Synthesis and molecular docking study of pyrazole clubbed oxazole as antibacterial agents

Research on Chemical Intermediates - We have developed a simple synthetic protocol for the preparation of novel 3-(3-(4-fluorophenyl)-1-phenyl-1H-pyrazol-4-yl)-5-arylisoxazoles. The structure of...     

Disintegration of Gaussian measures and average-case optimal algorithms

It is shown that a Gaussian measure in a given infinite-dimensional Banach space always admits an essentially unique Gaussian disintegration with respect to a given continuous linear operator. This covers a similar statement made earlier in [Lee and Wasilkowski, Approximation of linear functionals on a Banach space with a Gaussian measure, J. Complexity 2(1) (1986) 12–43.] for the case of finite-rank operators.     

Synthesis,biological evaluation,and molecular docking studies of novel pyrazole,pyrazoline-clubbed pyridine as potential antimicrobial agents

We have prepared 15 hybrid pyrazole, pyrazoline-clubbed pyridine–containing compounds (5a-o) and tested for their antibacterial and antifungal activities for the development of potential antimicrobial agents. The structures of this novel series were characterized by various spectral techniques like IR, ¹H NMR, ¹³C NMR, LC–MS, and elemental analysis. The synthesized compounds 5d, 5e, 5i, 5k, 5m, and 5o exhibited significant antimicrobial activity in the comparison of standard drugs. Molecular docking studies that have been carried out to emphasize the binding orientations of these molecules were in good compliance with crystal structure interactions. The predicted drug-likeness (ADME) properties were found to be in the acceptable range.     

Conway’s Question: The Chase for Completeness

We study various degrees of completeness for a Tychonoff space X. One of them plays a central role, namely X is called a Conway space if X is sequentially closed in its Stone–?ech compactification β X (a prominent example of Conway spaces is provided by Dieudonné complete spaces). The Conway spaces constitute a bireflective subcategory Conw of the category Tych of Tychonoff spaces. Replacing sequential closure by the general notion of a closure operator C, we introduce analogously the subcategory Conw _C of C-Conway spaces, that turns out to be again a bireflective subcategory of Tych. We show that every bireflective subcategory of Tych can be presented in this way by building a Galois connection between bireflective subcategories of Tych and closure operators of Top finer than the Kuratowski closure. Other levels of completeness are considered for the (underlying topological spaces of) topological groups. A topological group G is sequentially complete if it is sequentially closed in its Ra?kov completion ${ \ifmmode\expandafter\tilde\else\expandafter\~\fi{G}}$ . The sequential completeness for topological groups is stronger than Conway’s property, although they coincide in some classes of topological groups, for example: free (Abelian) topological groups, pseudocompact groups, etc.     

Observations about equicontinuity and related concepts

The concepts of equicontinuity, even continuity, topological equicontinuity and the newly defined concepts of compact equicontinuity and compact topological equicontinuity are compared. It is shown that for a set of group homomorphisms from a semitopological group to a topological group all these notions of equicontinuities coincide. It is shown also that an infinite-dimensional normed space endowed with its weak topology is an example of a space which does not satisfy the Ascoli theorem in Noble's sense.     

Synthesis,biological evaluation,and molecular docking study of pyridine clubbed 1,3,4-oxadiazoles as potential antituberculars

A series of pyridine clubbed 1,3,4-oxadiazole derivatives were efficiently synthesized, characterized by standard spectral techniques and evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis (MTB) H₃₇Ra and Mycobacterium bovis BCG in active and dormant state using an established methods. Compounds 5a, 5m, and 5t were identified as the most active compounds against MTB. Molecular docking was performed against MTB enoyl-ACP (CoA) reductase (FabI/ENR/InhA) enzyme to predict the binding modes and affinity. The theoretical predictions from molecular docking could establish a link between the observed biological activity and the binding affinity shedding light into specific bonded and non-bonded interactions influencing the activity. The active compounds were studied for cytotoxicity against three cell lines and were found to be non-cytotoxic. Specificity of these compounds was checked by screening them for their antibacterial activity against four bacterial strains.     

Synthesis and characterization of oxazine bearing pyridine scaffold as potential antimicrobial agents

A series of novel compounds 1-((1-(4-(2H-benzo[e][1,3]oxazin-3(4H)-yl)phenyl)ethylidene)amino)-6-((benzylidene)amino)-2-oxo-4-phenyl-1,2-dihydropyridine-3,5-dicarbonitriles (7a–o) were synthesized by a sequence of multistep reactions. IR, ¹H NMR, ¹³C NMR, and mass spectral techniques were used to confirm the structures newly synthesized compounds. Antimicrobial activity of the title compounds (7a–o) was studied against strains of bacteria (Staphylococcus aureus and Streptococcus pyogenes, Escherichia coli and Pseudomonas aeruginosa) and fungi (Candida albicans, Aspergillus niger and Aspergillus clavatus) by serial dilution method. Compounds 7f and 7k exhibited significant antimicrobial activity.