S i n c e s eve ra l ye a r s a g o, d i ve r s e corticosteroid derivatives have been development; for example, the synthesis 3α-acetoxy-16α

In this study two new indol-steroid derivatives were synthesized. The first stage involves the synthesis of 17-(2-amino-thiazol-5-yl)-

Two danazol derivatives were synthesized and characterized by spectral analyses. In order to characterize the structural and chemical requirements of danazol derivatives, several parameters such aslogP, π, Rmand Vmwere evaluated. The results showed an increase in the values oflogPfor the compound 6 in comparison with 3. The compound 3 showed an increase in the values of π, R Vmand V Vmwith respect to 6. These data indicate a high degree of lipophilicity and a low steric impediment for compound 6 in comparison with 3.

There are studies which show that several derivatives of brucine have been developed for its use in different biological and analytical methods 1-4. For example, a report shows the synthesis of N-chloromethylbrucine chloride by the reaction of brucine with dichloromethane 5. Other studies have shown the preparation of a brucine derivative (brucidine) by electrolytic reduction of brucine 6. In addition, there are reports of the synthesis of N-(5-carboxypentyl)brucinium bromide via N-alkylation of brucine with 6-bromohexanoic acid 7. Other experimental data showed the preparation of compounds brucinium hydrogen (S)-malate pentahydrate and anhydrous brucinium hydrogen (2R,3R)-tartrate by the reaction between brucine and D-L-malic acid or L-tartaric acid in ethanol:water 8. Additionally, the porphyrin-brucine conjugates was synthetized by the N-alkylation of brucine with alkylbromotetraphenylporphyrin derivatives 9. Recently, a brucine derivative (N 1-(2,3-dimethoxy strychnidin-10-yliden)-ethane-1,2-diamine) was synthetized by the reaction of brucine and ethylenediamine using boric acid as catalyst. Also other brucine derivative (11-[(2-aminoethylamino)-methyl]-2,3-dimethoxystrychnidin-10-ona) was prepared by the reaction of brucine with ethylenediamine in presence of formaldehyde 10. Additionally, other study showed the synthesis of a brucine-dihydropirymidine derivative using the multi-component system (brucine, benzaldehyde and

Experimental studies indicate that some steroid derivatives have inotropic activity; nevertheless, there is scarce information about the effects of the dehydroisoandrosterone and its derivatives at cardiovascular level. In addition, to date the cellular site and mechanism of action of dehydroisoandrosterone at cardiovascular level is very confusing. In order, to clarify those phenomena in this study, a dehydroisoandrosterone derivative was synthesized with the objective of to evaluate its activity on perfusion pressure and coronary resistance and compare this phenomenon with the effect exerted by dehydroisoandrosterone. The Langendorff technique was used to measure changes on perfusion pressure and coronary resistance in an isolated rat heart model in absence or presence of dehydroisoandrosterone and its derivative. Additionally, to characterize the molecular mechanism involved in the inotropic activity induced by dehydroisoandrosterone derivative was evaluated by measuring left ventricular pressure in absence or presence of following compounds; flutamide, prazosin, metoprolol and nifedipine. The results showed that dehydroisoandrosterone derivative significantly increased the perfusion pressure and coronary resistance in comparison with the control conditions and dehydroisoandrosterone. Additionally, other data indicate that dehydroisoandrosterone derivative increase left ventricular pressure in a dose-dependent manner [1 × 10(-9)-1 × 10(-4) mmol]; nevertheless, this phenomenon was significantly inhibited by nifedipine at a dose of 1 × 10(-6) mmol. In conclusion, these data suggest that dehydroisoandrosterone derivative induces positive inotropic activity through of activation the L-type calcium channel.

The aim of this study was synthesizing a steroid-oxazole-oxazete derivative (4) to evaluate their biological activity in vitro. The first stage was achieved by the preparation of a steroid-oxazole-1,2′-[1,3]oxazete] derivative using a series of reactions such as; (1) addition; (2) nitration and (3) cyclization. Then, the biological activity of steroid analog against infarct area was evaluated on an ischemia/reperfusion model using quinalizarin as a control. In addition, the interaction of steroid derivative with kinase protein (CK2) was evaluated using a docking model. The results showed a decrease infarct area (0.001 nM] in a similar form that quinalizarin. In addition, the theoretical analysis suggests that steroid derivative could interact with some aminoacid residues (Gln 86 , Lys 96 , Leu 97 , Leu 98) of 3FL5 protein surface. All these data indicate that steroid derivative can decrease the infarct area via CK2 inhibition.

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There are several methods reported for synthesis of naphthol derivatives; for example, the synthesis of 4-isopropoxynaphthalene-1-carbaldehyde by the reaction of isopropyl o-ethynyl benzoate with butyl vinyl ether using PtCl2 as catalyst 1. Other reports indicate the tandem pummerer Diels-Alder sequence for the preparation of α-thiosubstituted naphthalene derivatives 2. Additionally, other studies 3 showed the synthesis of 1carbamato-alkyl-2-naphthol derivatives via a three-component condensation reaction between aryl aldehydes, 2-naphthol and carbamates in the presence of SiO2-NaHSO4 as a heterogeneous catalyst under thermal and solvent-free conditions 3. Other reports indicate the synthesis of 1,8-diphenylnaphtalene and 1-iodo-8-phenylnaphtalene by the reaction of lithium diphenyl cuprate and aryl halides 4. Also, there are studies 5 which shown the development of (S)-1-(3-hydroxy-2-naphthylcarbonyl)pyrrolidine-2-carboxylic acid methyl ester by the reaction of 3-hydroxy-2-naphthoic acid and (S)-proline methyl ester in presence of SOCl2. In addition, some carbamato-alkyl-naphthol derivatives 6,7 have been synthetized by condensation of βnaphthol, aromatic aldehyde and methyl carbamate in ionic