Structure-Activity Relationships of 1-Substituted 2-Nitroimidazoles: Effect of Partition Coefficient and Side-Chain Hydroxyl Groups on Radiosensitization in Vitro

1982 ◽  
Vol 90 (1) ◽  
pp. 98 ◽  
Author(s):  
D. M. Brown ◽  
E. Parker ◽  
J. M. Brown
Keyword(s):  
Partition Coefficient ◽  
Side Chain ◽  
Hydroxyl Groups ◽  
Structure Activity Relationships ◽  
Structure Activity

scholarly journals UFLC-MS-IT-TOF and Bioassay Guided Isolation of Flavonoids as Xanthine Oxidase Inhibitors from Diospyros dumetorum

2017 ◽  
Vol 12 (11) ◽  
pp. 1934578X1701201
Author(s):  
Zhen-Tao Deng ◽  
Tong-Hua Yang ◽  
Xiao-Yan Huang ◽  
Xing-Long Chen ◽  
Jian-Gang Zhang ◽  
...  
Keyword(s):  
Xanthine Oxidase ◽  
Inhibitory Activity ◽  
Folk Medicine ◽  
Hydroxyl Groups ◽  
Active Constituents ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Pulmonary Abscess ◽  
Xanthine Oxidase Inhibitors

Diospyros dumetorum is an important folk medicine for treating pulmonary abscess and inflammation. The leaves of D. dumetorum revealed xanthine oxidase (XOD) inhibitory activity. With the guidance of UFLC-MS-IT-TOF analyses combined with bioassay in vitro, 15 flavonoids were isolated from the active parts of D. dumetorum. Except for 11 (IC50 > 200μM), all compounds showed obvious XOD inhibitory activity with IC50 values of 32.5 ± 0.7 ~ 145.0 ± 3.3 μM. The preliminary structure-activity relationships study suggested that glycosylation on C-3 was unfavorable for XOD inhibitory activity; hydroxyl groups on ring B were essential for maintaining activity; the activity was closely related with the position of galloylation. This is the first recognition of the XOD inhibitory activity and active constituents of D. dumetorum, and will provide valuable information for this plant as a new resource for treating hyperuricemia and gout.

Structure─activity relationships in semi-synthetic penicillins

1971 ◽  
Vol 179 (1057) ◽  
pp. 357-367 ◽  
Keyword(s):  
Antibacterial Activity ◽  
Chemical Nature ◽  
Side Chain ◽  
Structural Variations ◽  
Present Survey ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Large Numbers ◽  
The Relationship

Investigation of the relationship between the antibacterial activity of penicillins and the chemical nature of the side chain began in earnest in 1957, when the isolation of 6-aminopenicillanic acid (6-APA) made possible the preparation of large numbers of N -substituted derivatives. Since that time some 1800 different penicillins have been prepared and studied in Beecham Research Laboratories, and the number examined throughout the world must amount to several thousands. The purpose of the present survey is to try to summarize the general patterns of structure-activity relationships which have emerged from these studies. 6-APA itself has only a low order of antibacterial activity, and the same applies to derivatives in which the amino group at position 6 is substituted by radicals other than acyl groups (figure 1). Hence it soon became clear that no advantage was to be gained from such considerable structural variations, and efforts were concentrated on preparing true penicillins containing acyl side-chains. Virtually all of these show considerable activity in vitro against at least some bacteria, but the spectrum of activity varies widely.

scholarly journals Metallocene Antimalarials: The Continuing Quest

2008 ◽  
Vol 2008 ◽  
pp. 1-10 ◽  
Author(s):  
Margaret A. L. Blackie ◽  
Kelly Chibale
Keyword(s):  
Plasmodium Falciparum ◽  
Antiplasmodial Activity ◽  
Side Chain ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Resistant Strains ◽  
Antimalarial Compounds

Over the last decade, a significant body of research has been developed around the inclusion of a metallocene moiety into known antimalarial compounds. Ferroquine is the most successful of these compounds. Herein, we describe our contribution to metallocene antimalarials. Our approach has sought to introduce diversity sites in the side chain of ferroquine in order to develop a series of ferroquine derivatives. The replacement of the ferrocenyl moiety with ruthenocene has given rise to ruthenoquine and a modest series of analogues. The reaction of ferroquine and selected analogues with Au(PPh3)NO3, Au(C6F5)(tht), and [Rh(COD)Cl2] has resulted in a series of heterobimetallic derivatives. In all cases, compounds have been evaluated for in vitro antiplasmodial activity in both chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum. Preliminary structure-activity relationships have been delineated.

STRUCTURE–ACTIVITY RELATIONSHIPS OF CORTICOSTEROID FEEDBACK AT THE HYPOTHALAMIC LEVEL

1977 ◽  
Vol 74 (3) ◽  
pp. 415-424 ◽  
Author(s):  
M. T. JONES ◽  
E. W. HILLHOUSE ◽  
J. L. BURDEN
Keyword(s):  
Binding Site ◽  
Delayed Feedback ◽  
Hydroxyl Group ◽  
Hydroxyl Groups ◽  
Rat Hypothalamus ◽  
Structure Activity Relationships ◽  
Corticotrophin Releasing Factor ◽  
Structure Activity ◽  
Hypothalamic Level

SUMMARY Structure–activity studies on the corticosteroid fast and delayed feedback receptor mechanisms controlling the secretion of corticotrophin releasing factor (CRF) were carried out with the rat hypothalamus in vitro. The secretion of CRF was induced by acetylcholine (3 pg/ml). The fast feedback receptor appears highly specific, and the structure essential for efficacy involves an 11β-hydroxyl group and an unblocked 21-hydroxyl group. Several steroids showed antagonism and so the binding site is not very specific. 18-Hydroxy,11-deoxycorticosterone, progesterone, 17α-hydroxyprogesterone and 11-deoxycorticosterone were antagonists of fast feedback. The delayed feedback receptor required either an 11β- or a 21-hydroxyl group for efficacy. The binding site required a 17-hydroxyl group when the 11β- or 21-hydroxyl groups were absent. Binding also involved the 3-oxo,4,5-ene structure since steroids in which these are absent were inactive.

Structure-activity relationships of cysteine esters and their effects on thiol levels in rat lung in vitro

1993 ◽  
Vol 45 (8) ◽  
pp. 1605-1612 ◽  
Author(s):  
M.J. Hobbs ◽  
M. Butterworth ◽  
G.M. Cohen ◽  
D.G. Upshall
Keyword(s):  
Rat Lung ◽  
Structure Activity Relationships ◽  
Structure Activity
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