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The efficacy of Sparfloxacin (SPFX) for the control of bronchial asthma was evaluated in 26 patients with suspected Chlamydia pneumoniae infection. Patients were randomly allocated to receive SPFX 200 mg/day (n = 14) or control treatment (n = 12) for 21 days. Significant improvements in serum C-reactive protein levels, and significant decreases in peripheral eosinophil counts, serum eosinophil cationic protein (ECP) and sputum ECP were observed in the SPFX-treated group at day 21. SPFX-treated patients also had a significantly reduced frequency of asthma symptoms, reduced inhalant β2-stimulant use, and significant increases in morning peak expiratory flow. At the end of the study, C. pneumoniae was undetectable in two SPFX-treated patients who underwent polymerase chain reaction testing, but one control patient who was tested still had detectable levels of C. pneumoniae. These results suggest that SPFX could be used to control bronchial asthma in patients with suspected persistent C. pneumoniae infection.

Thiophene S-oxides 4 have been shown to undergo [4 + 2] cycloadditions with methylenecyclopropanes 2 with one or two electron acceptor substituents, i.e. even the tetrasubstituted 2-chloro-2-cyclopropylideneacetate 2c reacted well. However, for the tetrasubstituted alkene bi(cyclopropylidene) 2f high pressure had to be applied to make it react with 4. Only one diastereoisomer was formed in all the reactions. X-Ray crystal structure analyses of two of the cycloadducts, 3a and 3f, have been performed, their relative configuration determined as being endo,syn. The Wittig olefination of cyclopropanone hemiacetal to generate the methylenecyclopropanes and the subsequent cycloaddition can be carried out in a one-pot operation. This procedure is one of many potential one-pot or multi-component reactions involving stabilized phosphoranes. A further example of this type of reaction is shown in the novel desilylation–Wittig olefination of 1-ethoxy-1-trimethylsilyloxycyclopropane 5 to yield in one step cyclopropylideneacetates, e.g.2a.

The photochemical and electrochemical behavior of thiophene-S-oxides as a class was studied for the first time. It was shown that in both cases deoxygenation of the S-O functionality takes place. The outcome of the photoirradiation is very dependent on the substituent pattern of the starting material. Thiophene-S-oxides show different reduction behaviors in presence and absence of proton donors. In the absence of proton donors the reduction potential of the compounds is dependent on the substituents of the molecules. In the presence of proton donors, the substituents play a less significant role and a number of thiophene-S-oxides were reduced electrochemically to the corresponding thiophenes in presence of a 10-fold excess of benzoic acid. Copyright © 2000 John Wiley and Sons, Ltd.

Oligocycles with a 7-thiabicyclo[2.2.1]hept-5-ene unit have been prepared stereoselectively by cycloaddition of thiophene S-oxides to alkenes and subsequent deoxygenation of the sulfoxy bridge of the cycloadducts with PBr3.

Rigid, layered hetareno/hetareno- and hetareno/areno-cyclophanes with closely held, non-distorted, interacting π-systems can be synthesized easily by using various building blocks.

Rigid, layered hetareno/hetareno- and hetareno/areno-cyclophanes with closely held, non-distorted, interacting π-systems can be synthesized easily by using various building blocks.

A comparative study was conducted in elderly subjects with mild bronchial asthma to investigate the clinical usefulness of monotherapy with a leukotriene receptor antagonist in comparison to an inhaled corticosteroid. A total of 41 elderly patients aged 65 years or older with mild bronchial asthma, classified as being in severity step 1 and 2, were randomly assigned to the following two treatment groups: a pranlukast (CAS 103177-37-3, Onon) treatment group of 21 patients and an inhaled corticosteroid treatment group of 20 patients. Patients of the former group received pranlukast 450 mg daily and those of the latter group received fluticasone (CAS 90566-53-3) 200 microg daily for eight weeks. In the reference group, one patient was found to suffer from oral candidiasis 4 weeks after the start of the study. Therefore the evaluation was conducted on the remaining 19 participants. The evaluation parameters examined were obtained by keeping an asthma diary, determinations of PEF (peek expiratory flow), use frequency of beta2 stimulants, changes in symptom scores, and medication compliance. Further, measured before and after therapy were the ratio of peripheral blood eosinophils counts, serum ECP (eosinophils cationic protein), ECP levels induced sputum, and forced expiratory volume in one second (FEV1.0). As a result, in the time-course changes of symptoms scores and morning PEF, swift improvement was noted in the pranlukast group. Further, in the variables such as use frequency of beta2 stimulants, serum ECP levels, ECP levels induced sputum, and FEV1.0, an almost comparable level of improvement to the fluticasone group was demonstrated. From the above results, it was deemed that in elderly patients with mild bronchial asthma classified as steps 1 and 2, the pranlukast monotherapy, with superior medication compliance to inhaled therapy, would produce an equivalent level of clinical efficacy to the monotherapy with inhaled corticosteroid (fluticasone 200 microg daily).

Background: We investigated the possibility of preventing common cold-like symptoms as a previously unknown benefit of leukotriene receptor antagonists (LTRAs). Methods: A total of 279 adult patients with bronchial asthma referred to our hospital between June and December 2004 were retrospectively analyzed. Patients were divided into LTRA treated and untreated groups. Frequency of acute exacerbations and number of visits to emergency rooms and of hospital admissions were analyzed as indicators of frequency of infections and asthma exacerbation over the previous 12 months. Results: Irrespective of inhaled corticosteroid (ICS) use, frequency of infections was significantly lower in the LTRA treated group (0.3 ± 0.7 times/year) than in the LTRA untreated group (1.6 ± 4.2 times/year) (P < 0.05), suggesting that LTRA therapy prevents common cold-like symptoms. Frequency of acute exacerbations and number of hospital admissions were significantly lower in the LTRA treated versus LTRA untreated group (0.4 ± 0.8 versus 2.7 ± 4.3 times/year and 0.0 ± 0.2 versus 0.4 ± 0.7 times/year, respectively; both P < 0.01). When the patients were divided into ICS treated and untreated groups, none of the parameters analyzed differed significantly between the two groups, although all parameters tended to be lower in the ICS treated group. Conclusions: Adult asthma patients undergoing treatment with LTRAs exhibit lower incidence rates of common cold-like symptoms than those not receiving LTRAs. LTRAs play an important role in reducing the incidence of common cold-like symptoms among asthma patients and in suppressing exacerbation of asthma symptoms possibly associated with these symptoms.

In this randomized crossover study, 22 adult patients with moderate-to-severe persistent bronchial asthma were assigned to one of two groups. Patients in group 1 were administered fluticasone dry powder inhaler (DPI) for 8 weeks followed by a 2-week washout period, then hydrofluoroalkane-beclometasone dipropionate (HFA-BDP) for 8 weeks. After a further 2-week washout, they were again administered fluticasone DPI for 8 weeks. Patients in group 2 were assigned HFA-BDP followed by fluticasone PII and finally HFA-BDP over the same time periods. In both groups, no significant difference was observed in use of beta2-agonists and symptom score between the treatment periods; however, markers of pulmonary function were significantly higher when on HFA-BDP versus fluticasone DPI. Significant increases of morning peak expiratory flow (PEF) (p < 0.01), forced expiratory volume in 1 second (FEV1.0) (p < 0.01), V50 (p < 0.05), and V25 (p < 0.01) were observed at 18 weeks in group 1, whereas there were significant decreases of V50 (p < 0.05) at 18 weeks in group 2. No significant difference was noted in circulating eosinophil count and serum ECP between the 2 treatments; however, ECP in induced sputum and nitric oxide in expired gas were significantly lower (p < 0.05 and < 0.01, respectively) when on HFA-BDP versus fluticasone DPI. HFA-BDP might be delivered to small airways more effectively than fluticasone DPI.

Thiophene S-oxides have been prepared and their photoreactivity has been studied. In many cases, the sulfur moiety of the thiophene S-oxides is deoxygenated. Here, the corresponding thiophenes or hydroxylated thiophenes are isolated. In the case of the photoirradiation of tert-butyl substituted thiophene S-oxides, the oxygen of the sulfoxy unit is incorporated into the heterocyclic ring system and the corresponding furans have been isolated. Also, structures with two thiophene cores have been oxidized to the respective thiophene S-oxides. These molecules undergo photodeoxygenation, a reaction, which is catalysed by (non-oxidized) thiophenes.

Thiophenes have been treated with alkynes in the presence of m-chloroperoxybenzoic acid to give substituted arenes as cycloadducts. Alternatively, thiophene S-oxides have been prepared by oxidation from thiophenes and have been subjected to cycloaddition with alkynes in a subsequent step. The outcome of the reaction is dependent on the steric demand of the thiophene S-oxide. Some thiophene S-oxides can be reacted at temperatures as high as 140 °C without decomposition. Thiophenes as deoxygenated products are the main by-products. Reactions of thiophene S-oxides with allenes give in part thiabicyclo[2.2.1]heptene S-oxides of type 12a and 13 along with aromatized products. Thiophene S-oxides also cycloadd to benzyne.

Thiophene S-oxides 4 have been shown to undergo [4 + 2] cycloadditions with methylenecyclopropanes 2 with one or two electron acceptor substituents, i.e. even the tetrasubstituted 2-chloro-2-cyclopropylideneacetate 2c reacted well. However, for the tetrasubstituted alkene bi(cyclopropylidene) 2f high pressure had to be applied to make it react with 4. Only one diastereoisomer was formed in all the reactions. X-Ray crystal structure analyses of two of the cycloadducts, 3a and 3f, have been performed, their relative configuration determined as being endo,syn. The Wittig olefination of cyclopropanone hemiacetal to generate the methylenecyclopropanes and the subsequent cycloaddition can be carried out in a one-pot operation. This procedure is one of many potential one-pot or multi-component reactions involving stabilized phosphoranes. A further example of this type of reaction is shown in the novel desilylation–Wittig olefination of 1-ethoxy-1-trimethylsilyloxycyclopropane 5 to yield in one step cyclopropylideneacetates, e.g.2a.