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Quinoline and its derivatives comprise an important group of heterocyclic compounds that exhibits a wide range of pharmacological properties such as antibacterial, antiviral, anticancer, antiparasitic, anti-Alzheimer and anticholesterol. The quinoline nucleus is found in the structure of many drugs and rational design in medicinal chemistry for the discovery of novel bioactive molecules. Persistent efforts have been made over the years to develop novel congeners with superior biological activities and minimal potential for undesirable side effects. This review highlights some discoveries on the development of quinoline-based compounds in recent years (2013-2019), focusing on their biological activities, including anticancer, antitubercular, antimalarial, anti-ZIKV, anti-DENV, anti- Leishmania and anti-Alzheimers disease.

Proinflammatory cytokines are involved in regulating several reproductive processes that occur during the periovulatory period, including ovulation, corpus luteum formation, and preimplantation embryo development. The objective of this study was to determine whether stimulation of proinflammatory cytokines through administration of mycobacterium cell wall fraction (MCWF; Amplimune, NovaVive) could improve embryo development following superovulation in dairy heifers. A total of 34 independent embryo recovery procedures were performed using nulliparous, Holstein heifers (n = 20; age 12–18 mo) as donors. For superovulation, dominant follicle removal was performed and an intravaginal progesterone device was inserted on d −6. Thirty-six h later, on d −4, follicle stimulating hormone (FSH; 420 IU total) was administered in a decreasing dose regimen consisting of 8 injections given twice-daily at 12 h intervals. Prostaglandin F2αwas administered in conjunction with the 5th and 6th injections of FSH on d −2 and the intravaginal progesterone device was removed in the morning of d −1. Twenty-four hours later, on d 0, donors received their randomly assigned treatment (sterile saline or MCWF, 5 mL, i.m.) and gonadotropin releasing hormone was administered to induce ovulation. Donors were artificially inseminated with frozen-thawed semen at 12 and 24 h after induced ovulation. Non-surgical embryo recovery procedures were performed on d 7. Recovered structures were evaluated using a stereomicroscope to assess embryo development. There was no effect of MCWF treatment on the numbers of total structures, unfertilized oocytes, degenerate embryos, transferable embryos, or blastocysts. However, there was a trend for donors treated with MCWF to have a greater proportion of blastocysts out of total structures recovered. Overall, the efficacy of superovulation in virgin dairy heifer donors was not improved by administration of MCWF during the peri-ovulatory period, but results indicate that MCWF treatment may enhance embryo developmental kinetics.

Introduction: The association between polymorphisms in the bone morphogenetic protein (BMP4) gene and the development of non-syndromic cleft lip with or without cleft palate (NSCL±P) and non-syndromic cleft palate (NSCP) appears to vary between ethnicities. Objectives: To evaluate the association of the tag-SNPs rs11623717, rs17563, rs2071047, and rs2761887 in BMP4 and SNPSNP interaction with a gene from the same pathway in the susceptibility of non-syndromic oral cleft in the Brazilian population. Material and Methods: 800 patients with NSCL±P, 274 NSCP, and 881 controls were genotyped by applying Taqman allelic discrimination assays. The ancestry of each sample was determined with a discriminant panel containing markers of the ancestry of the Brazilian population. SNP-SNP interactions between polymorphisms in BMP4 and other previously studied genes were performed by a logistic regression analysis adjusted for genomic ancestry. Results: No significant association between the SNPs in BMP4 and developing NSCL±P was identified, the presence of polymorphisms rs17563 and rs2761887 were associated with the development of NSCP. In the subgroup with high African ancestry, rs2761887 show significant associations with NSCL±P and NSCP. Thirteen risk SNPSNP interactions for NSCL±P involving BMP4 and FGFR1, GREM1, NOG, VAX1, and the 4p16.2 were found. Conclusions: Our results demonstrate an association between rs17563 and rs2761887 with NSCP and rs2761887 in patients with NSCL±P and NSCP with high African ancestry. SNP-SNP interactions between BMP4 and genes of the same pathway may also be related to the pathogenesis of this common craniofacial malformation. [ABSTRACT FROM AUTHOR]

Benzothiazoles and its derivatives are an important group of heterocyclic compounds that exhibit a wide range of pharmacological properties such as antitumor, antimicrobial, antidiabetic, anticonvulsant and anti-inflammatory. These different biological applications for benzothiazole compounds have motivated new efforts in search for novel derivatives with improved biological activity and diverse applications in pharmaceutical industry. Owing to the importance of this system, the aim of this review is to highlight aspects reported on the chemistry and biological activity of benzothiazoles during the past few years (2000-2010).

A semi-empirical equation is derived to express apparent molar isentropic compressions of electrolytes as a function of the solution molality. This is achieved by combining a recent, more amenable equation for the difference between apparent molar isentropic and isothermal compressions, with Pitzer equations for the apparent molar quantities isothermal compression, isobaric expansion and isobaric thermal capacity. In addition to Pitzer's parameters, the new equation contains only pure-solvent quantities. Second and higher virial coefficients for the apparent molar isentropic compression embody contributions from lower-order coefficients. Contrary to conventional wisdom, the Debye–Hückel limiting law (DHLL) for apparent molar isentropic compressions of salt solutions cannot be translated into a linear dependence on a function of the solution molality. The equation herein introduced is tested with extensive literature data for aqueous solutions of sodium chloride up to saturation concentration at 278, 298 and 318 K. Evidence is found for quaternary ion interactions in apparent molar compressions of concentrated salt solutions below 318 K. The new equation and its up to five-parameter empirical versions are capable of extrapolation to infinite dilution. For the first time, experimental and theoretical DHLL slopes for the apparent molar isentropic compression are found to be in fair agreement. Finally, revised values are given for some thermodynamic properties of aqueous sodium chloride.