Role of synthetic researcher is to develop new routes to synthesize newer molecule and the medicinal chemist is most involved with drug designing and their development. Generally, drugs are the versatile organic molecules used as active ingredients in medicines to diagnose, cure, mitigate, treat, or prevent disease. Inorganic and organometallic molecules are also useful ingredients in medicines. Molecules are built by humans from other molecules found on earth using the skills inherent in our natural brains.

In the past several distinct “ageing” genes have been identified in small animals such as Caenorhabditis (C.) elegans, Drosophila and mouse. Among them are PI-3 kinase (Age), TOR (Target of Rapamycin), PAK1 (RAC/ CDC42-activated kinase 1) and ILK (Integrin-Linked Kinase). KO (Knock Out) of these genes extends the healthy lifespan, increases heat-endurance, and reduces brood size (fertility) of these small animals. In other words, there is a clear “trade-off” relationship between their fertility and survival. In this mini-review we focus mainly on natural or synthetic PAK1-blockers that affect both fertility and survival. Interestingly these PAK1-blockers are among anti-cancer reagents. Thus, unlike conventional anti-cancer drugs such as DNA/RNA/microtubule poisons, these PAK1-blockers could cure cancers without causing any side effects. Both melatonin and a bee product called propolis are among the “longevity-promoting” natural PAK1-blockers. Recently we and others found that even a few synthetic PAK1-blockers such as 15K, highly cell-permeable 1,2,3-triazolyl ester of an old pain killer called Ketorolac are able to boost both lifespan and heat-endurance of C. elegans, while they down regulate the fertility. Here we propose a unique notion that assaying for both anti-fertility and thermo-resistance in C.elegans could serve as both very sensitive and time-saving in vivo screening for potent PAK1-blockers that could cure cancers and many other PAK1-dependent diseases/disorders such as AD (Alzheimer’s disease) without any serious side effects.

Monoamine Oxidise-B is an enzyme which is present in mitochondrial outer membrane. It catalyzes the oxidative deamination of biogenic and xenobiotic amines and plays an important role in the metabolism of neuroactive and vasoactive amines in the central nervous system and peripheral tissues. In this review, we focused to report the synthesis and structure to activity relationship of substituted thiazolyl hydrazones which are selectively inhibitors of MAO-B enzyme.

A Gas Chromatography Mass Spectrometry (GC-MS) method was developed for the simultaneous determination of 3-chloropropane-1,2-diol fatty acid esters (3-MCPDEs), 2-chloropropane-1,3-diol fatty acid esters (2-MCPDEs), 1,3-dichloro-2-propanol fatty acid esters (1,3-DCPEs) and 2,3-dichloro-1-propanol fatty acid esters (2,3-DCPEs) in refined corn oil. The analytes were extracted by solid-phase extraction and were eluted with ethyl acetate. The detection was performed by selected ion monitoring mode for the target compounds. The procedure showed good linearity and precision. The limit of detection and quantification were 2ng/ml and 5ng/ml, respectively. The recoveries of chloropropanol fatty acid esters were in the range of 98.6 ~ 108.3 %. The method has been successfully applied to determine these compounds in refined corn oil.

Lipoxygenase (LOX) products (5- and 12- HETE) have been implicated in carcinogenesis, contribution to invasion and cancer progression. Several LOX-inhibitors have been studied as potential cancer preventive agents, but the specificity of these inhibitors has been doubted. It is therefore important to have a highly selective method, as UPLC-MS/MS, for assessment of the mechanism of action for LOX inhibitors in the cellular context. Design of Experiments (DoE) is a chemo metrical approach which allows for optimization of a quantification method using a limited number of experiments and interaction between experimental factors can be observed. This paper presents optimization of an UPLC-MS/MS method for accurate quantification of the LOX products, 5- and 12- HETE, utilizing DoE. Significant interaction effects where seen between amount of organic solvent in the mobile phase at initial condition and gradient slope as well as between mobile phase flow rate and capillary voltage. A UPLC-MS/MS quantification method was developed and validated for 5- and 12- HETE. An intraday validation assessment showed that the quantitative determination was linear for 5- and 12- HETE in the range tested (1.00-100 ng/ml), and accuracy and precision met the acceptance criteria with a coefficient of variations lower than 15%. Auto-sampler stability was established for 12 hours at 4°C. The optimized method was specific for evaluation of LOX activity in cultured AsPC-1 pancreatic cancer cells. Without added Arachidonic Acid (AA) as substrate LOX products were not detected. After addition of AA, 5- and 12- HETE were quantified in both supernatants and cell lysates, demonstrating the usefulness for cell-based studies in the evaluation of LOX inhibitors.

This report describes a specific and precise Gas Chromatography coupled to a flame ionization detector (GC-FID) method for the quantification of orto cresol (o-cresol) in human urine as biomarker of exposure to toluene. The procedure included an acid hydrolysis step, a liquid-liquid extraction and the GC-FID determination. The mean recovery ranged between 95.4% and 110.6%. The detection and quantification limits were 0.03 µg/ mL and 0.20 µg/mL respectively. The method described is a promising alternative tool for monitoring toluene exposed workers. Data of exposed and non-exposed population to toluene is shown.

Extraction of active polyphenol oxidase and peroxidase from a plant rich in phenolics and chlorophylls in the post-harvest browning syndrome is described. Initially, general optimization using conventional enzyme extractions was performed. However, along with membrane-bound proteins, chlorophylls and phenols were also released with Triton X (TTX). With a view to obtaining high enzymatic activity, removal of the released chlorophylls and phenols by formation of TTX-114 micelles in the detergent rich phase after high-temperature induced phase separation was tested

To detect volatile compounds in wheat flour and steamed bread and identify the variance of the volatiles as affected by wheat storage time, a strong gluten wheat cultivar was harvested and stored in 2009, 2012 and 2015 and then analyzed by Headspace-Solid Phase Micro Extraction (HS-SPME) coupled with Gas Chromatography Mass Spectrometry (GC-MS). A total of 60 types of volatiles were detected, of which 39 were in wheat flour, 33 were in steamed bread, and 11 were in both wheat flour and steamed bread. The compounds were alcohols, aldehydes, alkanes, alkenes, ketones, esters, and others. In wheat flour, alkanes were the most represented compounds, whereas in steamed bread, alcohols were the major compounds in each year. In wheat flour, the amounts of alcohols and aldehydes increased significantly with wheat storage time, whereas alkanes showed the opposite trend. In steamed bread, the amounts of alcohols and aldehydes increased and alkanes decreased markedly with storage time.