Design and Synthesis of a Lactam-Steroid Derivative and their Theoretical Interaction with a SAR-COV2

Several drugs have been developed for the treatment of severe acute respiratory syndrome coronavirus (SARS-CoV) using different protocols; however, some methods use different reagents that are dangerous and require special conditions. The objective of this research was to synthesize a Lactam-steroid derivative to evaluate its theoretical interaction with SARS-CoV using at 6LU7-protein as a theoretical model. Furthermore, this interaction was carried out in a docking model using hydroxychloroquine and favipiravir as controls. The results showed that the binding energy involved in the interaction of the lactam-steroid derivative with 6LU7 protein surface was lower compared with both hydroxychloroquine and favipiravir. In conclusion, the lactam-steroid derivative could be an alternative therapeutic to treatment of SARS-CoV.

New chloroamide-steroid derivative with biological activity on a casein kinase 2 (CK2)

Several casein kinase 2 inhibitors have been prepared using some protocols which require dangerous reagents and specific conditions. The aim of this study was to synthesize a new chloroacetamide-steroid derivative using some chemical tools. In addition, the effect exerted by chloroacetamide-steroid derivative on casein kinase 2 (CK2) was determinate in an ischemia-reperfusion injury model using quinalizarin and N-tertbuthyl-2-chloroacetamide as controls. The results showed that 1) the chloroacetamide-steroid derivative significantly decrease the ischemia-reperfusion injury translated as infarct area compared with quinalizarin and N-tertbuthyl-2-chloroacetamide. In conclusion, in this study, is reported a facile synthesis of a new chloroacetamide-steroid derivative with biological activity against CK2.

SYNTHESIS , CHARACTERIZATION AND STUDY BIOLOGICAL ACTIVITY SOME NEW DERIVATIVES AMIDE AND PYRAZOLE –PYRAZOLINE OF STEROID ANALOGS .

ABSTRACT The number of steroids and their derivatives possess divers pharmacological activities as drugs for the treatment of a large number of diseases so in this work was suggested prepared two series amides and pyrazoles of steroid analogs ( methyl((5-pregnant-3β,17-diol-15-yl) thio) propanoate) . Amides derivatives ( 6 - 9 ) prepared directionally after treated the steroid analogs with primary amine substituted in basic medium . Carbo hydrazide steroid derivative (10 ) was obtained by treated steroid analogs with hydrazine hydrate , this compound use as intermediate for synthesis Pyrazolin (13 ) as well as Pyrazole (14) . All the newly synthesized compounds have been identified by IR, 1H NMR, 13CNMR, 2D-NMR ( HMBC , HSQC ) and C.H.N Analysis

Synthesis of new azaindeno-acetonitrile derivative with inotropic activity against heart failure model

Several steroid derivatives have prepared as inotropic drugs; however, there are few reports on azaindeno-steroid derivatives with inotropic activity. The objective of this investigation was to prepare some azaindeno-acetonitrile derivatives (compounds 3 to 7) to evaluate their biological activity on left ventricular pressure. The first step was achieved by preparation of azaindeno-steroid derivatives using reactions of etherification and addition. The second stage involves the evaluation of biological activity from azaindeno-steroid derivatives on left ventricular pressure in a heart failure model using either estrone or an enone-steroid derivative (compound 2) as controls. The results showed that only compound 6 increases left ventricular pressure compared with estrone, compounds 2-5 and 6. In conclusion, the positive inotropic effect exerted by compound 6 depends on the functional groups involved in its chemical structure.

Experimental and theoretical evaluation of two indol-steroid-cyclobuta-imidazole derivatives as antibacterial drugs

There some for treatment of infectios deseasses; however, some drugs can induce several adverse effects. The aim of this study was synthesizing and to determinate the antibacterial activity of two indol-steroid-cyclobuta-imidazole complex (compound 11 and 12) against Staphylococcus aureus, Escherichia colli and Klebsiella pneumoniae in a minimum inhibitory concentration (MIC) model, using gentamicin, ciprofloxacin, cefotaxime as controls. The following stage involved the theoretical evaluation of the interaction of both compounds 11 and 12 with the β-lactamase enzyme (5f1g) using a docking software. The data found indicate that compound 12 decrease the growth bacterial of Staphylococcus aureus, Escherichia colli and Streptococcus pneumoniae in comparison with the compound 11 and this effect only was similar to cefotaxime Other theoretical data indicated that compound 12 could interact with different type of amino acids residues such as Ser61, Leu116, Gln117, Asp120, Tyr147, Asn149, Ser209, Tyr218, Thr318, Asn342 involved in the surface of 5f1g compared with 11. These data indicate that; i) the steroid derivative (12) show better affinity by the 5f1g protein in comparison with compound 11 which is translated as higher antibacterial activity; ii) this compound is particularly interesting because could constitute a novel therapy as antibacterial agent.

Design and synthesis of methylthiododec-5-en-7-yn-6-yl-steroid derivativewith positive inotropic activity

There are several drugs for the treatment of heart failure; however, some of these drugs can produce several secondary effects such as hyperkalemia, arrhythmias, and others. Therefore, the aim of this study was synthesized a new methylthiododec-5-en-7-yn-6-yl-steroid derivative using some chemical strategies. In addition, the biological activity of the steroid derivative against heart failure was evaluated using an isolated heart model. Also, the effect produced by this steroid derivative on left ventricular pressure (LVP) was determinate using some positive inotropic drugs such as milrinone, digoxin, levosimedan and dobutamine as controls. The results showed that methylthiododec-5-en-7-yn-6-yl-steroid derivative increase LVP in a dose-dependent manner and this effect was like that produced by milrinone. In conclusion, the biological activity produced by steroid-derivative; 1) depends on the functional groups involved in their chemical structure; 2) could act as a positive inotropic agent similar to milrinone. All these data suggest that steroid-derivative may be a good candidate for the treatment of heart failure.