Covey DF, Evers AS, Mennerick S, Zorumski CF, Purdy RH (Nov 2001). "Recent developments in structure-activity relationships for ... 8. Structure-activity studies of N-acylated 17a-aza-D-homosteroid analogues of the anesthetic steroids (3alpha, 5alpha)- and ( ... Structure- activity studies (SAR) showed that the 3alpha-OH group is essential for the anesthetic actions of these steroids,[31 ... Generally alkyl branching in position 5 means less lipid solubility and less activity. Unsaturation show less activity in ...
Structure activity relationship (SAR)[edit]. Aryloxypropanamine scaffold[edit]. Several reuptake inhibitors contain an ... "Discovery and structure-activity relationships of novel selective norepinephrine and dual serotonin/norepinephrine reuptake ... "Structure-activity relationships of the cycloalkanol ethylamine scaffold: discovery of selective norepinephrine reuptake ... Activity profiles[edit]. SNRIs at the human SERT and NET[49][50][51][52] Compound. SERT. NET. ~Ratio. (5-HT : NE) ...
Structure-activity relationship[edit]. In structure activity relationship experiments it was found that removal of the ... "Structure-activity relationships of aminocoumarin-type gyrase and topoisomerase IV inhibitors obtained by combinatorial ... Structure[edit]. Novobiocin is an aminocoumarin. Novobiocin may be divided up into three entities; a benzoic acid derivative, a ... The GyrA subunit is involved in the DNA nicking and ligation activity. ...
Chirality and structure activity relationships[edit]. Mefloquine is a chiral molecule with two asymmetric carbon centres, which ...
Possible structure-activity relationship for PDE2 inhibitors[edit]. There is a lack of co-crystal structures of inhibitors ... 5.3 Possible structure-activity relationship for PDE2 inhibitors *5.3.1 Upper binding pocket: Gln859 and Asp811 ... Crystal structure[edit]. The crystal structure of the active site of the PDE2 enzyme has been reported. (Picture online: 1Z1L​ ... This hypothesis is supported by the fact that the Asp811Ala mutant has decreased activity toward cAMP, whereas activity toward ...
Structure activity relationship[edit]. The pipecolate region of rapamycin structure seems necessary for rapamycin-binding to ... It was discovered that rapamycin had an anticancer activity and was a non-cytotoxic agent with cytostatic activity against ... The activity of these small molecules from rapalog activity differs in the way by blocking both mTORC1-dependent ... "In Hall, Michael N.; Tamanoi, Fuyuhiko (eds.). Structure, Function and Regulation of TOR complexes from Yeasts to Mammals. The ...
StructureActivity Relationship†". Journal of Agricultural and Food Chemistry. 44 (2): 497-501. doi:10.1021/jf950378u. ISSN ... Chen J, Chua KW, Chua CC, Yu H, Pei A, Chua BH, Hamdy RC, Xu X, Liu CF (2011). "Antioxidant activity of 7,8-dihydroxyflavone ... Unlike many other flavonoids, 7,8-DHF does not show any inhibitory activity on 17β-hydroxysteroid dehydrogenase. 7,8-DHF has ... Le Bail JC, Varnat F, Nicolas JC, Habrioux G (1998). "Estrogenic and antiproliferative activities on MCF-7 human breast cancer ...
Important structure-activity relationship: 1. Strict steric constraint exists around the pyrrolidine ring of cyanopyrrolidine- ... Each inhibitor was important to establish an early structure activity relationship (SAR) for subsequent investigation. It ... It is a potent and selective DPP-4 inhibitor with a 2D-structure very similar to sitagliptin. However, the 3D-structure is ... Existing X-ray structures show that there is not much difference in size and shape of the pocket that indicates that the S1- ...
Structure Activity Relationships "Antibacterial Agents; Structure Activity Relationships," André Bryskier MD. *v ... A quinolone antibiotic is a member of a large group of broad-spectrum bactericides that share a bicyclic core structure related ... The basic pharmacophore, or active structure, of the fluoroquinolone class is based upon the quinoline ring system.[49] The ... High activity against the eukaryotic type II enzyme is exhibited by drugs containing aromatic substituents at their C-7 ...
For the QSAR models, see Quantitative structure-activity relationship.. For the television and radio stations that used the ... The building material of the entire structure is normally adobe, or cut stone and adobe. The idea of the ksar as a granary is a ... Ksour in the Maghreb typically consist of attached houses, often having collective ghorfa (granaries) and other structures like ...
Singh S (March 2000). "Chemistry, design, and structure-activity relationship of cocaine antagonists". Chemical Reviews. 100 (3 ... however consider RTI-229 to be a controlled substance analogue of cocaine on the grounds of its related chemical structure. ...
Singh, S (8 March 2000). "Chemistry, design, and structure-activity relationship of cocaine antagonists". Chemical Reviews. 100 ... Structures closer to the radius are radial, structures closer to the ulna are ulnar, and structures relating to both bones are ... Similarly, in the lower leg, structures near the tibia (shinbone) are tibial and structures near the fibula are fibular (or ... These terms refer to the distance of a structure from the surface or structure.[4] ...
... structure-activity-relationship study". Curr Med Chem. 16 (9): 2468-2474. PMID 19601792. Niemegeers CJ, Schellekens KH, Van ...
Structure-activity relationships. I. Sympathomimetic and related amines." J. Med. Chem. 9 273-280. L. I. Goldberg, P. F. ... The pressor activity of DMDA was partially inhibited by the α-antagonist phentolamine. From these and other observations, the ... J. M. Kitzen, M. Ilhan, J. G. Cannon and J. P. Long (1976). "α-Adrenergic activity of N,N-dimethyldopamine (DMDA)." Eur. J. ... In another assay, 6 mg/kg of DMDA (i.p. in mice) only slightly antagonized the reduced locomotor activity resulting from pre- ...
Structure-activity relationships. I. Sympathomimetic and related amines." J. Med. Chem. 9 273-280. C. J. Barwell et al. (1989 ... Ernst Späth subsequently showed that these alkaloids were identical and proposed the correct molecular structure for this ...
Structure activity relationship (SAR)Edit. Aryloxypropanamine scaffoldEdit. Several reuptake inhibitors contain an ... 2005). "Discovery and structure-activity relationships of novel selective norepinephrine and dual serotonin/norepinephrine ... 2008). "StructureActivity Relationships of the Cycloalkanol Ethylamine Scaffold: Discovery of Selective Norepinephrine ... Activity profilesEdit. SNRIs at the human SERT and NET[49]. Compound. SERT. NET. ~Ratio. (5-HT/NE). ...
"Tetracycline - Structure-activity relationships". University of Bristol. Retrieved 2 October 2018.. *^ Forsberg, Kevin J.; ... "Classification Framework and Structure-Activity-Relationship (SAR) of Tetracycline-Structure-Based Drugs". Antibiotics. 1 (1-13 ... Structure-activity relationshipEdit. Tetracyclines are composed of a rigid skeleton of 4 fused rings (see figure 1).[2] The ... Blackwood, Robert K.; English, Arthur R. (1970). Structure-Activity Relationships in the Tetracycline Series. Advances in ...
Structure-activity relationshipsEdit. Optimal binding at the CB1 receptor requires a para-substituted phenyl ring at the ... Jagerovic, N.; Fernandez - Fernandez, C.; Goya, P. (2008), "CB1 Cannabinoid Antagonists: Structure - Activity Relationships and ... leading to a good understanding of the structure-activity relationship (SAR) within this chemical group. While most compounds ... CBD is a very low-affinity CB1 ligand, that can nevertheless affect CB1 receptor activity in vivo in an indirect manner, while ...
Structure activity relationship (SAR)Edit. Aryloxypropanamine scaffoldEdit. Several reuptake inhibitors contain an ... July 2008). "Structure-activity relationships of the cycloalkanol ethylamine scaffold: discovery of selective norepinephrine ... February 2005). "Discovery and structure-activity relationships of novel selective norepinephrine and dual serotonin/ ... Activity profilesEdit. SNRIs at the human SERT and NET[62][63][7][64]. Compound. SERT. NET. ~Ratio. (5-HT : NE) ...
Structure-activity relationship of N-aryl cinnamides". Journal of Medicinal Chemistry. 48 (1): 71-90. doi:10.1021/jm049485i. ... Gore VK, Ma VV, Tamir R, Gavva NR, Treanor JJ, Norman MH (November 2007). "Structure-activity relationship (SAR) investigations ... "Analysis of structure-activity relationships for the 'A-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl] ... structure-activity relationship of 1,3-diarylalkyl thioureas possessing new vanilloid equivalents". Journal of Medicinal ...
Structure-activity relationship of cloned LPA receptors". FEBS Lett. 478 (1-2): 159-65. doi:10.1016/S0014-5793(00)01827-5. PMID ...
Structure-Activity Relationships". Current Medicinal Chemistry. 7 (2): 211-247. doi:10.2174/0929867003375371. ISSN 0929-8673. ... Isotretinoin, a sebosuppressive agent, may be used to reduce sebaceous gland activity as a last resort in refractory disease. ...
Structure-Activity Relationships". Current Medicinal Chemistry. 7 (2): 211-247. doi:10.2174/0929867003375371. ISSN 0929-8673. ... Because of their non-uniform structure, they breach the skin's barrier function. This barrier breach induces an irritation ... sebosuppressive agent isotretinoin may be used to reduce sebaceous gland activity. However, isotretinoin has potentially ...
Singh SM, Gauthier S, Labrie F (2000). "Androgen receptor antagonists (antiandrogens): structure-activity relationships". Curr ... structure-activity relationships". Current Medicinal Chemistry. 7 (2): 211-47. doi:10.2174/0929867003375371. PMID 10637363.. ... and/or glucocorticoid activity in addition to their antiandrogen activity, and these off-target activities can result in ... Antiandrogens are substances which prevent androgens from expressing their activity at target sites. The inhibitory effect of ...
P.K. Gessner; D.D. Godse; A.H. Krull; J.M. McMullan (March 1968). "Structure-activity relationships among 5-methoxy-N:N- ... Quantitative Structure-Activity Relationships. 18 (6): 548-560. doi:10.1002/(SICI)1521-3838(199912)18:6. 3.0.CO;2-B. Michael B ...
Models of working memory, relying on theories of network oscillations and persistent activity, have been built to capture some ... structure, physiology and cognitive abilities of the nervous system.[1][2][3][4] ... features of the prefrontal cortex in context-related memory.[27] Additional models look at the close relationship between the ... These are the bases for some quantitative modeling of large-scale brain activity.[35] ...