A Critical Review on Therapeutic Potential of Benzimidazole Derivatives: A Privileged Scaffold.

Benzimidazole nucleus is a predominant heterocycle displaying a wide spectrum of pharmacological activities. The privileged nature of the benzimidazole scaffold has been revealed by its presence in most small molecule drugs and in its ability to bind multiple receptors with high affinity. A literature review of the scaffold reveals several instances where structural modifications of the benzimidazole core have resulted in high-affinity lead compounds against a variety of biological targets.

A Unique Perspective on Lead Compounds for Dementia with the Lewy Body.

Dementia with Lewy Bodies is a neurodegenerative disorder characterised by abnormal α-Synuclein aggregate accumulation in Lewy Bodies and Lewy Neurites and the most common form of dementia after Alzheimer's disease. The presynaptic protein alpha-synuclein (α-Syn) regulates synaptic vesicle trafficking and the subsequent release of neurotransmitters in the brain. These aggregates go through a number of crucial stages, such as aggregation, oligomerization, and fibrillation.

2D QSAR, Design, and in Silico Analysis of Thiophene-Tethered Lactam Derivatives as Antimicrobial Agents.

Background: A very high rate of resistance causes health-care-associated and community-acquired infections. E. coli is one of the nine pathogens of highest concern to most of the antibiotics and other class of antimicrobials.

Structure-Activity Relationships of Pyrimidine Derivatives and their Biological Activity - A Review.

Background: Heterocycles play a major role in many fields of biochemical and physiological such as amino acids, DNA bases, vitamins, endogenous neurotransmitters, etc. Nitrogencontaining heterocyclic compounds play a vital role in medicinal chemistry and exhibit notable biological and pharmacological activities. In the past two decades, scientists focused more on the diverse biological activities of pyrimidine derivatives.

QSAR and Molecular Docking Studies of Pyrimidine-Coumarin-Triazole Conjugates as Prospective Anti-Breast Cancer Agents.

Cancer is a life-threatening disease and is the second leading cause of death worldwide. Although many drugs are available for the treatment of cancer, survival outcomes are very low. Hence, rapid development of newer anticancer agents is a prime focus of the medicinal chemistry community.

Acetylcholinesterase Enzyme Inhibitor Molecules with Therapeutic Potential for Alzheimer's Disease.

Acetylcholinesterase (AchE), hydrolase enzyme, regulates the hydrolysis of acetylcholine neurotransmitter in the neurons. AchE is found majorly in the central nervous system at the site of cholinergic neurotransmission. It is involved in the pathophysiology of Alzheimer's diseasecausing dementia, cognitive impairment, behavioral and psychological symptoms.

Multitarget Directed Ligand Approaches for Alzheimer's Disease: A Comprehensive Review.

Background: Alzheimer's disease (AD) is a multifactorial neurodegenerative disease, and a drug which targets a single protein would not provide a cure for this disease. Currently available drugs for AD are all palliative rather than curative. FDA approved only five drugs for the treatment of AD, which include tacrine, donepezil, galantamine, rivastigmine, and memantine.

2D QSAR Analysis of Substituted Quinoxalines for their Antitubercular and Antileptospiral Activities.

Background: The Quantitative structure activity relationship for thirty two novel substituted quinoxalines was performed for their antitubercular (Mycobacterium tuberculosis H37Rv) and antileptospiral (Leptospirainterrogans) activities. The quinoxalines were substituted with azetidinones, thiazolidinones and fluoroquinolones. Several compounds exhibited good activity against both the infections and they all possess fluoroquinolone moiety with the quinoxaline.

Synthesis, leptospirocidal activity and QSAR analysis of novel quinoxaline derivatives.

A simple and efficient method has been developed for the synthesis of series of N-Mannich bases of (E)-3- (phenylimino/4-chlorophenylimino)-2,3-dihydro-1-[(N-substituted piperazinyl) methyl]quinoxaline-2-(1H)-one 3a-f and 4a-f. The requisite 2a and 2b were obtained by reaction between quinoxaline-2,3-dione 1 and aniline/p-chloroaniline. These compounds underwent NMannich reaction with various substituted piperazines to yield (title compounds 3a-f and 4a-f respectively.

Synthesis, in vitro antitubercular activity and 3D-QSAR of novel quinoxaline derivatives.

Twenty new quinoxalines bearing azetidinone and thiazolidinone groups were synthesized by cyclocondensation of Schiff bases of quinoxaline-2, 3-dione and were characterized with several analytical tools. They were tested against Mycobacterium tuberculosis H37Rv at a concentration of 10 μg/mL by Microplate Alamar Blue Assay method. Quinoxaline derivatives with 2-chloro, dimethylamino and nitro substitutions exhibited in vitro activity, comparable to that of the drug, isoniazid.