Optimising dynamic mechanical analysis experiments on soft rubbers for use in time temperature superposition.

Rubbers are ubiquitous in engineering applications where they are often subjected to loading leading to high strain rate deformation. The strong rate and temperature dependence of rubbers and their composites motivates research into understanding their mechanical response under a wide range of conditions. However, experimental characterisation of the rate-temperature dependence of soft rubbers is challenging. In this methods paper, an improved methodology is proposed for conducting Dynamic Mechanical Analysis (DMA) experiments on rubbers. The higher quality data produced can be used in time-temperature superposition (TTS) applications to derive a more accurate definition of the rubber's rate-temperature dependence. Overall, the improvements obtained can be summarised as follows:•Overall, the proposed methodology can be summarised with the following improvements:•Reducing clamping artefacts due to volume expansion•Ensuring high quality temperature stability•Improving the contact area between the specimen and the clamps.

Preparation, biological evaluation and molecular docking study of imidazolyl dihydropyrimidines as potential Mycobacterium tuberculosis dihydrofolate reductase inhibitors.

A series of novel dihydropyrimidine derivatives bearing an imidazole nucleus at C-4 position were synthesized in excellent yields via Biginelli multi-component reaction. The newly synthesized compounds were characterized by IR, (1)H NMR, (13)C NMR and Mass spectroscopy. In vitro antitubercular evaluation of all the newly synthesized compounds 4a-p against Mycobacterium tuberculosis (Mtb) H37Rv showed, 4j (MIC: 0.39µg/mL; SI: >25.64), 4m (MIC: 0.78µg/mL; SI: >12.82) and 4p (MIC: 0.39µg/mL; SI: 24.10) as the most promising lead analogues. Compounds 4j, 4m and 4p displayed effective reduction in residual Mtb growth within the tuberculosis-infected macrophage model. Further, molecular docking study of active molecules 4j, 4m and 4p against Mycobacterium tuberculosis dihydrofolate reductase (Mtb DHFR) proved their potency as Mtb DHFR inhibitors acting as potential leads for further development. Pharmacokinetic properties leading to drug-likeness were also predicted for most active molecules 4j, 4m and 4p.

Studies on molecular properties prediction, antitubercular and antimicrobial activities of novel quinoline based pyrimidine motifs.

In the present study, a series of 3-((6-(2,6-dichloroquinolin-3-yl)-4-aryl-1,6-dihydro-pyrimidin-2-yl)thio)propanenitriles 5a-o were synthesized and subjected to molecular properties prediction and drug-likeness model score by Molinspiration property calculation toolkit and MolSoft software, respectively. Compound 5m (4-OCH3) was found to be maximum drug-likeness model score (0.42). Among the screened compounds, 5m showed the most promising antitubercular activity with MIC of 0.20 µg/mL, while compounds 5g, 5k and 5m displayed broad spectrum antibacterial activity against all the bacterial strains. Moreover, compound 5k was found to be the most potent antifungal agent. Further, the results of preliminary MTT cytotoxicity studies on HeLa cells suggested that potent antimicrobial activity of 5g, 5k and 5m was escorted by low cytotoxicity.

Synthesis and evaluation of chalcone analogues based pyrimidines as angiotensin converting enzyme inhibitors.

Hypertension is a widespread and frequently progressive ailment that imparts a foremost threat for cardiovascular and renal disorders. Mammoth efforts are needed for the synthesis of innovative antihypertensive agents to combat this lethal disease. Chalcones have shown antihypertensive activity through inhibition of Angiotensin Converting Enzyme (ACE). Hence, a series of chalcone analogues is synthesized and used as precursor for the synthesis of novel series of pyrimidines. Precursor chalcones were prepared by reacting aldehydes and ketones in presence of sodium hydroxide followed by synthesis of corresponding pyrimidines by reaction with urea in presence of potassium hydroxide. Both groups were then evaluated for their effects on ACE. The results depicted that pyrimidines were more active than chalcones with methoxy (C5 and P5) substitution showing best results to inhibit ACE. Given that chalcone analogues and pyrimidines show a potential as the angiotensin converting enzyme inhibitors.

FUNCTIONS OF VATA (BASED ON CHARAKA) A Passage from Vaatkalaakaleeyam.

The author has chosen 12(th) Chapter from the Sutra Sthana of this great epic containing 12,000 verses and passages which is replete with materials to revive the whole art of healing even if the whole medical literatures is lost. The passage puts in a nutshell the key role played by Vayu / Vata in the working of the tantra and yantra of the body. Though exploration of the humours is yet to be done by modern physiologists to explain the Ayurvedic Vata which is responsible to no less than 18 functions of the normal body mechanism.