Effect of the Epoxide Contents of Liquid Isoprene Rubber as a Processing Aid on the Properties of Silica-filled Natural Rubber Compounds

In this study, we examined the feasibility of using epoxidized liquid isoprene rubber (E-LqIR) as a processing aid for truck and bus radial (TBR) tire treads and investigated the effects of the epoxide content on the wear resistance, fuel efficiency, and resistance to extraction of the E-LqIRs. The results confirmed that, compared to the treated distillate aromatic extract (TDAE) oil, the E-LqIRs could enhance the filler–rubber interactions and reduce the oil migration. However, the consumption of sulfur by the E-LqIRs resulted in a lower crosslink density compared to that of the TDAE oil, and the higher epoxide content decreased the wear resistance and fuel efficiency because of the increased glass-transition temperature (Tg). In contrast, the E-LqIR with a low epoxide content of 6 mol% had no significant effect on the Tg of the final compound and resulted in superior wear resistance and fuel efficiency, compared to those shown by TDAE oil, because of the higher filler–rubber interactions.

Effects of co-administration of Unani pharmacopoeia formulations Qurs Tabasheer Sartani and Arq Hara Bhara with CAT-I antitubercular drugs in rats

Objectives Tuberculosis continues to be a major public health problem globally, despite incredible advancements in healthcare system. In Unani system of medicine, Qurs Tabasheer Sarthani (QTS) and Arq Hara Bhara (AHB) have been traditionally used for tuberculosis like conditions. The study was aimed to investigate the effects of co-administration of QTS and AHB with category I first line antitubercular drugs (CAT-I) on the indices of liver and kidney function in rats. Methods QTS and AHB were prepared individually and mixed to achieve final compound Unani pharmacopoeia formulation (UPF). The human equivalent doses for rats were calculated and administered with and without CAT-I. The effects of the formulations on serum indices of kidney and liver function, hematological markers and plasma CAT-I drug levels were estimated at 14th, 60th & 180th days of treatment. Results The administration of UPF, CAT-I and UPF + CAT-I altered the levels of aspartate transaminase (AST), alanine transaminase (ALT), alkaline phosphatase (ALP) and gamma glutamyltransferase (GGT) and haematological markers. These alterations were within permissible range and randomly distributed among groups during various time points. Administration of CAT-I alone resulted in moderate histopathological changes which were completely abrogated in CAT-I + UPF co-administered animals. The co-administration of UPF with CAT-I improved the plasma peak rifampicin (RIF) levels, without altering the liver and kidney functions. Conclusions The co-administration of UPF with ATT improved liver and kidney functions and increased the plasma levels of RIF. These beneficial findings provide a scope to evaluate the pharmacokinetic studies in humans.

Isolation and degradation characteristics of bacteria in black and odorous water

Bioremediation is one of the treatment technologies for the black-odorous water, and obtaining functional bacteria is the key step to its success. In this study, a number of highly efficient pollutant degrading strains were isolated from the sediment of black-odorous river, and were identified by phenotypic and phylogenetic analysis. The composite bacterial agent J1 was mixed by strains A1, A2, A5 and A7, with a volume ratio of 4:4:2:1. And the final compound bacteria injected into black-odorous water were composed of J1 and NS3, with the volume ratio of 1:1. Optimized degradation conditions of compound bacterium agent were as follows: pH 7.5, DO 2.5 mg/L, temperature 30 °C. Under optimized conditions, add 1% by volume to the black-odorous water for a 50-day experimental operation. Finally, the overlying water ammonia nitrogen, chemical oxygen demand (COD), and total phosphorus has been significantly degraded. The research is expected to contribute to the use of bioremediation methods to repair black-odorous water, and the application of isolates can be carried out in-situ for water types similar to pollute waterways.

UTILIZAÇÃO DA TÉCNICA DE VERMICOMPOSTAGEM PARA REUTILIZAÇÃO DE RESÍDUOS ORGÂNICOS E DE MACRÓFITAS AQUÁTICAS

Currently, the final destination of organic residues and aquatic macrophytes does not occur effectively, directly interfering with the environment and causing environmental problems. Therefore, the work aimed to reuse the organic waste from UNOESTE Campus 2, which comes from the university restaurant, urban cleaning and dairy cattle manure, as well as the aquatic macrophytes of the Cica dam in the municipality of President Prudent, using the vermicomposting technique in different treatments, analyzing the physical and chemical properties of the final compound and suggesting a better destination for such residues. Four treatments were carried out, with three repetitions each, namely: T1 (Dung, Organic waste), T2 (Aquatic Macrophyte, Dung, Organic waste), T3 (Urban cleaning waste, Dung, Organic waste) and T4 (Macrophyte, Waste urban cleaning, manure, organic waste).After collecting the compost, laboratory analyzes were carried out, which showed a significant increase in humidity when compared to the parametersof Normative Instruction SDA No. 25 of 2009. In the treatments carried out, T4 was highlighted by the breeding of earthworms. Therefore, through the execution of this work it was possible to confirm that the application of the vermicomposting technique is feasible for the treatment of organic waste.

Route Exploration and Synthesis of the Reported Pyridone-Based PDI Inhibitor STK076545

The enzyme protein disulfide isomerase (PDI) is essential for the correct folding of proteins and the activation of certain cell surface receptors, and is a promising target for the treatment of cancer and thrombotic conditions. A previous high-throughput screen identified the commercial compound STK076545 as a promising PDI inhibitor. To confirm its activity and support further biological studies, a resynthesis was pursued of the reported b-keto-amide with an N-alkylated pyridone at the a-position. Numerous conventional approaches were complicated by undesired fragmentations or rearrangements. However, a successful 5-step synthetic route was achieved using an aldol reaction with an a-pyridone allyl ester as a key step. An X-ray crystal structure of the final compound confirmed that the reported structure of STK076545 was achieved, however its lack of PDI activity and inconsistent spectral data suggest that the commercial structure was misassigned.

Route Exploration and Synthesis of the Reported Pyridone-Based PDI Inhibitor STK076545

The enzyme protein disulfide isomerase (PDI) is essential for the correct folding of proteins and the activation of certain cell surface receptors, and is a promising target for the treatment of cancer and thrombotic conditions. A previous high-throughput screen identified the commercial compound STK076545 as a promising PDI inhibitor. To confirm its activity and support further biological studies, a resynthesis was pursued of the reported b-keto-amide with an N-alkylated pyridone at the a-position. Numerous conventional approaches were complicated by undesired fragmentations or rearrangements. However, a successful 5-step synthetic route was achieved using an aldol reaction with an a-pyridone allyl ester as a key step. An X-ray crystal structure of the final compound confirmed that the reported structure of STK076545 was achieved, however its lack of PDI activity and inconsistent spectral data suggest that the commercial structure was misassigned.

Efficient and Sustainable Synthesis of a Potent and Selective 5-HT7 Receptor Antagonist Using a Mechanochemical Approach

<div> <p>Recently, ball milling has become an excellent tool in synthetic organic chemistry as it offers several advantages over classical batch synthesis. Here, an efficient and sustainable mechanochemical procedure was developed to obtain <b>PZ-1361</b>, a potent and selective 5-HT₇ receptor antagonist, with significant antidepressant properties in rodents. The elaborated protocol limited the use of organic solvents, reduced the excess of the alkylating agent, and enabled to avoid column chromatography purification of intermediates and the final compound.</p> </div>

Efficient and Sustainable Synthesis of a Potent and Selective 5-HT7 Receptor Antagonist Using a Mechanochemical Approach

<div> <p>Recently, ball milling has become an excellent tool in synthetic organic chemistry as it offers several advantages over classical batch synthesis. Here, an efficient and sustainable mechanochemical procedure was developed to obtain <b>PZ-1361</b>, a potent and selective 5-HT₇ receptor antagonist, with significant antidepressant properties in rodents. The elaborated protocol limited the use of organic solvents, reduced the excess of the alkylating agent, and enabled to avoid column chromatography purification of intermediates and the final compound.</p> </div>

Detailed Molecular and Structural Analysis of Dual Emitter IrQ(ppy)2 Complex

The molecular structure of the 8-hydroxyquinoline–bis (2-phenylpyridyl) iridium (IrQ(ppy)2) dual emitter organometallic compound is determined based on detailed 1D and 2D nuclear magnetic resonance (NMR), to identify metal-ligands coordination, isomerization and chemical yield of the desired compound. Meanwhile, the extended X-ray absorption fine structure (EXAFS) was used to determine the interatomic distances around the iridium ion. From the NMR results, this compound IrQ(ppy)2 exhibits a trans isomerization with a distribution of coordinated N-atoms in a similar way to facial Ir(ppy)3. The EXAFS measurements confirm the structural model of the IrQ(ppy)2 compound where the oxygen atoms from the quinoline ligands induce the splitting of the next-nearest neighboring C in the second shell of the Ir3+ ions. The high-performance liquid chromatography (HPLC), as a part of the detailed molecular analysis, confirms the purity of the desired IrQ(ppy)2 organometallic compound as being more than 95%, together with the progress of the chemical reactions towards the final compound. The theoretical model of the IrQ(ppy)2, concerning the expected bond lengths, is compared with the structural model from the EXAFS and XRD measurements.

Discovery of a picomolar potency pharmacological corrector of the mutant CFTR chloride channel

F508del, the most frequent mutation causing cystic fibrosis (CF), results in mistrafficking and premature degradation of the CFTR chloride channel. Small molecules named correctors may rescue F508del-CFTR and therefore represent promising drugs to target the basic defect in CF. We screened a carefully designed chemical library to find F508del-CFTR correctors. The initial active compound resulting from the primary screening underwent extensive chemical optimization. The final compound, ARN23765, showed an extremely high potency in bronchial epithelial cells from F508del homozygous patients, with an EC50 of 38 picomolar, which is more than 5000-fold lower compared to presently available corrector drugs. ARN23765 also showed high efficacy, synergy with other types of correctors, and compatibility with chronic VX-770 potentiator. Besides being a promising drug, particularly suited for drug combinations, ARN23765 represents a high-affinity probe for CFTR structure-function studies.