[Acute renal insufficiency in a patient with intra- and extracapillary Henoch's nephritis]. / Ostra bubrechna nedostatuchnost pri bolen s intra- i ekstrakapiliaren Khenoxh-nefrit.

Case is described with acute renal failure in Henoch's nephritis with intra- and extracapillary cellular proliferation. The disease was manifested with its classical picture: characteristic purpura, articular pains in the wrist and ankle joints, mucous-bloody diarrhea. The renal changes originated at the very beginning of the hemorrhagic vasculitis and clinically was manifested with acute renal failure and severe nephrotic syndrome. Under the effect of hemodialysis and complex drug treatment with cytostatics, glucocorticoids, anticoagulants, plasma- and bloodtransfusions, a very good clinical and paraclinical effect was attained. No recurrences of the main disease were recorded during the six-year clinical observation. A stability of the renal function was observed in the patient, with the exception of the persiting proteinuria with values under 10 g/l.

Antiviral activity of tetrahydro-2(1H)-pyrimidinones and related compounds.

24 derivatives of tetrahydro-2(1H)-pyrimidinone and related compounds were tested in vitro for antiviral activity against representatives of six viral taxonomic groups. The screening was carried out by a two-stage procedure including the agar-diffusion plaque-inhibition test and the one-step growth cycle setup. A distinct activity of three mono- and bis-morpholinomethyl derivatives of tetrahydro-2(1H)-pyrimidinone (THP), 1,3-bis(piperidinomethyl)-THP, the 1-morpholinomethyl derivative of tetrahydro-2(1H)-pyrimidinethione (THPT) and the related N,N'-bis(morpholinomethyl)-urea against the fowl plague virus was established. In the one-step growth cycle setup these compounds inhibited 87.5-99.6% of the infectious virus yield. Two of the compounds, namely 1-morpholinomethyl derivatives of THP and THPT manifested a strong inhibitory effect on the reproduction of Semliki Forest virus as well, exceeding 99.9% in the one-step growth cycle test. A borderline effect was observed in some derivatives against vaccinia virus and Newcastle disease virus. The structure-activity relationship of this group of compounds is discussed.

Benzoxazolone-5-sulphonanilides, 1-(benzoxazolone-5'-sulphonyl)-benzotriazoles and 4-hydroxy-3,2'-diaminobenzenesulphonanilides with antiviral activity.

benzoxazolone-5-(2'-nitro)-sulphonanilides were synthesized by acylation of o-nitroanilines with benzoxazolone-5-sulphochloride or 3-methylbenzoxazolone-5-sulphochloride. The nitro group in these compounds was subjected to reduction and the resulting amino derivatives were cyclysed to yield the corresponding 1-(benzoxazolone-5'-sulphonyl)-benzotriazoles. Decyclization of the oxazolone cycle of benzoxazolone-5-(2'-amino)-sulphonanilides resulted in 4-hydroxy-3,2'-diaminobenzenesulphonanilides. In vitro testing of the antiviral activity of the compounds obtained during successive synthetic steps revealed that some of them exhibited marked antiviral effect against toga, orthomixo, oncorna and herpes viruses.

Antiviral, antibacterial and antitumor activity of the hydrazide and the ethyl ester of 2,2'-anhydro-1-(beta-D-arabinofuranosyl)-orotic acid.

It has been demonstrated that the hydrazide and the ethyl ester of 2,2'-anhydro-1-(beta-D-arabinofuranosyl) orotic acid inhibit selectively the multiplication of some DNA-containing viruses (PsRV, VV, AdV5), suppress the growth of E. coli and St. aureus in vitro and exhibit an antitumor effect with Lewis lung carcinoma and sarcoma 298.

Antirival activity of N-phenyl-N'-arylthiourea derivatives against some Rhinoviruses.

The effect of 12 derivatives of N-phenyl-N'-aryl- or alkylthiourea, inhibitors of human enteroviruses and foot-and-mouth disease virus, on reproduction of some rhinoviruses (H-17, B-632) in HeLa Bristol cells was studied. As screening methods both the multicylce growth test in roller tube cultures and two variants of plaque inhibition tests were employed. The compounds selected were tested in one-step growth cycle set-up. We established that N-phenyl-N'-4-hydroxyphenylthiourea (V-24) and N-phenyl-N'-2-carboxyphenylthiourea (V-17) have a distinct inhibitory effect on the growth of rhinovirus H-17, and N-phenyl-N'-2-hydroxy-5-nitrophenylthiourea (V-25) inhibited strongly the multiplication of rhinovirus B-632.

Antiviral activity of N-phenyl-N'-aryl- or alkylthiourea derivatives in Coxsackie virus infections in mice.

The effect of five derivatives of N-phenyl-N'-aryl- or alkylthiourea-inhibitors of the multiplication of Coxsackie virus B1 and other picornaviruses in vitro-was tested in experimental infections with Coxsackie viruses B1, B3, A6, and A7 in newborn mice. Under the action of N-phenyl-N'-3-hydroxyphenylthiourea (no. 23) and N-phenyl-N'-4-carboxy-5-hydroxyphenylthiourea (no. 20) a two- to threefold reduction in mortality was observed, as well as an appreciable delay in the course of the disease (mean effective dose, lengthening by 2 to 6 days) after infection with Coxsackie viruses B1, B3, and A7. The infection with Coxsackie virus A6 was affected only by compound no. 23 and, at that, to a low degree. If the antiviral effect is to be obtained, the compounds must be applied daily (once subcutaneously) from the 24th to the 144th h after virus inoculation, a period which corresponds to the incubation period and the beginning of the manifested infection. On the basis of these data, as well as of the relatively high selectivity (therapeutic index of 3 to 20), the two indicated substances may be considered to be reliable antiviral chemotherapeutic agents.