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Cationic Surfactants and Quaternary Derivatives for Hair and Skin Care
Published in Randy Schueller, Perry Romanowski, Conditioning Agents for Hair and Skin, 2020
Matthew F. Jurczyk, David T. Floyd, Burghard H. Grüning
The alkyl imidazolines are liquids and normally distributed as aqueous solutions. Imidazolines themselves are not used widely in cosmetics. Amphoteric surfactants, however, can be derived from fatty imidazolines. They are employed in aqueous media. Imidazolines are subject to hydrolysis to the amide, and re-formation of the cyclic structure is probably pH dependent. It has not been established whether the cyclic imidazolines or their hydrolysis products constitute the active species.
Adrenergic Antagonists
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
It is an α-adrenoceptor nonselective antagonist which produces competitive antagonism. Phentolamine, a derivative of imidazoline has a similar/comparable cardiovascular activity to that of phenoxybenzamine. It causes vasodilation by competitively blocking both α1, α2 adrenoceptors with an abatement in PR and systemic BP (Majid et al., 1971; Russell et al., 1998; Juenemann et al., 1986). Activation of reflex sympathetic nerve elevates CO as outlined in Figure 4.3. It is utilized for managing short-term hypertension and bowel pseudo obstruction in pheochromocytoma patients. Moreover, it is utilized to counter anesthesia effect by antagonism of α receptor mediated vasoconstriction brought about by sympathomimetics usually administered along local anesthetics. A main adverse event observed is hypotension. Other effects include cardiac arrhythmia, ischemic cardiac events MI, and tachycardia. The drug administration is via parenteral route (Juenemann et al., 1986). Activity is instant on administration through intravenous route and about 15–20 min through intramuscular (IM) or subcutaneous (SC) route of administration. Its effect endures for about 10–15 min on intravenous administration and through intramuscular it takes 3–4 h. Biotransformation happens in the liver and elimination through urine (Brunton et al., 2011; Seideman, 1982).
Molecular Aspects of the Activity and Inhibition of the FAD-Containing Monoamine Oxidases
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
The one clear example of mixed inhibition that has been fully established is for the imidazoline compound 2-(2-benzofuranyl)-2-imidazoline (2-BFI). The 2-BFI binds in the entrance cavity of MAO B when the cavity is in a particular conformation that can be stabilized by tranylcypromine bound in the catalytic site (Bonivento et al., 2010; McDonald et al., 2010). The I2-type imidazoline compounds bind to a subset of MAO molecules with nanomolar affinity but inhibition of the bulk population of MAO requires micromolar concentrations (Jones et al., 2007; McDonald et al., 2010). The significance of imidazoline binding to MAO in the cell is not clear.
Synthesis, antiproliferative and antitrypanosomal activities, and DNA binding of novel 6-amidino-2-arylbenzothiazoles
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2021
Livio Racané, Valentina Rep, Sandra Kraljević Pavelić, Petra Grbčić, Iva Zonjić, Marijana Radić Stojković, Martin C. Taylor, John M. Kelly, Silvana Raić-Malić
Similarly, the antitrypanosomal evaluations showed that benzothiazole imidazolines 11a–11c and 14a–14c exhibited the best potency, with values that paralleled antiproliferative activity. In contrast to antitumor results, a direct fusion of benzothiazole to 1,2,3-triazole decreased antitrypanosomal activity. 6-Imidazolinobenzothiazole 11b containing p-chlorophenyl at N-1 of 1,2,3-triazole displayed the highest antitrypanosomal potency (IC50 = 0.09 µM, IC90 = 0.12 µM). UV–Vis and CD spectroscopy, as well as thermal denaturation assays, indicated the binding affinities of 6-amidinobenzothiazoles towards ctDNA. Strong positive ICD bands supported minor groove binding, as the dominant binding mode of 11a, 12b and 15b, while small negative and positive ICD signals identified intercalation, as the predominant binding mode of 10b and 11b and 14a–14c.
Synthesis and carbonic anhydrase activating properties of a series of 2-amino-imidazolines structurally related to clonidine1
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
Niccolò Chiaramonte, Soumia Maach, Caterina Biliotti, Andrea Angeli, Gianluca Bartolucci, Laura Braconi, Silvia Dei, Elisabetta Teodori, Claudiu T. Supuran, Maria Novella Romanelli
In search for bioisosters of the imidazole moiety, our attention was attracted by the imidazoline ring. This feature is present in a well-known drug, Clonidine (CLO, Chart 1), which is clinically used as an antihypertensive agent being an agonist at the central α2-adrenergic receptor, but it is able to interact with other targets, such as the imidazoline binding sites and the hyperpolarization-activated cyclic nucleotide gated channels16,17. Therefore, we decided to measure the potential CA activating properties of this compound, finding that CLO behaves as CAA on several CA isoforms (Table 1). Encouraged by this positive outcome, we synthesised a series of 2-substituted imidazolines (compounds 1–24, Chart 1) and tested their activity on five different hCA isoforms. The ubiquitous cytosolic enzymes CA I and II, the mitochondrial CA VA, which is associated with the glucose homeostasis,18 the cytosolic CA VII which is particularly abundant in the CNS and has been recently demonstrated to have a protective role against oxidative damage,19 and the cytosolic CA XIII, which is particularly expressed in the reproductive organs20,21 were selected.
Pharmacotherapeutic strategies for treating hypertension in patients with obesity
Published in Expert Opinion on Pharmacotherapy, 2018
Revathy Carnagarin, Vance Matthews, Cynthia Gregory, Markus P. Schlaich
Given the important role of increased sympathetic outflow in the pathogenesis of OHT, it is perhaps surprising that central sympatholytic blockade with imidazoline I1-receptor agonists is not used more frequently in the management of OHT. Some misconceptions may exist relating to the adverse effects of older central sympatholytic agents such as clonidine or α-methyldopa, which were commonly associated with tiredness, sedation, and rebound hypertension when ceased (clonidine). The newer imidazoline I1-receptor agonists such as moxonidine and rilmenidine have been demonstrated to be well tolerated and effective in lowering BP. In contrast to clonidine which binds to central α2 receptors, the newer agents bind to the Imidazoline I1-receptor thereby largely avoiding the clonidine like side effects [66,67]. However, a dry mouth sensation can occur in up to 10% of patients on moxonidine due to its inhibitory effect on salivary flow [68]. From a metabolic perspective, moxonidine has been demonstrated to enhance insulin sensitivity, as shown with an insulin clamp technique in obese spontaneously hypertensive rats [69]. In addition to BP lowering, moxonidine treatment improves insulin sensitivity in patients with obesity hypertension [70]. The BP-lowering effect of moxonidine was comparable to amlodipine, but with additional effects such as the improvement of insulin resistance, reduction of plasma leptin levels and attenuation of sympathetic overdrive [71].