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Synthesis and evaluation of novel naphthol diazenyl scaffold based Schiff bases as potential antimicrobial and cytotoxic agents against human colorectal carcinoma cell line (HT-29)

BackgroundIn search of new antimicrobial and cytotoxic agents, a series of new naphthol diazenyl scaffold based Schiff bases (NS1–NS23) was efficiently synthesized by condensation of 2-hydroxy naphthaldehyde azo dyes with various substituted aromatic/heteroaromatic/aliphatic amines.MethodologyThe synthesized derivatives were characterized by various physicochemical and spectral...

A comprehensive review on biological activities of oxazole derivatives

The utility of oxazole as intermediates for the synthesis of new chemical entities in medicinal chemistry have been increased in the past few years. Oxazole is an important heterocyclic nucleus having a wide spectrum of biological activities which drew the attention of researchers round the globe to synthesize various oxazole derivatives and screen them for their various...

Antimicrobial potential of 1H-benzo[d]imidazole scaffold: a review

BackgroundBenzimidazole is a heterocyclic moiety whose derivatives are present in many of the bioactive compounds and posses diverse biological and clinical applications. Benzimidazole agents are the vital pharmacophore and privileged sub-structures in chemistry of medicine. They have received much interest in drug discovery because benzimidazoles exhibited enormous significance...

Synthesis, molecular modelling and biological significance of N-(4-(4-bromophenyl) thiazol-2-yl)-2-chloroacetamide derivatives as prospective antimicrobial and antiproliferative agents

To combat the antimicrobial and anticancer drug resistance by pathogens and cancerous cells, efforts has been made to study the pharmacological activities of newly synthesized N-(4-(4-bromophenyl)thiazol-2-yl)-2-chloroacetamide derivatives. The molecular structures of the synthesized derivatives were confirmed by their physicochemical properties and spectroanalytical data (NMR...

Design, synthesis and biological profile of heterocyclic benzimidazole analogues as prospective antimicrobial and antiproliferative agents

BackgroundNitrogen containing heterocycles are widely used and investigated by pharmaceutical industry, as they are important in discovery and designing of new drug molecules. Drugs with a benzimidazole nucleus possess exclusive structural features and electron-rich atmosphere, which enable them to bind to a number of biologically important targets and result in a wide range of...

4-(2-(1H-Benzo[d]imidazol-2-ylthio)acetamido)-N-(substituted phenyl)benzamides: design, synthesis and biological evaluation

BackgroundDihydrofolate reductase (DHFR) is an important target for antimetabolite class of antimicrobials because it participates in purine synthesis. 2-mercaptobenzimidazole (2MBI) has similar structural features as purine nucleotides. Given that benzimidazole and similar heteroaromatics have been broadly examined for their anticancer potential, so, we hereby report the design...

Estrogen alpha receptor antagonists for the treatment of breast cancer: a review

BackgroundCancer is at present one of the leading causes of death in the world. It accounts for 13% of deaths occurred worldwide and is continuously rising, with an estimated million of deaths up to 2030. Due to poor availability of prevention, diagnosis and treatment of breast cancer, the rate of mortality is at alarming level globally. In women, hormone-dependent estrogen...

Design, synthesis and therapeutic potential of 3-(2-(1H-benzo[d]imidazol-2-ylthio)acetamido)-N-(substituted phenyl)benzamide analogues

BackgroundThe emergence of bacterial resistance is a major public health problem. It is essential to develop and synthesize new therapeutic agents with better activity. The mode of actions of certain newly developed antimicrobial agents, however, exhibited very limited effect in treating life threatening systemic infections. Therefore, the advancement of multi-potent and...

Design, synthesis and biological evaluation of 3-(2-aminooxazol-5-yl)-2H-chromen-2-one derivatives

BackgroundIn view of wide range of biological activities of oxazole, a new series of oxazole analogues was synthesized and its chemical structures were confirmed by spectral data (Proton/Carbon-NMR, IR, MS etc.). The synthesized oxazole derivatives were screened for their antimicrobial and antiproliferative activities.Results and discussionThe antimicrobial activity was performed...

Reverse pharmacophore mapping and molecular docking studies for discovery of GTPase HRas as promising drug target for bis-pyrimidine derivatives

BackgroundPyrimidine is an important pharmacophore in the field of medicinal chemistry and exhibit a broad spectrum of biological potentials. A study was carried out to identify the target protein of potent bis-pyrimidine derivatives using reverse docking program. PharmMapper, a robust online tool was used for identifying the target proteins based on reverse pharmacophore mapping...

Design, synthesis and biological potential of heterocyclic benzoxazole scaffolds as promising antimicrobial and anticancer agents

BackgroundBenzoxazole is the most important class of heterocyclic compound in medicinal chemistry. It has been incorporated in many medicinal compounds making it a versatile heterocyclic compound that possess a wide spectrum of biological activities.ResultsThe molecular structures of synthesized benzoxazole derivatives were confirmed by physicochemical and spectral means. The...

Benzoxazole derivatives: design, synthesis and biological evaluation

BackgroundA new series of benzoxazole analogues was synthesized and checked for their in vitro antibacterial, antifungal and anticancer activities.Results and discussionThe synthesized benzoxazole compounds were confirmed by IR, 1H/13C-NMR, mass and screened for their in vitro antimicrobial activity against Gram-positive bacterium: Bacillus subtilis, four Gram-negative bacteria...

Design, synthesis, antimicrobial and cytotoxicity study on human colorectal carcinoma cell line of new 4,4′-(1,4-phenylene)bis(pyrimidin-2-amine) derivatives

BackgroundPyrimidine molecules attracted organic chemists very much due to their biological and chemotherapeutic importance. Their related fused heterocycles are of interest as potential bioactive molecules so, we have designed and prepared a new class of 4,4′-(1,4-phenylene)bis(pyrimidin-2-amine) molecules and screened for their in vitro antibacterial, antifungal and...

Synthesis and evaluation of antimicrobial, antitubercular and anticancer activities of 2-(1-benzoyl-1H-benzo[d]imidazol-2-ylthio)-N-substituted acetamides

BackgroundThe study describes the synthesis, characterization, in vitro antimicrobial and anticancer evaluation of a series of 2-(1-benzoyl-1H-benzo[d]imidazol-2-ylthio)-N-substituted acetamide derivatives. The synthesized derivatives were also assessed for in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv. The compounds found active in in vitro study were...

Synthesis, characterization, biological evaluation and molecular docking studies of 2-(1H-benzo[d]imidazol-2-ylthio)-N-(substituted 4-oxothiazolidin-3-yl) acetamides

Background A series of 2-(1H-benzo[d]imidazol-2-ylthio)-N-(substituted 4-oxothiazolidin-3-yl) acetamides was synthesized and characterized by physicochemical and spectral means. The synthesized compounds were evaluated for their in vitro antimicrobial activity against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Candida albicans and Aspergillus niger by tube...

Synthesis, molecular docking and biological evaluation of bis-pyrimidine Schiff base derivatives

Vasudevan Syed Adnan Ali Shah Manikandan Selvaraj Balasubramanian Narasimhan 0 0 Faculty of Pharmaceutical Sciences, Maharshi Dayanand University , Rohtak 124001 , India Background: Heterocyclic pyrimidine

Bis-pyrimidine acetamides: design, synthesis and biological evaluation

BackgroundIn the past few years, increased resistance of microorganisms towards antimicrobial agents become a serious health problem, so there is a need for the discovery of new antimicrobial agents. On the other hand, bis-pyrimidines possess various types of biological activity. In view of this, in the present study we have designed and synthesized a new series of bis-pyrimidine...

Variability in CRP, regulatory T cells and effector T cells over time in gynaecological cancer patients: a study of potential oscillatory behaviour and correlations

Mutsa T Madondo 0 Sandra Tuyaerts Brit B Turnbull Anke Vanderstraeten Holbrook Kohrt Balasubramanian Narasimhan Frederic Amant Michael Quinn Magdalena Plebanski 0 1 0 Department of Immunology, Vaccine

A method for calling gains and losses in array CGH data

Array CGH is a powerful technique for genomic studies of cancer. It enables one to carry out genome-wide screening for regions of genetic alterations, such as chromosome gains and losses, or localized amplifications and deletions. In this paper, we propose a new algorithm ‘Cluster along chromosomes’ (CLAC) for the analysis of array CGH data. CLAC builds hierarchical clustering...