1,721,026 research outputs found
Epoxidation of 17-oxo-15,16-methylene steroids with sulfoxonium ylides
No full textA process was disclosed for the epoxidn. of 17-oxo-15,16-methylene steroids, such as I [R3a = R4 = R7 = H, R3b = OH, R5R6 = bond; R3aR3b = O, R4R5 = bond, R6R7 = CH2; R3a = R4 = H, R3b = R5 = OH, R6R7 = CH2], and comprised the use of sulfoxonium ylides, in particular trimethylsulfoxonium iodide. The process allows the prepn. of 17-spiro epoxides with good yields which can be easily transformed into therapeutically useful 17-spironolactone-steroids, such as drospirenone (II)
Co‐Crystalline Phases of Syndiotactic Polystyrene with Azelaic Acid Molecules of Pharmaceutical Interest
Full text linkSorption of dicarboxylic acid molecules of pharmaceutical interest such as azelaic acid (AzA), in syndiotactic polystyrene (sPS) films presenting δ and ε nanoporous crystalline structure, is reported. Fourier Transform Infrared (FTIR), Polarized FTIR and Wide-Angle X-ray diffraction (WAXD) patterns on axially oriented sPS films has been performed to verify their sorption in crystalline lattices resulting in the formation of co-crystalline (CC) phases.
Experimental evidence provides that AzA molecules can be included in the crystalline nanochannels of ε phase both as isolated and hydrogen-bonded molecules whereas they are only dissolved in the amorphous phase of δ sample
Colorimetric tools for solid-phase organic synthesis
Full text linkOne of the unresolved problems of solid-phase organic synthesis (SPOS) is the availability of general and rapid methods to monitor the transformation of functional groups present in molecules supported on insoluble supports. Color tests, far from providing the ultimate solution, may help in detection (and sometimes in quantification) of different functional groups. In this short review, we have collected most of the methods available and applied in SPOS with an Experimental Section that describes the procedure we have successfully applied to bead analyses in our laboratories
Histone deacetylase inhibitors in the treatment of cancer: overview and perspectives
No full textHistone deacetylase inhibitors (HDACis) are one of the last frontiers in pharmaceutical research. Several classes of HDACi have been identified. Although more than 20 HDACi are under preclinical and clinical investigation as single agents and in combination therapies against different cancers, just two of them were approved by the US FDA: Zolinza® and Istodax®, both licensed for the treatment of cutaneous T-cell lymphoma, the latter also of peripheral T-cell lymphoma. Since HDAC enzymes act by forming multiprotein complexes (clusters), containing cofactors, the main problem in designing new HDACi is that the inhibition activity evaluated on isolated enzyme isoforms does not match the in vivo outcomes. In the coming years, the research will be oriented toward a better understanding of the functioning of these protein complexes as well as the development of new screening assays, with the final goal to obtain new drug candidates for the treatment of cancer
A simple procedure for the transformation of L- Glutamic acid into the corresponding g-aldehyde
No full text2-Dibenzylamino-5-oxopentanoic acid benzyl ester has been obtained in good yields by complete benzylation of L-glutamic acid in NaOH and Na2CO3, selective reduction of the gamma-ester into alcohol with DIBAL and further transformation into aldehyde using Swern oxidation. The overall three-step procedure from Glu gave aldehyde in 49% yield
Solid-Phase Synthesis of Conformationally Constrained Peptidomimetics Based on a 3,6-Disubstituted-1,4-diazepan-2,5-dione Core
No full textStarting from a chlorotrityl resin-linked hydroxylamine, a hydroxamic dipeptide having serine at the N-terminus was prepd. by using DMTMM [4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-methylmorpholinium chloride] as the coupling agent. Under microwave heating, Mitsunobu cyclization of the hydroxamic dipeptide gave a 3,6-disubstituted-perhydro-diazepin-2,5-dione in very good yields. Thus, by using Fmoc-Ser-Glu(OCH2CH:CH2)-NH-O-Resin, H3CCO-Gly-OH and H-Pro-OMe, peptidomimetic I was prepd. in four steps in 75% yield
Sensible Improvements Induced by Ionic Liquids in the Reaction of Modified Carbasugars with Bases for the Building of Constrained Carbanucleosides
No full textStarting from racemic 4-hydroxy-4-methyl-2-
cyclopentenone, a family of enantiopure carbanucleosides
locked in the northern conformation has been synthesized.
The use of ionic liquids was determinant in the last step
resulting in a tangible increase of the yields and dramatic
reduction of reaction times and volumes of organic solvents.
To our knowledge, this is the first example of the use of ionic
liquids in the coupling of carbasugars with heterocyclic
bases
Epoxidation of 17-oxo-15,16-methylene steroids with sulfoxonium ylides
No full textA process was disclosed for the epoxidn. of 17-oxo-15,16-methylene steroids, such as I [R3a = R4 = R7 = H, R3b = OH, R5R6 = bond; R3aR3b = O, R4R5 = bond, R6R7 = CH2; R3a = R4 = H, R3b = R5 = OH, R6R7 = CH2], and comprised the use of sulfoxonium ylides, in particular trimethylsulfoxonium iodide. The process allows the prepn. of 17-spiro epoxides with good yields which can be easily transformed into therapeutically useful 17-spironolactone-steroids, such as drospirenone (II)
Apicidine, nuovi peptidi ciclici inibitori dell'istone deacetilasi (HDAC). Sintesi dei residui derivati dall'acido 2-amino 8-oxodecanoico (AODA)
Full text linkLe Apicidine, una famiglia di tetrapeptidi ciclici di origine fungina, hanno mostrato una
elevatissima attività come inibitori reversibili di HDAC. Con l'obiettivo di sintetizzare le Apicidine e preparare analoghi semplificati che mantengano
l'attività di inibitori di HDAC, abbiamo progettato una sintesi generale e multivariabile di
derivati dell'acido 2-ammino-8-oxodecanoico
Is it time to integrate sex and gender into drug design and development?
No full textWhat is gender medicine?
Gender medicine investigates the relation- ship between gender and effectiveness of diagnosis and therapies in the treatment of diseases. Sex and gender affect a broad range of pathophysiological functions, having a sig- ni cant impact on a wide group of diseases. The main areas in uenced by gender are those concerning the cardiovascular, pulmo- nary and autoimmune systems, in addition to diseases involving gastroenterology, hepatol- ogy, nephrology, endocrinology, hematology and neurology. Moreover, the therapeutic processes determining the pharmacokinet- ics and pharmacodynamics [1–3] of drugs and therapeutic agents have been found to differ as a function of gender and sex.
As personalized medicine becomes an increasingly popular concept, the emphasis on gender in tailoring medicine toward an individual has in turn grown [4]. To date, gender medicine has largely focused on women, although gender pharmacology and, gender oriented drug design tends to focus on both sexes, with greater attention given to either women or men depending on if it is an area of insuf cient researc
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