Thursday, 15 December 2016

Pharmacological Potential of Benzamide Analogues and their Uses in Medicinal Chemistry


Benzamide is a carbonic acid amide of benzoic acid. Amide is a group of organic chemicals with the general formula RCO-NH2 in which a carbon atom is attached to oxygen in double bond and also attached to an hydroxyl group, where ‘R’ groups range from hydrogen to various linear and ring structures or a compound with a metal replacing hydrogen in ammonia such as sodium amide, NaNH2- Amides are divided into subclasses according to the number of substituents on nitrogen. The primary amide is formed by replacementof the carboxylic hydroxyl group by the NH2, amino group. An example is acetamide (acetic acid+amide). Amide is obtained by reaction of an acid chloride, acid anhydride, or ester with an amine.

 Benzamide Analogues

Amides are named with adding ‘-ic acid’ or ‘-oic acid’ from the name of the parent carboxylic acid and replacing it with the suffix ‘amide’. Amide can be formed from ammonia (NH3). The secondary and tertiary amides are the compounds in which one or bothhydrogens in primacy amides are replaced by other groups. The names of secondary and tertiary amides are denoted by the replaced groups with the prefix capital N (meaning nitrogen) prior to the names of parent amides. Low molecular weight amides are soluble in water due to the formation of hydrogen bonds. Primary amides have higher melting and boiling points than secondary and tertiary amides.

Tuesday, 6 December 2016

New Roles of Mitochondrial Transcription Factor A in Cancer



Mitochondria generate cellular energy in the form of adenosine triphosphate (ATP) by the process of oxidative phosphorylation. The organelle contains a small genome that, in animals, encodes 13 essential subunits of the respiratory chain complexes as well as all the rRNAs and tRNAs necessary for their translation. The mitochondrial genome is more vulnerable tooxidative damage and undergoes a higher rate of mutation than the nucleargenome. Otto Warburg observed that tumor slices have elevated levels of glucose consumption and lactate production in the presence of ample oxygen (termed the Warburg effect). He later postulated that cancer originates from irreversible injury to respiration followed by an increase in glycolysis to replace ATP loss due to defective oxidative phosphorylation. 

Mitochondrial Transcription Factor A in Cancer

According to Warburg, this metabolic shift from oxidative phosphorylation to glycolysis converts differentiated cells into undifferentiated cells that proliferate as cancer cells. Although the observation that tumor cells exhibit high levels of aerobic glycolysis has been corroborated, the role of mitochondria in tumor cells has been contentious. While multiple investigators have demonstrated that mitochondria are indeed functional in most tumor cells, some argue that decreases in mitochondrialmetabolism and respiratory rate are essential for tumor cell proliferation. However, the only tumor cells shown to exhibit mitochondrial dysfunction are those that have mutations in the tricarboxylic acid cycle enzymes succinate dehydrogenase or fumarate hydratase. Furthermore, oncogene activation increases mitochondrial metabolism, correlating with metastatic potential.
 

Monday, 28 November 2016

A New Mononuclear Complex: Structure, Vibrational (FT-IR and Raman), Hirshfeld Surfaces Analysis, Electrical Properties and Equivalent Circuit


Hybrid compounds offer attractive opportunities to combine useful properties of both organic and inorganic simples within a single molecular scale composite. On the one hand, these salts offer, scientifically and technologically significant chances in different areas of catalysis, optical properties, biology, magnetic functional materials. On the other hand,they may contribute to higher electrical mobility (as a result of the strongcovalent bonding within these systems). Halogenometalate hybrid compounds based on elements of transition (II) ions prove to have a significant weight to fabricate low-cost electronic devices (as Thin Film Transistor or Organice- Inorganic Emitting Diode). 

A New Mononuclear Complex

Among the most frequently used of polydentate ligands which have the ability with bond to several metal centers, dipicolinic acid (C7H5NO4, 2,6-pyridinedicarboxylic acid) is a well-known that occurs in many natural compounds exhibiting various biological functions and potential pharmacological activities. 2,6-pyridinedicarboxylic The ligand containing N and O polydentate donors, which pave the way provide great advantages for assembling compounds with new structures. The dipicolinic acid ‘dpc’ ligandwith Zn (II) ions has commonly 1 or 2 coordination modes. In one coordination mode, a single planar dpc ligand associates in the equatorial plane of a Zn (II) cation with other ligands such as H2O or pyridine-based heterocycles, which occupy the remaining sites. This leads to the formation of square pyramidal or octahedral coordination geometry or two perpendicularly coordinated planar dipicolinic molecules generating distorted octahedral coordination geometry.

Friday, 25 November 2016

Structure Antimutagenicity Relationship of Anthraquinones



Mutation refers to a heritable change in nucleotide sequence or number, which occurs due to an alteration in the sequence of the code in a gene due to change, removal or insertion of one or more bases in agene, and resulting in an altered gene product. This may be expressed by the change in the structure of a protein which alters or abolishes its enzymatic properties.

Anthraquinones
Mutation occurs spontaneously or may be induced by environmental, industrial, dietary and natural chemicals; it is a cause of innate metabolic defects in cellular systems, triggering morbidity and mortality in living organisms. Mutations cause permanent alteration in DNAstructure, which have been implicated in the etiopathology of cancer and otherdegenerative diseases. A plethora of synthetic and natural substances are known to act as mutagenic, co-carcinogenic and/or carcinogenic agents. These agents produce a variety of lesions in DNA including strand break, base damage and dimerization of bases. De Flora et al.

Friday, 18 November 2016

Conducting Polymers in Biological Systems



Electronics based on π-conjugated organic polymers and molecules have been extensively explored during the last years. The significant interest in the development of organic electronics results in part from the fact that this technology offers new or improved electroactive and opto-electronic features as compared to the inorganic counterparts. The organic electronic materials may be flexible andcan be also fabricated using printing devices. Other characteristics that make organic electronic materials promising as the active material in bioelectronics include:

Polymers in Biological Systems
Functionality which can easily be defined at the materials level, giving that chemical biosignals can be translated into electronics signatures or signals within the material itself.In the thin-layer state organic electronic materials are often transparent, which permits optical transmission imaging and use of various microscopy-based techniques when analyzing biological specimens interacting with the tool.Organic electronic materials are soft and can be (self-)organized to mimic biological structures.Organic conjugated materials conduct electrons as well as ions.Organic conjugated materials can be equipped with (bio-) molecular side-groups to promote cell viability.