A series of new dicarboxylic acid derivatives of 1,3,4-thiadiazines, 1,4-benzopiperizines, 1,4-thiazines, 1,3-thiazoles, 1,3-oxazoles and 1,3-imidazoles have been synthesized in 80-87% yield by the environmentally benign microwave induced technique involving the cyclocondensation of 2,3-dibromosuccinic acid with 2-aminothiophenol, o-phenylene diamine, 1,2,4-triazole, amidinothiocarbamide, amidinocarbamide and guanidine hydrochloride. The structures of all newly synthesized compounds have been established on the basis of analytical and spectral data. Evaluation of antibacterial and antifungal activity showed that almost all compounds exhibited better results than reference drugs thus they could be promising candidates for novel drugs.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3267305 | PMC |
| http://dx.doi.org/10.4103/0250-474x.91581 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Microwave-Assisted Synthesis of Heterocycles via Rhodium(III)-Catalyzed C-H Activation: Norbornadiene as an Acetylene Equivalent.
Org Lett
January 2025
Pfizer Oncology Medicinal Chemistry, 10770 Science Center Drive, San Diego, California 92121, United States.
General procedures for the rhodium-catalyzed annulation of aryl/heteroaryl -pivaloyl hydroxamic acids and norbornadiene have been developed. Employing norbornadiene as an acetylene equivalent enables utilization of diverse heterocyclic substrates for this transformation which fail to react or undergo competitive Lossen rearrangement under previously reported conditions. Microwave heating significantly reduces reaction times compared to conventional protocols and allows a one-step process to be realized.
View Article and Find Full Text PDFRecent Updates on Antibacterial Quinolones: Green Synthesis, Mode of Interaction and Structure-Activity Relationship.
Chem Biodivers
January 2025
Department of Pharmaceutical Chemistry, MM College of Pharmacy, Maharishi Markandeshwar (Deemed to be University), Ambala, India.
Quinolone antibiotics are a crucial class of synthetic antibacterial agents, widely utilized due to their broad spectrum of antibacterial activity. Due to the development of antimicrobial resistance, the potency of quinolone drugs decreased. Many conventional methods have been developed to elevate amination rate and to improve yield.
View Article and Find Full Text PDFSustainable synthesis of antibacterial 3-aryl-2-benzo[b,1,4]oxazin-2-ones via SAr Csp-Csp coupling.
Front Chem
November 2024
Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran.
Introduction: The increasing prevalence of antibiotic-resistant pathogens necessitates the urgent development of new antibacterial agents. Concurrently, synthetic chemistry is moving towards more sustainable practices that minimize environmental impact. This study aims to synthesize 3-aryl-2-benzo[b][1,4]oxazin-2-one derivatives, including the natural product cephalandole A, using a sustainable approach that avoids metal catalysts.
View Article and Find Full Text PDFRecent developments in the photoredox catalyzed Minisci-type reactions under continuous flow.
Chem Commun (Camb)
December 2024
Department of Chemistry and Biochemistry, University of Missouri-St. Louis, One University Boulevard, St. Louis, MO 63121, USA.
Article Synopsis
- The Minisci reaction is an effective method for directly modifying heterocyclic molecules through C-H functionalization, relying on radical chemistry.
- It has gained popularity because its results are predictable based on the types of radicals and heterocycles used.
- The review discusses recent strategies, particularly the use of continuous flow techniques, to scale up this reaction for drug development purposes.
Green Synthesis of 2-Mercapto 5,6-Dihydro-4-1,3-Thiazines via Sequential C-S Couplings.
Molecules
November 2024
State Key Laboratory of NBC Protection for Civilian, Beijing 102205, China.
The six-membered N,S-heterocyclic 1,3-thiazines and their derivatives are widely acknowledged as pharmaceutical molecules with a wide range of biological activities. In this study, we developed a unique thiol-involved cascade reaction that enables the efficient construction of the 5,6-dihydro-4-1,3-thiazine scaffold through consecutive intermolecular thiol-isothiocyanate and intramolecular thiol-halogen click reactions. Structurally diverse 2-mercapto dihydrothiazines including three antitumour candidates of -dihydrothiazines were readily obtained in high yields from the readily available thiols and 3-chloroisothiocyanate in the green solvent EtOH/HO (1:1) using KCO (0.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!