SYNTHESIS OF SOME NOVEL BENZIMIDAZOL-2-ONE DERIVATIVES

For the development of medical and pharmaceutical chemistry is essential to optimize and change relevant structures, possessing biological activity. Herein we report the synthesis of some novel 1H-benzimidazolon-2-one derivatives using aza-Michael addition.For the development of medical and pharmaceutical chemistry is essential to optimize and change relevant structures, possessing biological activity. Herein we report the synthesis of some novel 1H-benzimidazolon-2-one derivatives using aza-Michael addition

Enzyme Inhibition and more--a tribute to John Smith.

When John Smith founded Journal of Enzyme Inhibition in 1985, there were only a few journals publishing interdisciplinary papers on medicinal/pharmaceutical chemistry. Since it focused on a niche a..

Precise Molecular Structures of Cysteine, Cystine, Hydrogen-Bonded Dicysteine, Cysteine Dipeptide, Glutathione and Acetyl Cysteine Based on Additivity of Atomic Radii

Structures of molecules are usually represented by arbitrary line drawings, ball and stick or space filling models. In recent years, the author found that using the appropriate radii of atoms and ions, bond lengths in inorganic, organic and biomolecules and of hydrogen bonds are exact sums of the radii of the adjacent atoms and or ions. This additivity of atomic radii was shown to hold also for the bond lengths in the twenty essential amino acids. On this basis, the atomic structures of the very important molecules mentioned in the title, have been presented here for the first time. It is hoped that these precise structures and their dimensions will shed new light into their role in biochemistry, pharmaceutical chemistry, environmental chemistry, biomedicine and in the mechanism of protein folding

Linking a Pharmaceutical Chemistry Workshop to Pharmacy Practice

This paper describes the design and implementation of a workshop to enhance pharmacy students’ appreciation of the importance of chemistry for pharmacy practice. The workshop was designed to form part of the practical work of two modules taught in the second year of the MPharm degree. In this mandatory workshop, second year pharmacy students were required to spot in the dispensary drugs based on their chemical properties like chirality, their origin and chemical structure. The lecturers involved in the workshop showed examples of the application of chemistry in the day to day work of the dispensary (e.g. calculating the dose for a patient in millimoles or how small modifications from a natural product can change its ability to cross the blood-brain-barrier). Feedback from participating students was collected via two survey instruments to examine the impact of the intervention. The survey results showed a clear shift towards a more positive perception by students of the chemistry taught in the MPharm curriculum

Experimental pharmacological research regarding some new quinazolin-4-ones derivatives

A series of new compounds with quinazolin-4-one structure, synthesized by the Pharmaceutical Chemistry Department of the Faculty of Pharmacy of the University of Medicine and Pharmacy “Carol Davila” Bucharest, was studied. Five of them were selected, conventionally named S1, S2, S3, S4, S5, and investigated in terms of their potential influence on the central nervous system (CNS). For this purpose, the antidepressant effect was determined using the forced swimming test; the anxiolytic/ anxiogenic effect was determined using the suspended plus-shaped maze (Ugo Basile); the effect on the motor activity was determined using the Ugo Basile activity cage; and the potential analgesic effect was investigated using the hot plate test (Ugo Basile). Compounds S3 and S5 lowered the motor activity and showed an anxiolytic effect, while S1 and S2 proved to have antidepressant and analgesic effects. A good correlation between antidepressant and analgesic effects was observed, consistent with the fact that analgesic drugs, by increasing norepinephrine and serotonin levels in the pain inhibiting descendent pathways, can be used as co-analgesics in therapy

Experimental pharmacological research regarding some newly synthesized benzamides on central nervous system functions

Three newly synthesized benzamides by the Department of Pharmaceutical Chemistry of the Faculty of pharmacy from the University of Medicine and Pharmacy „Carol Davila” Bucharest were tested in order to determine whether these new molecules have similar effects on the central nervous system as those already in therapeutic use belonging to the same chemical group, such as tiapride (neuroleptic) or lidocaine (local anaesthetic). Tests were carried out on NMRI mice which were given new compounds, conventionally named I5C, I14C, and II5C in a dose of 1/20 of the lethal dose 50% (LD50), as previously determined. They received this treatment daily for 21 days. The evasive–investigating capacity of mice was determined using the platform test, and the motor activity using an Activity cage device. The results have shown that compounds I5C and II5C decrease the investigation capacity of the mice; and compound I5C inhibits motor activity, while II5C stimulates it. Thus we concluded that only compounds I5C and II5C have a neuroleptic potential that might be investigated further

Advanced strategy for teaching pharmaceutical chemistry courses by implementing pharmacophores strategy instead of SAR one

After studying pharmaceutical chemistry course, the students should learn exact relation between chemical structures of drugs (medicines) and their biological activity. This means that when students watch the chemical  structure of any drug, they should predict their biological activity at a  definite target. In this article a new method was implemented, for the first time, to predict the biological activity of any drug based on  pharmacophores concept rather than the structure-activity-relationship  (SAR) one. The pharmacophores are template that could represent the  interactions exerted by the essential function groups that are carried by  chemical nucleus of the drug. The nucleus of any drug acts only as a  scaffold to carry the essential groups to the nearest point to the  complementary function groups at the binding sites of the drug targets. If we change the chemical nucleus by bioisosteric one that have the same interactions pattern, it will exert the same activity. Implementing this  technique in teaching pharmaceutical chemistry courses may be more  beneficial and accurate for the students to predict the biological activity ofany drugs. [AJCE 4(2), Special Issue, May 2014