation of N-benzoyl-2-alkylserines (1a-d). Oxazolones 2a-d in the presence of amine rearrange subsequently to corresponding 4-alkyl-2-phenyl-4,5-dihydro-1,3-oxazole-5 carboxylic acids (4a-d) at a 20-68% yield.

Film badges for personal dosimetry of roentgen radiation.

The paper describes the calibration procedure for and data obtained from routine X-ray dosimetry service in Poland. In 1998 the number of readouts amounted to 152,000. The dosimetry concerned 31,281 workers in 3,113 enterprises. The annual collective dose was assessed to be 16.7 man.Sv. The analysis of the calibration quality is discussed as well. Only 2.9% of all points lay outside the quality curve while the number of the acceptable outliers was 5%.

Triazine-based condensing reagents.

The synthesis, properties, and application of condensing reagents derived from 1,3,5-triazines are described. The mechanism of activation of carboxylic function, structure of reactive intermediates, and mechanism of acylation of nucleophiles are presented. The synthetic versatility of mono- and bifunctional reagents for syntheses in solution, triazine-based immobilized reagents, chiral triazines for enantiodifferentiating syntheses, are discussed. The scope and limitation of the synthetic utility of triazine reagents in the preparation of heterocyclic compounds, amides, esters, oligopeptides-including large-scale syntheses and use in the combinatorial chemistry-is demonstrated.

[Cooperation between pharmacists of Gdansk and Wielkopolska region in the XX century]. / Wspólpraca farmaceutów gdanskich i wielkopolskich w XX wieku.

The University of Poznan, with its Pharmaceutical Department was established after the First World War. Many of the pharmacists educated in Poznan were employed in the Pomorze Gdanskie region. This article describes the activities of these pharmacists in the years 1920-1939 and during the Second World War. The article also discusses the assistance of the University of Poznan in the organization of the Pharmaceutical Faculty of the Medical University of Gdansk and of pharmacy in the Pomorze Gdanskie region. Those pharmacists who came back to Poznan after years spent at the Baltic seaside and those who studied in Gdansk and were then employed in Poznan are also mentioned in the article.

Synthesis and immunomodulatory activity of novel analogues of human beta-casein fragment [54-59].

Three novel analogues of human beta-casein fragment [54-59] have been synthesized and tested for their immunomodulatory activity. Interestingly, human beta-casein fragment [54-59] has been found to be increased nitric oxide release from neutrophils. The obtained analogues have shown less immunomodulatory activity than native hexapeptide.

The library of p-nitrophenyl esters of oligopeptides as a model to study the anticancer drug-peptide conjugates activated during tumor angiogenesis.

An indexed library of oligopeptide p-nitrophenyl esters immobilized via methoxy-1,3,5-triazine scaffold on the cellulose support, was synthesized by the step by step procedure and by segment coupling, involving 2-chloro-4,6-dimethoxy-1,3,5-triazine as a condensing reagent. The substrate specificity towards homogenate supernatant of mouse lung cancer LL2 cells has been studied.

The library of p-nitrophenyl esters of oligopeptides as a model to study the anticancer drug-peptide conjugates activated during tumor angiogenesis.

An indexed library of oligopeptide p-nitrophenyl esters immobilized via methoxy-1,3,5-triazine scaffold on the cellulose support, was synthesized by the step by step procedure and by segment coupling, involving 2-chloro-4,6-dimethoxy-1,3,5-triazine as a condensing reagent. The substrate specificity towards homogenate supernatant of mouse lung cancer LL2 cells has been studied.

Radium and radon in natural underground water supply in the region of Lódz, Poland.

The region of Lódz, located in the central part of Poland, is very specific with respect to water supply coverage. In this densly populated and extensively industrialised region there is a lack of natural reservoirs of surface water in the nearest vicinity of Lódz. Therefore, over 50% of water for public and domestic use is provided from underground water intakes. It is well known from the literature that in underground water may occur radionuclides in the uranium and thorium decay series. Underground water intakes in Lódz used for public water supplies have been surveyed for the presence of radium-226 and radon-222 since the earlier studies of quality standards of the gross alpha and gross beta activity pointed to their possible excessive values. The surveillance was based on the guidelines set by the World Health Organisation (WHO). The measurements of radium-226 activity showed its different concentrations depending on the age of the water-bearing level. These concentrations fell within the range of < 10 divided by 50 Bqm-3. Measurements of radon yielded similar results and its highest concentrations were found in the Lower cretaceous and Jurassic formations. Radon concentrations ranged from 200 to 11,400 Bqm-3. A maximum annual dose taken into the body in the population drinking this water may account for 0.85 microSv which is lower than the limit recommended by WHO.

[Pneumocystis carinii infections in patients with neoplasms and AIDS--clinical-pathologic changes in the lungs]. / Zakazenia pneumocystis carinii u chorych na nowotwory i AIDS--obraz kliniczno-patologiczny zmian w plucach.

Pneumocystis carinii (PC) has been documented as a cause of pneumonia in a broad range of immunocompromised patients. The presentation of disease will very based on the underlying predisposing condition but a confirmation depends upon the identification of organisms in a bronchial aspiration or lung biopsy specimen. This retrospective study based on autopsies of 15 patients (pts) with AIDS and 12 non AIDS pts with neoplastic diseases. Pneumocystis carinii pneumonia (PCP) was confirmed by histologic examination. The clinico-pathological analysis emphasizes a spectrum of morphologic variation of the disease in relation to the clinical course of a principal disease. A distinction was made between the microscopical diagnosis of PC infection in AIDS and non AIDS pts; the burden of organisms in infected AIDS pts appeared greater than that of neoplastic diseases (mostly with small cell lung carcinoma). Nonspecific features of diffuse alveolar damage associated with PC organisms were identified in 67% of non AIDS pts and 13% of AIDS pts. Various degree of interstitial fibrosis was more prominent in AIDS pts (67%) than in non AIDS pts. The high frequency of atypical changes in lung might be the result of various chemotherapeutic agents used in managing these pts or repeated pulmonary infections.

[Mycology perirenal abscess as a complication of choledochoduodenal anastomosis due to stenosing papillitis]. / Ropien okolonerkowy pochodzenia grzybiczego w przebiegu pooperacyjnym u chorego po zespoleniu przewodowo-dwunastniczym z powodu papillitis stenosans.

This elaboration presents the seldom case of perirenal abscess insued after choledochoduodenoanastomosis. It refers to 71 years old patient, who was treated in General Hospital Biala Podlaska, Department of Surgery, with good results. Aetiology of that abscess is very seldom too, because it is concerned with Candida sp.

[Mediastinal abscesses and empyema of the pleural cavity after iatrogenic fracture of the sternum]. / Ropien sródpiersia i ropniaki oplucnej w wyniku jatrogennego zlamania mostka.

A case report presents fracture of sternum during the resuscitation and in continuity iatrogenic hematoma and afterwards abscessus of mediastinum, and empyema the both of pleura cavities. Fracture of thorax wall is rather often event, but in the most, it has not adverse effects. This case refers to 68 years old patient, who had one of the most serious complications: abscessus of mediastinum, empyema of left and right pleura cavities with perforation outside the anterior wall of thorax. He was treated in General Hospital Biala Podlaska, Department of Surgery with good results and was extracted home as well-being patient after 35 days spent in hospital the second hospitalisation.

AIDS pathology: infections and neoplasms in 55 fatal AIDS cases. A postmortem study.

The study evaluated the incidence of infections and neoplasms in 55 out of 104 patients with AIDS who died in Poland from January 1986 to April 1994 (the estimated autopsy rate-52.8%). Histopathological examination revealed 103 infections and 11 neoplasms. In 40 persons (73%) either multiple infections or a neoplasm and an infection were diagnosed. Cytomegalovirus infection was most common. (65.5% of cases) followed by Pneumocystis carinii (24% of cases). These infections were the leading cause of death in 20% and 16% of cases, respectively. The results of this study showed a significantly lower incidence of Pneumocystis carinii, Kaposi's sarcoma and non-Hodgkin's lymphoma in comparison with the results of similar studies in countries with a large number of AIDS cases.

Treatment of vancomycin-resistant Enterococcus faecium infections with an investigational streptogramin antibiotic (quinupristin/dalfopristin): a report of fifteen cases.

New therapies for vancomycin-resistant Enterococcus faecium (VREF) infections are urgently needed. We describe the treatment of 15 patients with VREF infection with quinupristin/dalfopristin (RP 59500), a new injectable streptogramin antibiotic. Primary infections treated were bacteremia (4), urinary tract (4), intraabdominal (5), otitis externa (1), and meningitis (1). Minimum inhibitory concentrations for quinupristin/dalfopristin ranged from 0.5 microgram/ml or less to 2 micrograms/ml, and minimum bactericidal concentrations were greater than 64 micrograms/ml for all VREF isolates tested. Peak serum inhibitory titers following infusion of quinupristin/dalfopristin ranged from 1:8 to 1:64; all bactericidal titers were less than 1:2. Development of resistance to quinupristin/dalfopristin during therapy was not observed. The only drug-related adverse effect noted was phlebitis in 4 patients; all had received quinupristin/dalfopristin by peripheral venous infusion. Three patients had clinical and bacteriologic cures. Relapses occurred in 5 patients with recovery of VREF from infected sites in post-treatment cultures. Ten patients died of severe underlying disease; VREF was believed to contribute directly to the death of only 1 patient. While evaluation of clinical efficacy was complicated by the severity of underlying disease in patients with VREF infection, our experience suggests that quinupristin/dalfopristin is a safe and potentially useful agent for the treatment of VREF infections.