The Role of Five-Membered Heterocycles in the Molecular Structure of Antibacterial Drugs Used in Therapy

Abstract

Five-membered heterocycles are essential structural components in various antibacterial drugs; the physicochemical properties of a five-membered heterocycle can play a crucial role in determining the biological activity of an antibacterial drug. These properties can affect the drug’s activity spectrum, potency, and pharmacokinetic and toxicological properties. Using scientific databases, we identified and discussed the antibacterials used in therapy, containing five-membered heterocycles in their molecular structure. The identified five-membered heterocycles used in antibacterial design contain one to four heteroatoms (nitrogen, oxygen, and sulfur). Antibacterials containing five-membered heterocycles were discussed, highlighting the biological properties imprinted by the targeted heterocycle. In some antibacterials, heterocycles with five atoms are pharmacophores responsible for their specific antibacterial activity. As pharmacophores, these heterocycles help design new medicinal molecules, improving their potency and selectivity and comprehending the structure-activity relationship of antibiotics. Unfortunately, particular heterocycles can also affect the drug’s potential toxicity. The review extensively presents the most successful five-atom heterocycles used to design antibacterial essential medicines. Understanding and optimizing the intrinsic characteristics of a five-membered heterocycle can help the development of antibacterial drugs with improved activity, pharmacokinetic profile, and safety.

Synthesis and Anti‐Bacterial Evaluation of Novel Scaffolds Based on Bis‐Thiazole or bis‐1,3,4‐Thiadiazole Linked to Thieno[2,3‐b]Thiophene as New Hybrid Molecules

“…Several thiazole and thiadiazole compounds are efficient antibacterial agents. They can alter the composition and metabolism of both Gram‐positive and Gram‐negative [79] . According to the results in Table 1, of the thiadiazole derivatives 13 a – n , compound 13 a , which contains the phenyl group at the five‐position of thiadiazole, has the best antibacterial activity against three different bacteria, whereas compound 13 k , which contains the benzoyl group at the same position on the thiadiazole ring, exhibits moderate reactivity.…”

“…They can alter the composition and metabolism of both Gram-positive and Gram-negative. [79] According to the results in Table 1, of the thiadiazole derivatives 13 a-n, compound 13 a, which contains the phenyl group at the five-position of thiadiazole, has the best antibacterial activity against three different bacteria, whereas compound 13 k, which contains the benzoyl group at the same position on the thiadiazole ring, exhibits moderate reactivity. In the case of thiazole derivatives 15 a-f, compound 15 b containing (2-(ptolyl)hydrazineylidene) at the five-position of the thiazole ring was shown to have the highest antibacterial activity when compared to other derivatives.…”

New quinazolin-2,4-dione derivatives incorporating acylthiourea, pyrazole and/or oxazole moieties as antibacterial agents via DNA gyrase inhibition

“…Moreover, ve membered nitrogen heterocycles are vital targets that exploited in the design of antibacterial drug candidates. [12][13][14][15][16] According to the recent studies, quinazolin-2,4-dione fragment attached to acylthiourea core and/or ve membered nitrogen heterocycles possess biological activity, 17 including anticancer, 18 anti-malarial, 19 antibacterial, 20 antiviral, 21 antifungal 22 and anti-inammatory. 23 Our targeted molecules structure design has created from marketed available drugs.…”

Elastic and Electronically Inelastic Cross Sections for the Scattering of Electrons by Pyrrole

“…Five-membered heterocyclic systems play a crucial role in both chemistry and biology, being indispensable for the existence and maintenance of life. These ring molecules, composed of carbon atoms and heteroatoms such as nitrogen, oxygen, or sulfur, are widely recognized for their versatility and significance in various fields of basic and applied research, particularly in the pharmaceutical industry. , Many complex biological systems (including vitamins, hemoglobin, hormones, and others) feature these heterocyclic rings as basic structural components . Furthermore, the presence of these molecules in a compound provides greater metabolic stability, solubility, and bioavailability, characteristics that are crucial in drug design and development.…”