scholarly journals Structural Features of Photoallergy to Salicylanilides and Related Compounds*

1966 ◽  
Vol 46 (3) ◽  
pp. 303-305 ◽  
Author(s):  
Leonard C Harber ◽  
Harriet Harris ◽  
Rudolf L Baer
ChemInform ◽  
2006 ◽  
Vol 37 (40) ◽  
Author(s):  
Francesco Caruso ◽  
Miriam Rossi ◽  
Cristian Opazo ◽  
Claudio Pettinari

2012 ◽  
Vol 56 (6) ◽  
pp. 3207-3215 ◽  
Author(s):  
Katrin Ingram ◽  
William Ellis ◽  
Jennifer Keiser

ABSTRACTInteresting antischistosomal properties have been documented for the antimalarial mefloquine, a 4-quinolinemethanol. We evaluated the antischistosomal activities of nine mefloquine-related compounds belonging to the 4-pyridinemethanols, 9-phenanthrenmethanols, and 4-quinolinemethanols. Eight compounds revealed high activities againstSchistosoma mansoni in vitro, with two drugs (the 4-quinolinemethanols WR7573 and WR7930) characterized by significantly lower half-maximal inhibitory concentrations (IC50s) (2.7 and 3.5 μM, respectively) compared to mefloquine (11.4 μM). Mefloquine and WR7930 showed significantly decreased IC50s when incubated in the presence of hemoglobin. High worm burden reductions (WBR) were obtained with enpiroline (WBR, 82.7%; dosage, 200 mg/kg of body weight) and itsthreoisomers (+)-threo(WBR, 100%) and (−)-threo(WBR, 89%) and with WR7930 (WBR, 87%; dosage, 100 mg/kg) against adultS. mansoniin mice. Furthermore, excellentin vitroandin vivoantischistosomal activity was observed for two WR7930-related structures (WR29252 and WR7524). In addition, mefloquine (WBR, 81%), enpiroline (WBR, 77%), and WR7930 (WBR, 100%) showed high activities againstS. haematobiumharbored in mice following single oral doses of 200 mg/kg. These results provide a deeper insight into the structural features of the arylmethanols that rule antischistosomal activity. Further studies should be launched with enpiroline and WR7930.


1967 ◽  
Vol 21 (1) ◽  
pp. 9-15 ◽  
Author(s):  
T. H. Siddall ◽  
C. A. Prohaska

Proton magnetic resonance and infrared spectra were obtained for 44 carbamylphosphonates and related compounds, the common structural features being the grouping As with ordinary amides, slow rotation is observed around the carbonyl-to-nitrogen bond, but the chemical shift between nitrogen substituents is three to five times as great. Evidence is presented for long range coupling of phosphorus to protons in N-substituents. Correlations are observed between the carbonyl and phosphoryl stretching frequencies and substituents both on nitrogen and on phosphorus.


Author(s):  
Luca Bindi ◽  
Cristian Biagioni

Copper and silver are common constituents in natural sulfosalts and can be present as minor or major components. Owing to the different kinds of coordination they can assume, these elements give rise to a number of sulfosalts that are usually quite complex to describe from a structural point of view because of the presence of twinning, disorder, polytypism and sometimes incommensurate modulation. Moreover, it is common to find them in different, partially occupied split sites, favoring the presence of strong ionic conductivity that can be related to a number of interesting technological properties. In this regard, a series of Cu- and Ag-rich sulfosalts showing an excess of these cations with respect to As, Sb and Bi is particularly interesting. Their crystal structures as well as their potential interest for materials science and solid-state physics are outlined. Copper- and mixed (Cu, Ag)-sulfosalts belonging to the wittichenite, tetrahedrite, galkhaite, routhierite and nowackiite series are discussed, together with some related compounds. Whereas in the wittichenite series Cu has either a trigonal planar or tetrahedral coordination, in members of the other series this element forms three-dimensional tetrahedral frameworks giving rise to cavities hosting other cations and anions. More difficult is the description of Ag-rich sulfosalts owing to the highly variable coordination environments shown by this element. Structural features of selected Ag sulfosalts together with members of the argyrodite series are discussed, highlighting the particular properties derived from the behavior of Ag.


1949 ◽  
Vol 27d (2) ◽  
pp. 59-67 ◽  
Author(s):  
Jean P. Picard ◽  
C. W. Kearns

Three series of compounds have been prepared and compared for the insecticidal activities against German roaches and houseflies. The substituted 2,2-diphenyltrichloroethanes and substituted benzohydrols have been found to have comparable activities on roaches. The substituted 2,2-diphenyltrichloroethanes alone had insecticidal properties against houseflies. The benzophenone derivatives were ineffective against both groups of insects.


1965 ◽  
Vol 43 (2) ◽  
pp. 281-290 ◽  
Author(s):  
Catherine Lazier ◽  
P. H. Jellinck

Inhibition studies with compounds having structural features in common with the natural estrogens have shown that 2-hydroxyestrone and 2-hydroxyestradiol are potent inhibitors of the rat liver microsomal system, which converts estrone to water-soluble protein-bound products. Simple phenols and naphthols hydroxylated in the ortho and para positions were also found to be good inhibitors, but the corresponding meta-hydroxylated compounds, as well as various anthraquinones and estrogens substituted in the 6, 10, or 16 positions, were inactive in this respect. The synthetic estrogen, hexestrol, lost its inhibitory activity on conversion to dihydroxy hexestrol, a nonestrogenic analogue. The type of inhibition produced by 2-hydroxyestrone, equilenin, diethylstilbestrol, and menadione has been determined by the Lineweaver–Burk method and shown to be competitive for the first three of these compounds.


INEOS OPEN ◽  
2021 ◽  
Author(s):  
F. V. Drozdov ◽  
◽  
V. M. Kotov ◽  

This review is devoted to the general methods for obtaining guanidine derivatives and related compounds, their chemical properties, and structural features. On the one hand, guanidine and its derivatives play a crucial role in the metabolism of living organisms. On the other hand, owing to their unique properties and simple synthesis, the guanidine derivatives are used as synthetic drugs and biocidal agents, catalysts, ligands, and sweeteners. Furthermore, the guanidine derivatives serve as a basis for the creation of modern smart materials.


Author(s):  
Gary W. Morrow

We saw in the previous chapter how Otto Wallach’s early proposal regarding the structural origin of terpenoid natural products was later refined by the insightful work of Leopold Rudzicka, leading to the biogenetic isoprene rule and all that it implies. In a nearly parallel fashion, we find in our present chapter a second, unrelated class of naturally occurring compounds whose characteristic structural features prompted an initial innovative hypothesis by J. N. Collie near the turn of the 20th century. Collie proposed that certain natural compounds might arise from precursors containing repeated “ketide” (–CH2CO–) units which could then undergo subsequent condensations and other reactions typical of carbonyl compounds to produce some of the observed structures. Unfortunately, Collie’s work was more or less ignored and largely forgotten for nearly a half century, only to be reimagined and expanded in the middle of the century by A. J. Birch, another pioneer whose proposals met with considerable initial resistance. But unlike his predecessor, Birch ultimately prevailed by providing experimental results that supported a comprehensive theory of the biochemical origin of the group of compounds now universally known as “polyketide” natural products. This structurally diverse family includes some of the most useful medicinal agents now known to us, with many members possessing powerful antibacterial, antifungal, anticancer, immunosuppressant, and even cholesterol-lowering biological properties. As we see in Fig. 5.1, such structures range from the relatively simple to the exceedingly complex and may include large macrocyclic lactone rings (macrolides) such as erythromycin, polycyclic ethers such as monensin A, polycyclic structures which may be partly or mostly aromatic as in tetracycline, griseofulvin, or daunorubicin, or nonaromatic polycyclics such as tacrolimus and lovastatin. Some also contain noncyclic linear components that may be saturated, oxygenated, or unsaturated, as seen in different regions of amphotericin B which, like erythromycin, daunorubicin, and many other polyketides, also possesses an aglycone core which has been glycosylated with a carbohydrate component at a specific position. But in spite of this range of structures, many polyketide compounds share some common features that ultimately become more evident upon closer inspection; six-membered rings (either aromatic or nonaromatic) and multiple oxygens which tend to appear in a repeating 1,3-relationship to one another on both acyclic, cyclic, and aromatic structures.


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