Nitrogen heterocycles are among the most significant structural components of pharmaceuticals. Analysis of our database of U.S. FDA approved drugs reveals that 59% of unique small-molecule drugs contain a nitrogen heterocycle. In this review we report on the top 25 most commonly utilized nitrogen heterocycles found in pharmaceuticals. The main part of our analysis is divided into seven sections: (1) three- and four-membered heterocycles, (2) five-, (3) six-, and (4) seven- and eight-membered heterocycles, as well as (5) fused, (6) bridged bicyclic, and (7) macrocyclic nitrogen heterocycles. Each section reveals the top nitrogen heterocyclic structures and their relative impact for that ring type. For the most commonly used nitrogen heterocycles, we report detailed substitution patterns, highlight common architectural cores, and discuss unusual or rare structures.

Analysis of the Structural Diversity, Substitution Patterns, and Frequency of Nitrogen Heterocycles among U.S. FDA Approved Pharmaceuticals

Polycationic Synergistic Antibacterial Agents with Multiple Functional Components for Efficient Anti-Infective Therapy

Synthesis, antimicrobial and cytotoxic activities of some novel thiazole clubbed 1,3,4-oxadiazoles.

The emergence of antibiotic-resistant bacterial strains has made conventional antibiotic therapies less efficient. The development of a novel nanoantibiotic approach for efficiently ablating such bacterial infections is becoming crucial. Herein, a collection of poly(5-(2-ethyl acrylate)-4-methylthiazole-g-butyl)/copper sulfide nanoclusters (PATA-C4@CuS) was synthesized for efficient capture and effective ablation of levofloxacin-resistant Gram-negative and Gram-positive bacteria upon tissue-penetrable near-infrared (NIR) laser irradiation. In this work, we took advantage of the excellent photothermal and photodynamic properties of copper sulfide nanoparticles (CuSNPs) upon NIR laser irradiation and thiazole derivative as a membrane-targeting cationic ligand toward bacteria. The conjugated nanoclusters could anchor the bacteria to trigger the bacterial aggregation quickly and efficiently kill them. These conjugated nanoclusters could significantly inhibit levofloxacin-resistant Staphylococcus aureus, Esche...

Single Continuous Near-Infrared Laser-Triggered Photodynamic and Photothermal Ablation of Antibiotic-Resistant Bacteria Using Effective Targeted Copper Sulfide Nanoclusters

Synthesis of some new 2-(3-pyridyl)-4,5-disubstituted thiazoles as potent antimicrobial agents

In the last few decades, a lot of work has been done on thiazole ring to find new compounds related to this scaffold to act as antioxidant, analgesic, anti-inflammatory, antimicrobial, antifungal, antiviral, diuretic, anticonvulsant, neuroprotective, and antitumor or cytotoxic drug molecules with lesser side effects. This review presents the up to date development on the design and development of different thiazole derivatives.

Thiazoles: having diverse biological activities

After post General agreement on tariffs and trade (GATT) era there is big surge in herbal based medicines to find out their potential for treatment and cure of diseases and ailments which can or cannot by cured by well established allopathic formulations. For preparation of any herbal formulation identification, evaluation and standardization is rudimentary. Identification involves the morphology, microscopy parameter of plants, evaluation and standardization of herbal drugs includes physical, chemical and biological parameters. These parameters are crucial for preparation of accurate and potent formulation. Reason of these studies involve the safe and accurately selection and handling of crude materials, ensure efficacy and stability of finished product, documentation of safety and risk based on experience, provision of product information to consumer and product promotion.

Identification, evaluation and standardization of herbal drugs: A review

Thiazoles, Having Diverse Biological Activities

Synthesis and Various Biological Potentials of Thiazolopyrimidine Derivatives

The series of eighteen chalcone derivatives were synthesized from various substituted benzaldehyde and acetophenone and evaluated for their possible in-vitro antioxidant activity through free radical scavenging activity using DPPH(1,1-diphenyl-2-picryl-hydrazyl) method. All the synthesized compounds have been confirmed by I.R, 1 H NMR and elemental analysis. Compounds Id, Ie, Ij, Il, Im and Irshowed 50% scavenging during the free radicals

Shiv Jee Kashyap

Papers

Thiazoles: having diverse biological activities

Identification, evaluation and standardization of herbal drugs: A review

Thiazoles, Having Diverse Biological Activities

Synthesis and Various Biological Potentials of Thiazolopyrimidine Derivatives

International journal of drug formulation and research synthesis and in-vitro antioxidant activity of substituted chalcone derivatives