Analogs structure/-activity relationships

Kodavanti PRS, Ward TR, McKinney JD, et al. 1996a. Increased pH]phorboI ester binding in rat cerebellar granule cells and inhibition of sequestration in rat cerebellum by polychlorinated diphenyl ether congeners and analogs Structure-activity relationships. Toxicol Appl Pharmacol 138 251-261. 

GR Marshall, CD Barry, HE Bosshard, RA Dammkoehler, DA Dunn. The conformational parameter m drug design The active analog approach. ACS Symp Ser 112 205-226, 1979. JL Fauchere, ed. QSAR Quantitative Structure-Activity Relationships m Drug Design. New York Alan R Liss, 1989, pp 177-181. 

Urotensin II Receptor (GPR14). The vasoactive cyclic peptide urotensin II (U-II) is the endogenous ligand of the G protein-coupled orphan receptor GPR14. Structure-activity relationships from 25 peptide analogs, which mobilize intracellular calcium in GPR14-transfected CHO cells, and the... 

Most relevant for the affinity for A9-THC and analogs to CB-receptors are the phenolic hydroxyl group at C-1, the kind of substitution at C-9, and the properties of the side chain at C-3. Relating to the structure-activity relationships (SAR) between cannabinoids and the CB-receptors, many different modified strucfures of fhis subsfance group were developed and fesfed. The most important variations include variations of the side chain at the olivetolic moiety of the molecules and different substitutions at positions C-11 and C-9. One of the most popular analogous compounds of A9-THC is HU-210 or (-)-trans-ll-OH-A8-THC-DMH, a cannabinoid with a F,l-dimethylheptyl side... 

Mokrosz JL et al. (1995) Structure-activity relationship studies of CNS agents, XIX Quantitative analysis of the alkyl chain effects on the 5-HTlA and 5-HT2 receptor affinities of 4-alkyl-1-arylpiperazines and their analogs. Arch Pharm (Weinheim) 328(2) 143-148... 

TABLE 2. Structure-activity relationship for piperidine analogs... 

Clark-Lewis I, Schumacher C, Baggiofini M, Moser B. Structure-activity relationships of interleukin-8 determined using chemically synthesized analogs. Critical role of NH2-terminal residues and evidence for uncoupling of neutrophil chemo-taxis, exocytosis, and receptor binding activities. J Biol Chem 1991 266 23128-34. 

In addition, the elucidation of structure-activity relationships might provide a lead to the preparation of simpler analogs with biological activity. The use of synthetic intermediates encountered enroute to strigol can be used for the preparation of several analogs representing partial strigol structures. Our endeavors on this theme will be outlined. 

The synthetic studies which have been described have resulted in significant improvements in the preparation of racemic strigol and have also provided access to several analogs which will subsequently be tested for seed germination activity in order to elucidate key structure-activity relationships. These results and further investigations will hopefully lead to effective synthetic compounds for the control of witchweed and related parasitic plants. 

Okada, Y. and Kuroda, Y., Inhibitory action of adenosine and adenosine analogs on neurotransmission in the olfactory cortex slice of guinea pig Structure-activity relationships, European Journal of Pharmacology, 61, 137, 1980. 

Schmid, D., Ecker, G., Kopp, S., Hitzler, M., Chiba, P., Structure-activity relationship studies of propafenone analogs based on P-glycoprotein ATPase activity measurements, Biochem. Pharmacol. 1999, 58, 1447-1456. 

G., Raschack, M., Cappelletto, B., Gigante, M., Boiocchi, M., Structure—activity relationship of verapamil analogs and reversal of multidrug resistance, Biochem. Pharmacol. 1995, 50, 1245-1255. 

The development of new synthetic methodology has successfully enabled the investigation of structure-activity relationships (SAR) of perylenequinone agents for use in photodynamic therapy. Simplified analogs, such as (M)-96, that have potency equal to the natural product hypocrellin and superior chromophores to improve photoactivation in the therapeutic window were prepared. 

With the synthesis of epothilones A and B secured, subsequent studies concentrated on the preparation of analogs of the natural molecules. In addition to providing structure-activity relationships, it was anticipated that these studies would provide a further test for the generality of the RCM process. In this context, a general strategy was developed by Nicolaou et al. [20] to investigate the... 

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