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Biomedical subjects

H Yellin

Publications and source records attributed to H Yellin.

At least 19 recordsLinked to original sources
PubMed1986

Synthesis, saludiuretic, and antihypertensive activity of 6,7-disubstituted 1(2H)- and 3,4-dihydro-1(2H)-phthalazinones.

The synthesis of the isomeric series 6-chloro-7-sulfamoyl- and 7-chloro-6-sulfamoyl-1(2H)-phthalazinones (1 and 2) and 6-chloro-7-sulfamoyl- and 7-chloro-6-sulfamoyl-3,4-dihydo-1(2H)-phthalazinones (3 and 4), combining structural features characteristic to furosemide and hydralazine, is described, the mechanism of the formation of 1 and 2 is discussed, and their structure-activities relationships are studied. Preliminary screening in the rat shows that series 1 and 3 exhibit diuretic and saluretic activity similar to that of chlorothiazide with, however, Na+/K+ ratios more favorable than chlorothiazide and furosemide. The compounds of series 2 and 4 are practically inactive. All four series show initial antihypertensive activity lower than that of hydralazine. However, compounds 1a, 1c, and 4a show a higher activity at 8 and/or 24 h after administration and thus may offer a unique combination of a "loop" diuresis with direct long-acting peripheral vasodilating effects.

Animals↗
PubMed1983

Structure activity correlation for diuretic furosemide congeners.

The structure activity correlation of several groups of anthranilic acid derivatives was studied. 59 compounds, most of them possessing the anthranilic acid moiety, were synthesized and tested for diuretic and saluretic activities. Equations correlating the biological activities of these compounds with their physicochemical constants suggest positive dependence of the diuretic activity on log P (octanol:water partition coefficient). It is concluded that, within limits, the variation in biological activity is primarily governed by the lipophilicity of the molecule, and further increase in log P value will not enhance this activity.

Animals↗
PubMed1979

Structure-activity relationship in a new series of atropine analogues. 1. N,N'-Disubstituted 6,7-diazabicyclo[3.2.2]nonane derivatives.

The synthesis of a new series of N,N'-disubstituted 6,7-diazabicyclo[3.2.2]nonane derivatives is described. The antimuscarinic potency of these drugs was evaluated in the guinea pig ileum and compared to that of atropine sulfate. All the drugs tested competitively inhibited the acetylcholine-induced contractions. Kd values were calculated and, in several cases, compared to those obtained by direct binding to the muscarinic receptor from mouse brain. The order of potencies followed that which is known for various tropine and pseudotropine esters; that is, the 3alpha configuration is more potent than the 3beta configuration, and the quaternary analogues are more potent than the tertiary ones. The antimuscarinic activity of the drugs is dicussed in terms of their acetylcholine-like molecular arrangement that gives rise to a characteristic interaction pharmacophore.

Animals↗
PubMed1975

Limitations to the neuroregulation of enzymes in mammalian skeletal muscle.

Muscle fibers of the sternomastoid and the tongue of the rat were characterized histochemically according to mitochondrial distribution (succinic dehydrogenase), as well as reactivity for the alkali- and acid-stabile "myofibrillar" adenosine triphosphatases. The principal fiber types of the sternomastoid was the large, "white" AalphabetaM fibers and the smaller, "intermediate" BbetaD and "red CalphaL fibers (figs. 1, 2, 3). The unusual musculature of the tongue was populated by diminutive AalphaM and CalphaM fibers, and variants thereof; all with relatively high mitochondrial content (figs. 4, 5, 6). Reinnervation of the sternomastoid muscle by the hypoglossal nerve caused most fibers of the sternomastoid to assume histochemical profiles reminiscent of those commonly observed in the tongue. However, the BbetaD fibers of the sternomastoid persisted in near usual numbers and disposition (fig. 17), despite their reinnervation by a nerve normally destined for a muscle lacking that particular fiber type. Thus, there are as yet unrecognized factors, possibly of neural origin, though more likely of muscle origin (genetic), that impose restrictions on the metabolism-regulating functions of substitute motoneurons.

Adenosine Triphosphatases↗