Molecular conformation and biological activity of central nervous system active drugs

1982 ◽  
Vol 2 (4) ◽  
pp. 355-393 ◽  
Author(s):  
P. R. Andrews ◽  
E. J. Lloyd
Author(s):  
Jyothi M ◽  
Ramchander Merugu

Benzoxazoles being structurally similar to bases adenine and guanine interact with biomolecules present in living systems. These compounds possess antimicrobial, central nervous system activities, antihyperglycemic potentiating activity, analgesic, and anti-inflammatory activity. It can also be used as starting material for other bioactive molecules. Modifications in structure and the biological profiles of new generations of benzoxazoles were found to be more potent with enhanced biological activity. Considering all these, we have prepared this review and discussed the synthesis and biological activities of benzoxazoles.


1975 ◽  
Vol 88 (1) ◽  
pp. 1-14 ◽  
Author(s):  
I. Kraulis ◽  
G. Foldes ◽  
H. Traikov ◽  
B. Dubrovsky ◽  
M.K. Birmingham

PEDIATRICS ◽  
1978 ◽  
Vol 62 (6) ◽  
pp. 1128-1133
Author(s):  
Jack Fishman ◽  
Charles Martucci

Assessment of the biological potency of an estrogen in the human has been and remains a formidable task. The problem arises not only from the lack of a readily distinguished physiological endpoint, but also from the diversity of the biological actions of the estrogens. Estrogens exert proliferative effects in recognized target tissues such as endometrium, vagina, and breast,1 and this action is the one commonly associated with the term "estrogenicity." Estrogens, however, also participate in inducing a host of other peripheral responses in tissues such as blood, bone, skin, and others.2 More importantly, the estrogens also exercise major regulatory functions in the central nervous system, including control of pituitary hormone secretion3 and influencing behavior such as food intake4 and sexual receptivity.5 Much attention had been devoted to the design of estrogen structures that would exhibit a specific type of estrogenic activity, such as gonadotropic regulation, without retaining any uterotropic action. Despite the vast numbers of structures synthesized, little clear-cut separation of these activities has been achieved, suggesting that these dual actions of estrogens may be inextricably linked to each other. On the other hand, much effort has also gone into the study of the mechanism of estrogen action in the uterus and in the central nervous system; despite much progress in both directions, little evidence of a commonality between these two responses to estradiol has so far emerged, suggesting that they may not be directly linked. In our studies, we sought to examine whether estradiol metabolism may play a critical role in the expression of the biological activity of the female sex hormone.


2020 ◽  
Vol 31 (4) ◽  
pp. 931-938 ◽  
Author(s):  
Mauro Maccarrone

Abstract Cannabis is one of the earliest cultivated plants, of which Cannabis sativa and Cannabis indica are the most widespread and best characterized species. Their extracts contain (phyto)cannabinoids (pCBs) of therapeutic interest, such as Δ9-tetrahydrocannabinol and cannabidiol, along with many other compounds, so that there is no “one cannabis” but several mixtures even from the same plant. This complexity is mirrored, or even exceeded, by the complexity of the molecular targets that pCBs find in our body, most of which belong to the so-called “endocannabinoid (eCB) system”. Here, we describe the major pCBs and the main components of the eCB system to appreciate their differences and mutual interactions, as well as the potential of using pCB/eCB-based drugs as novel therapeutics to treat human diseases, both in the central nervous system and at the periphery. Moreover, we address the question of the evolution of pCBs and eCBs, showing that the latter compounds were the first to appear in nature, and that the former substances took a few million years to mimic the three-dimensional structures of the latter, and hence their biological activity in our body. Graphic abstract


1997 ◽  
Vol 30 (4-5) ◽  
pp. 433-439 ◽  
Author(s):  
CRISTINA ZOCCHIA ◽  
GIULIO SPIGA ◽  
STUART J RABIN ◽  
MARIA GREKOVA ◽  
JOHN RICHERT ◽  
...  

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