Strong inhibitory effect

Hirsutine (2-795), which belongs to the corynanthe subgroup of the indole alkaloids, was isolated from the plant Uncaria rhynchophylla MIQ and used for the preparation of the old Chinese folk medicine Kampo [397]. It is of pharmacological interest as it shows a strong inhibitory effect on the influenza A virus (subtype H3N2) with an EC50 = 0.40-0.57 pg ml. which is about 11- to 20-fold higher than that of the clinically used ribavirin [398]. 

Twenty-three triterpenoid hydrocarbons isolated from ferns were screened [67]. The following eight exhibited strong inhibitory effects at lxlO2 mol ratio compound/TPA with >80% viability of Raji cells [67]. They are multiflor-8-ene (220 45%), multiflor-9(ll)-ene (228 41%), taraxastane (237 43%), taraxerane (241 37%), glutin-5(10)-ene (244 52%), hop-17(2l)-ene (275 51%), neohop-13(18)-ene (277 37%), and neohop-12-ene (278 37%). It should be mentioned that the inhibitory... 

Suenaga, H., et al. 1995. Strong inhibitory effect of sugar biphenylboronic acid complexes on the hydrolytic activity of alpha-chymotrypsin. J Chem Soc 13 1733. 

Nagai, M., Conney, A.H., and Zhu, B.T., Strong inhibitory effects of common tea catechins and bioflavonoids on the O-methylation of catechol estrogens catalyzed by human Ever cytosolic catechol-O-methyltransferase, Drug Metab. Dispos., 32,497, 2004. 

Our synthesis of OKA and TTM provided various opportunities for collaborating with biochemists, and this collaboration has given birth to our expanding interests toward structural recognition between protein phosphatases (PP) and inhibitors such as OKA or TTM (5). OKA has strong inhibitory effect... 

Crude extracts of the ascidian Didemnum candidum exhibit strong inhibitory effects against phospholipase A2 in vitro. A search for the active component led to the discovery of ascidiatrienolide A 33 (20), an eicosatetraene derivative that is closely related to the didemnilactones 34-36 derived from the tunicate Didemnum moseley (27). The latter are endowed with high affinity to the leukotriene B4 receptor of human polymorphonuclear leucocyte membrane fractions. These fatty acid derivatives of marine origin provided yet another opportunity to validate our strategy for ( ,Z)-control outlined in the previous chapter based upon proper matching of the reactivity of the metathesis catalyst with the conformational preferences of a constrained substrate (22). 

Maprotiline Tetracyclic Strong inhibitory effect on noradrenaline uptake Skin rashes (3%) Increased incidence of seizures in overdose Similar adverse effects profile to tricyclic compounds... 

Maprotiline has a tetracyclic structure, in which the tricyclic nucleus adjoins a fourth ring formed by an ethylene bridge vertical to the major plane of the molecule (SEDA-5, 34). It has a strong inhibitory effect on noradrenaline uptake across cell membranes, and relatively weak effects on serotonergic mechanisms. The half-life averages 43 hours (1), allowing once-daily dosing. 

Of all protease inhibitors, saquinavir is the most potent in vitro. However, owing to poor systemic availability (less than 4%), it is the least potent of all protease inhibitors in use, although a formulation with increased availability has been marketed. However, when saquinavir is given together with ritonavir, the strong inhibitory effect on CYP3A4 of the latter results in high plasma concentrations of saquinavir. This interaction has been exploited, with favorable results, both in... 

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