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Biomedical subjects

H Horn

Publications and source records attributed to H Horn.

At least 73 records · Page 4Linked to original sources
PubMed1983

[Synthetic serine protease inhibitors. 29. Synthesis of alpha-arylsulphonylamino-beta-(4-amidinophenyl)ethyl-chloromethylketones and their inhibitory activity against trypsin, plasmin and thrombin].

The synthesis of alpha-arylsulphonylamino-beta-(4-amidinophenyl)ethyl-chloromethylketones, the structures of which correspond largely to those of the antiproteolytically very potent N alpha-arylsulphonylated 4-amidinophenylalaninamides, was realized starting from 4-cyanophenylalanine hydrochloride. After N alpha-arylsulphonylation this compound was converted via the acid chlorides by treatment with diazomethane into alpha-arylsulphonylamino-beta-(4-cyanophenyl)ethyl-diazomethylketones from which the corresponding chloromethylketones were afforded by treatment with concentrated hydrochloric acid. The conversion of the cyano function into the amidine function via the thiocarbamoyl and the thioimidic acid esters yielded the compounds named in the title. The substances produced no irreversible inhibition of the serine proteinases trypsin, plasmin and thrombin. Their competitive inhibitory effect was almost as potent as that of N alpha-arylsulphonylated 4-amidinophenylalanine ethylesters.

Amidines↗
PubMed1981

[Clinidine-induced bradycardia: studies of the effect on the human sinus node (author's transl)].

Heart rate, atrioventricular conduction, sinus-node recovery time and effectiveness of carotid-sinus massage on heart rate were measured before and every five minutes after intravenous injection of 0.15 mg clonidine (Catapresan) in 11 patients (averaged age 60 years) with symptomatic bradycardia (dizzy spells, syncope, palpitations). Th results indicated the following significant (P less than 0.05) mean maximal effects: heart rate fell by 12% (from 59 to 52/min), capacity of atrioventricular conduction by 9% (from 132 to 121/min), while maximal sinus-node recovery time ("over-drive suppression") doubled (from 1704 to 3562 ms), heart rates of 120, 150 and 200/min being used for diagnostic atrial overdrive stimulation at each five-minute period after clonidine. During clonidine administration three patients developed a so-called hypersensitive carotid sinus reflex, in two patients the effectiveness of carotid sinus massage decreased, in three if increased, while in three it remained normal. It is concluded that (1) during bradycardia, initiated or increased by sympatholytic drugs, tests should be undertaken to exclude latent sinus-node syndrome and (or) hypertensive carotid-sinus reflex; (2) clonidine should not be used in patients with signs of sinus-node dysfunction.

Aged↗
PubMed1981

[Synthetic inhibitors of serine proteinases. Part 25: Inhibition of trypsin, plasmin and thrombin by amides of N alpha-substituted amidinophenylalanines and 3-amidinophenyl-3-aminopropionic acids (author's transl)].

Amides of N alpha-substituted 3-amidinophenylalanine are potent inhibitors of the serine proteinases trypsin, plasmin and thrombin. They belong to the most potent inhibitors of these enzymes of the benzamidine type. In contrast, amides of 4-amidinophenylalanine possess weak inhibitory activity towards trypsin and plasmin. The cyclic amides of this group, however, are potent thrombin inhibitors. These derivatives are the first benzamidines with specific antithrombin activity. The isomeric compounds of 3-amidinophenyl-3-aminopropionic acids possess weak inhibitory effects on trypsin, plasmin and thrombin.

Amidines↗