No abstract

ChemInform Abstract The β-aroylpropionic acids (I) react with thiophene-2-carboxaldehyde (II) to give the butenolides (IIIa) which are transformed into the 5-oxopyrrolines (IIIb) and into the acrylic acid hydrazides (VI). Upon treatment with acid, the hydrazides (VI) are cyclized, forming the pyridazinones (VII). The compounds are tested for their activity against bacteria and yeasts.

The reaction of ethyl 2-arylhydrazono-3-oxobutyrates (Ia, Ib) with active methylene ketones afforded pyridazin-5-carbonitrile derivatives. The methyl function in the ethyl pyridazin-3-carboxylate derivatives IIa, IIb reacted with arylidenemalononitrile to yield the phthalazine derivatives Va-Vf and with elemental sulfur to yield the thienopyridazines XIXa, XIXb. The cinnolines are producted from reaction of IIa, IIb with diethyl acetonedicarboxylate.

Background11β HSD1 generates cortisol from cortisone. 11β HSD1 single-nucleotide polymorphism (SNP) was associated with metabolic syndrome (MeTS). Although the relation of acne vulgaris (AV) and skin tags (STs) with MeTS has been reported, the relationship between 11β HSD 1 SNP and cortisol activity in those patients has not studied till now.AimsTo investigate, two 11β-HSD1 SNPs (rs846910 and rs12086634), serum lipid profile and cortisol levels in patients with AV and STs in an Egyptian population.Patients and methodsThis case–control study was performed on 50 patients having STs and 50 complaining of AV and 50 sex- and age-matched controls. We searched for serum lipid profile, cortisol levels, and 11β-HSD1 rs846910 and rs12086634 SNPs using real time-PCR.ResultsCompared to controls,11β-HSD1 rs846910 GA genotype carriers had significantly higher risks for developing AV and STs by 3.4- and 4.9-fold, respectively, and its A allele increases these risks by 3.1 and 4.4 times, respectively. Also, 11β-HSD1 rs12086634 TG genotype increases the risk of AV by 3.2-fold, as well as STs by 3.5-fold, and its G allele increases the risk of AV by 3.2-fold and STs by 7-fold. In AV and ST patients, rs846910 GA genotype demonstrated significant associations with elevated body mass index (BMI), and cholesterol, low density lipoprotein (LDL), cortisol, and decreased high density lipoprotein serum levels, respectively. However, rs12086634 GG genotype was significantly associated with increased BMI, cholesterol, and LDL serum levels in patients with AV and STs, in addition to the number of STs and serum cortisol levels in ST patients.Conclusion11β-HSD1 rs846910 and rs12086634 gene polymorphisms may contribute to AV and STs pathogenesis, that may be mediated through enhancing the enzymatic activity (increasing cortisol levels). AV and STs are associated with obesity and atherogenic lipid profile. Diagnosis of AV and STs may play a role in early detection of the MeTS.

ChemInform Abstract Coupling of vω-bromoacetophenone (I) with malononitrile (II) gives the phenacylmalononitrile (III) which is cyclized with trichloroacetonitrile (IV), forming the pyrrole (V). Treatment of (III) with AcOH/H2SO4 affords the furan (VI). Starting with the ketone (I), the Knoevenagel product (VII) is prepared, yielding the pyridine (X) via the derivative (IX). This produces also the furan (XI). (No yields given).

The reaction of active methylene reagents Ia-Ie with phenyl isothiocyanate in basic N,N-dimethylformamide solution followed by cyclization with ethyl cyanobromoacetate II affords the acyclic thioether derivatives IVa-IVe. The use of IVa-IVe in heterocyclic synthesis was described.

No abstract

Durch Behandlung der Butenolide (I) bzw. (IV) mit P2S5 (III) erhält man die Thioderivate (II) (orangefarben bis braun) bzw. (V) (rotbraun).