Facile synthesis of some 5-(3-substituted-thiophene)-pyrimidine derivatives and their pharmacological and computational studies

A series of 5-(3-substituted-thiophene)-pyrimidine derivatives (3a-d) were synthesized via Knoevenagel condensation reaction in aq. ethanol using H2O2:HCl as a catalyst. Their pharmacological effects were evaluated. Analytical and spectroscopic methods confirmed the structures of the target molecules. The antibacterial activity studies revealed that compounds 3b and 3d exhibited the most effective zone of inhibition against bacterial strains E. coli and S. aureus, respectively. The in vitro cytotoxicity was carried out by MTT assay against MCF-7 cell line. The results showed excellent selectivity for all four compounds, among which the compound 3a exhibited remarkable cytotoxicity with a minimum cell viability range of 23.68 to 44.16%. The interaction of compounds with calf thymus DNA was determined using UV-absorption spectroscopy. The results confirmed that all the synthesized compounds interacted strongly with CT DNA through electrostatic or groove binding. In silico ADME-toxicology studies indicated that all the molecules under investigation are non-toxic with good oral bioavailability. The drug-likeness score indicated that they are suitable as drug-leads. In silico molecular docking the specified compound 3b bound with GlcN-6-P and P38 MAPk with a minimum binding energy of –7.9 and –6.4 kcal/mol, respectively. DFT study demonstrated that compound 3d was chemically and biologically more reactive due to less energy gap

PHARMACEUTICAL WASTE WATER TREATMENT - A REVIEW

The demand for Air conditioning keeps rising, especially in developing countries where the standard of living has improved. This Results in an increased consumption of electricity and put further pressure on the power grid. Agro industry plays a crucial role in the industrialization process of developing countries. Sugar industry is second largest agro industry in the world. In sugar manufacturing plants there are various processes for production of sugar i.e. extraction of juice, clarification, evaporation, concentration of juice, forming and separating crystals etc. These processes consume energies in the form of mechanical energy, electrical energy and heat energy. So there are various sources of waste heat in sugar factory i.e. waste heat from hot flue gasses, hot water from evaporative body and boiler blow down. The large amount of waste heat passes from various devices of sugar factory causes decrease in the efficiency of sugar plants, and also increase the Global Warming which is very dangerous for our environment

Pharmaceutical Waste Water Treatment - a Review

The demand for Air conditioning keeps rising, especially in developing countries where the standard of living has improved. This Results in an increased consumption of electricity and put further pressure on the power grid. Agro industry plays a crucial role in the industrialization process of developing countries. Sugar industry is second largest agro industry in the world. In sugar manufacturing plants there are various processes for production of sugar i.e. extraction of juice, clarification, evaporation, concentration of juice, forming and separating crystals etc. These processes consume energies in the form of mechanical energy, electrical energy and heat energy. So there are various sources of waste heat in sugar factory i.e. waste heat from hot flue gasses, hot water from evaporative body and boiler blow down. The large amount of waste heat passes from various devices of sugar factory causes decrease in the efficiency of sugar plants, and also increase the Global Warming which is very dangerous for our environment

A Conserved PP2A Regulatory Subunit Enforces Proportional Relationships Between Cell Size and Growth Rate

Cell size is proportional to growth rate. Thus, cells growing rapidly in rich nutrients can be nearly twice the size of cells growing slowly in poor nutrients. This proportional relationship appears to hold across all orders of life, yet the underlying mechanisms are unknown. In budding yeast, most growth occurs during mitosis, and the proportional relationship between cell size and growth rate is therefore enforced primarily by modulating growth in mitosis. When growth is slow, the duration of mitosis is increased to allow more time for growth, yet the amount of growth required to complete mitosis is reduced, which leads to the birth of small daughter cells. Previous studies have found that Rts1, a member of the conserved B56 family of protein phosphatase 2A regulatory subunits, works in a TORC2 signaling network that influences cell size and growth rate. However, it was unclear whether Rts1 influences cell growth and size in mitosis. Here, we show that Rts1 is required for the proportional relationship between cell size and growth rate during mitosis. Moreover, nutrients and Rts1 influence the duration and extent of growth in mitosis via Wee1 and Pds1/securin, two conserved regulators of mitotic progression. Together, the data are consistent with a model in which global signals that set growth rate also set the critical amount of growth required for cell cycle progression, which would provide a simple mechanistic explanation for the proportional relationship between cell size and growth rate

Fe(III)-montmorillonite catalysed one pot synthesis of 5-substituted dihydropyrimidine derivatives as potent antimicrobial agents

أهداف البحث: تهدف هذه الورقة إلى وصف تصنيع سلسلة حديثة من مشتقات بيريميدين ثنائي الهيدرجة خماسي الاستبدال٬ باستخدام مونتموريلونايت الحديديك كعامل مساعد فعال وقابل لإعادة الاستخدام. طرق البحث: تم التأكد من تركيب المركبات المنتَجة باستخدام جهاز ”فورييه“ لتحويل طيف الأشعة تحت الحمراء٬ والرنين المغناطيسي النووي والطرق الطيفية الجماعية. كما تم فحص المركبات المعنونة لمعرفة قدراتها كمضادات للميكروبات والالتحام الجزيئي. النتائج: أظهرت النتائج بأن العامل المساعد ذو قيمة في ما يتعلق بمدة التفاعل وكمية المنتج المُحصَّل. كما تشير النتائج المتعلقة بالنشاط المضاد للميكروبات إلى أن المركبات ”٤ سي “و ” ٤ إي “ و ” ٤ كَي “ أظهرت نشاطا واعدا مضادا للميكروبات ضد الميكروبات المختبرة. الاستنتاجات: من الممكن إعادة تدوير العامل المساعد مرتان إلى ثلاث مرات على الأقل دون انخفاض ملحوظ في فاعليته كعامل مساعد. وأظهرت المركبات المصنّعة نشاطا واعدا مضادا للميكروبات

NMI-SO₂Cl₂-Mediated Amide Bond Formation: Facile Synthesis of Some Dihydrotriazolopyrimidine Amide Derivatives as Potential Anti-Inflammatory and Anti-Tubercular Agents

Facile access to some novel biologically relevant dihydrotriazolopyrimidine carboxylic acid-derived amide analogues using NMI/SO2Cl2, and aromatic and aliphatic primary and secondary amines, is reported herein. The role of N-methylimidazole (NMI) as the base and sulfuryl chloride (SO2Cl2) as the coupling reagent has been effectively realized in accessing these molecules in good to excellent yields. The feasibility of the developed protocol has also been extended to the gram-scale synthesis of N-benzylbenzamide in a 75% yield from benzoic acid and benzyl amine. The newly synthesized compounds were tested via in vitro anti-inflammatory and anti-tubercular activity studies. The compounds 6aa and 6be were found to be the most active anti-inflammatory agents, whereas 6cb and 6ch were found to exhibit promising anti-tubercular potency when compared to other synthesized molecules. The structure–activity relationship (SAR) studies revealed the importance of the presence of electron-donating functionalities in enhancing the anti-inflammatory potential of the newly synthesized molecules. However, the presence of electron-withdrawing substituents was found to be significant for improving their anti-tubercular potency

An exceptional storm accumulation of nautilids in the Lower Cretaceous of the Neuquén Basin, Argentina

An exceptional accumulation of nautilid shells of the species Cymatoceras perstriatum (Steuer) is reported and described in the Lower Cretaceous Agrio Formation of the Neuquén Basin (west-central Argentina). The bed represents a storm deposit in a shallow-water environment within the mid-ramp. The evidences of a storm-related origin of the bed come from the petrographic analysis and taphonomic features of the shells, specially the sedimentary infill pattern. The shells are dispersed in patches within the stratum, without any orientation relative to the bedding plane. It is proposed that the shells were floating after the death of the animals, although most of them have an almost complete living chamber. The presence of some heavily encrusted shells suggests that there is a mixing of specimens with different drift times. A variety of factors related to the origin of such high number of nautilid shells are discussed, including a transgressive stand system tract, the possible existence of a gregarious behaviour, changes in salinity and wind directions. Lower Cretaceous, Nautilids, Neuquén Basin, shell accumulation, storm deposit.Fil: Cichowolski, Marcela. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Ciudad Universitaria. Instituto de Estudios Andinos "Don Pablo Groeber". Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales. Instituto de Estudios Andinos "Don Pablo Groeber"; ArgentinaFil: Pazos, Pablo Jose. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Ciudad Universitaria. Instituto de Estudios Andinos "Don Pablo Groeber". Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales. Instituto de Estudios Andinos "Don Pablo Groeber"; ArgentinaFil: Tunik, Maisa Andrea. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Ciudad Universitaria. Instituto de Estudios Andinos "Don Pablo Groeber". Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales. Instituto de Estudios Andinos "Don Pablo Groeber"; ArgentinaFil: Aguirre Urreta, María Beatriz. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Ciudad Universitaria. Instituto de Estudios Andinos "Don Pablo Groeber". Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales. Instituto de Estudios Andinos "Don Pablo Groeber"; Argentin