Facile synthesis of aminobiphenyl sulfonamides via Chan-Lam coupling and their biological evaluation as potent carbonic anhydrase inhibitors.

Inhibition of carbonic anhydrases (EC 4.2.1.

From molecule to medicine: introducing emerging strategies to synthesize potent anticancer purine scaffolds.

Cancer remains a major global health concern, necessitating the continuous development of novel anticancer agents with enhanced efficacy and reduced side effects. Purine derivatives are privileged bioactive scaffolds that play a crucial role in drug discovery due to their presence in essential biomolecules such as DNA, RNA, ATP, and coenzymes. This review highlights the synthesis, structure-activity relationships (SARs), and anticancer evaluations of various purine hybrids, including aryl piperazine, triazole-hybrid piperidine/pyrrolidine, and diazenyl-containing purines, from 2020 to 2024.

An updated survey on the recent advancement of antimalarial molecules: synthetic methodologies and SAR studies.

An ongoing escalation in malaria cases is a critical global health issue and also a leading source of increased mortality rates. Infected mosquitos spread the Plasmodium parasite-based disease,. Recent advancements in antimalarial drug discovery have focused on developing novel molecules with unique mechanisms of action to combat this growing resistance.

Metallo-Organic Complexes Containing Transition Metals; Synthetic Approaches and Pharmaceutical Aspects.

Coordination compounds offer a flexible framework for the thoughtful design of novel therapeutic-metallodrugs because of the unique properties of metal ions, such as their ability to coordinate with a wide range of organic ligands, variable oxidation states, a wide range of geometries, and coordination numbers. The pharmaceutical potential of a metal ion and associated substances is validated by the prevalence of various disease states linked to a metal ion's excess or deficiency within the biological system. Researchers have sought more selective, efficacious metallodrugs that cause fewer adverse effects.

Cracking the code: the clinical and molecular impact of aminopyridines; a review (2019-2024).

Aminopyridines belong to a class of compounds that are monoamino and diamino derivatives of pyridine. They work primarily by blocking voltage-gated potassium channels in a dose-dependent manner. Essential heterocycles used extensively in synthetic, natural products, and medicinal chemistry are aminopyridine and its derivatives.

Cobalt-catalyzed reductive cross-coupling: a review.

Transition-metal-catalyzed reductive cross-coupling is highly efficient for forming C-C bonds. It earns its limelight from its application by coupling unreactive electrophilic substrates to synthesize a variety of carbon-carbon bonds with various hybridizations (sp, sp, and sp), late-stage functionalization, and bioactive molecules' synthesis. Reductive cross-coupling is challenging to bring selectivity but promising approach.

Pd-, Cu-, and Ni-Catalyzed Reactions: A Comprehensive Review of the Efficient Approaches towards the Synthesis of Antibacterial Molecules.

A strong synthetic tool for many naturally occurring chemicals, polymers, and pharmaceutical substances is transition metal-catalyzed synthesis. A serious concern to human health is the emergence of bacterial resistance to a broad spectrum of antibacterial medications. The synthesis of chemical molecules that are potential antibacterial candidates is underway.

Facile Synthesis of -(4-Bromo-3-methylphenyl)pyrazine-2-carboxamide Derivatives, Their Antibacterial Activities against Clinically Isolated XDR , Alkaline Phosphatase Inhibitor Activities, and Docking Studies.

The emergence of extensively drug-resistant Typhi (XDR-) poses a grave public health threat due to its resistance to fluoroquinolones and third-generation cephalosporins. This resistance significantly complicates treatment options, underscoring the urgent need for new therapeutic strategies. In this study, we synthesized pyrazine carboxamides (-) in good yields through the Suzuki reaction.

Approachable Synthetic Methodologies for Second-Generation -Lactamase Inhibitors: A Review.

Some antibiotics that are frequently employed are -lactams. In light of the hydrolytic process of -lactamase, found in Gram-negative bacteria, inhibitors of -lactamase (BLIs) have been produced. Examples of first-generation -lactamase inhibitors include sulbactam, clavulanic acid, and tazobactam.

Microwave-assisted protocol towards synthesis of heterocyclic molecules: a comparative analysis with conventional synthetic methodologies (years 2019-2023): a review.

Microwave-assisted protocols have become extensively accepted across various scientific and technological domains because of their numerous advantages, shorter reaction times, higher yields, and often milder reaction conditions. In this review, we focus on the synthesis of N, O, and S-containing heterocyclic structural cores, crucial in the development of pharmaceuticals, agrochemicals, and materials science following through conventional and microwave method via eliminating the side products and enhances the product yield that is nowadays the biggest barrier for a synthetic chemist. The major findings emphasizes the substantial advantages of microwave-assisted techniques over conventional synthetic protocols.

Recent synthetic strategies for N-arylation of pyrrolidines: a potential template for biologically active molecules.

The chemistry of nitrogen-containing heterocyclic compounds has been a multifaceted area of research for an extended period due to their varied therapeutic and biological significance. N-Aryl pyrrolidine formed by condensation of aryl group with nitrogen atom of pyrrolidine is present in a wide array of compounds. Various significant activities shown by N-arylated pyrrolidine include anti-Alzheimer, antihypoxic, anticancer, plant activator, analgesic effect, and hepatitis C inhibitor.

Facile Synthesis of 5-Bromo--Alkylthiophene-2-Sulfonamides and Its Activities Against Clinically Isolated New Delhi Metallo--Lactamase Producing ST147.

Introduction: New Delhi Metallo--lactamase producing (NDM-1-KP) sequence type (ST) 147 poses a significant threat in clinical settings due to its evolution into two distinct directions: hypervirulence and carbapenem resistance. Hypervirulence results from a range of virulence factors, while carbapenem resistance stems from complex biological mechanisms. The NDM-1-KP ST147 clone has emerged as a recent addition to the family of successful clones within the species.

Synthesis of 2-Ethylhexyl 5-Bromothiophene-2-Carboxylates; Antibacterial Activities against Typhi, Validation via Docking Studies, Pharmacokinetics, and Structural Features Determination through DFT.

A new class of thiophene-based molecules of 5-bromothiophene-2-carboxylic acid () have been synthesized in current research work. All analogs - were synthesized with optimized conditions by coupling reactions of 2-ethylhexyl 5-bromothiophene-2-carboxylate () with various arylboronic acids. The results indicated that the majority of compounds showed promising effective in vitro antibacterial activity.

-Heterocycles as Promising Antiviral Agents: A Comprehensive Overview.

Viruses are a real threat to every organism at any stage of life leading to extensive infections and casualties. -heterocycles can affect the viral life cycle at many points, including viral entrance into host cells, viral genome replication, and the production of novel viral species. Certain -heterocycles can also stimulate the host's immune system, producing antiviral cytokines and chemokines that can stop the reproduction of viruses.

First-Principles Investigations of Novel Guanidine-Based Dyes.

In the pursuit of finding efficient D-π-A organic dyes as photosensitizers for dye-sensitized solar cells (DSSCs), first-principles calculations of guanidine-based dyes [-] were executed using density functional theory (DFT). The various electronic and optical properties of guanidine-based organic dyes with different D-π-A structural modifications were investigated. The structural modification of guanidine-based dyes largely affects the properties of molecules, such as excitation energies, the oscillator strength dipole moment, the transition dipole moment, and light-harvesting efficiencies.

Synthesis of anti-depressant molecules metal-catalyzed reactions: a review.

Depression is one of the most mutilating conditions in the world today. It has been difficult to make advancements toward better, more effective therapies since the introduction of antidepressant medicines in the late 1950s. One important field of medicinal chemistry is the synthesis of antidepressant molecules through metal-catalyzed procedures.

Dinuclear Zn-Catalytic System as Brønsted Base and Lewis Acid for Enantioselectivity in Same Chiral Environment.

Zinc (Zn) is a crucial element with remarkable significance in organic transformations. The profusion of harmless zinc salts in the Earth's outer layer qualifies zinc as a noteworthy contender for inexpensive and eco-friendly reagents and catalysts. Recently, widely recognized uses of organo-Zn compounds in the field of organic synthesis have undergone extensive expansion toward asymmetric transformations.

Synthesis of 1-(4-Bromobenzoyl)-1,3-dicyclohexylurea and Its Arylation via Readily Available Palladium Catalyst-Their Electronic, Spectroscopic, and Nonlinear Optical Studies via a Computational Approach.

In this study, we reported the synthesis of 1-(4-bromobenzoyl)-1,3-dicyclohexylurea by the reaction of DCC (,'-dicyclohexylcarbodiimide) with 4-bromobenzoic acid. Subsequently, we further synthesized a new series of 1-(4-arylbenzoyl)-1,3-dicyclohexylurea (-) derivatives using a Suzuki cross-coupling reaction between 1-(4-bromobenzoyl)-1,3-dicyclohexylurea () and various aryl/heteroaryl boronic acids (). Thus, density functional theory (DFT) calculations have been performed to examine the electronic structure of the synthesized compounds (, -) and to calculate their spectroscopic data.

Synthesis, Anti-Bacterial and Molecular Docking Studies of Arylated Butyl 2-Bromoisonicotinate Against Clinical Isolates of ESBL-Producing ST405 and Methicillin-Resistant .

Introduction: Global public health concerns include the emergence and spread of methicillin-resistant (MRSA) and extended-spectrum beta-lactamase (ESBL-). These pathogens cause infections that are difficult to treat, which can have fatal outcomes and require lengthy hospital stays. As a result, we created butyl 2-bromoisonicotinate and tested its antibacterial effectiveness against the ESBL- ST 405 and MRSA pathogens.

Bio-Oriented Synthesis and Molecular Docking Studies of 1,2,4-Triazole Based Derivatives as Potential Anti-Cancer Agents against HepG2 Cell Line.

Triazole-based acetamides serve as important scaffolds for various pharmacologically active drugs. In the present work, structural hybrids of 1,2,4-triazole and acetamides were furnished by chemically modifying 2-(4-isobutylphenyl) propanoic acid (). Target compounds were produced in considerable yields (70-76%) by coupling the triazole of compound 1 with different electrophiles under different reaction conditions.

Synergistic Antibacterial Screening of and : Phytochemical Profiling and Antioxidant and Hemolytic Activities.

Current studies were performed to investigate the phytochemistry, synergistic antibacterial, antioxidant, and hemolytic activities of ethanolic and aqueous extracts of (EA and WA) and (EC and WC) leaves. Fourier transform infrared data verified the existence of alcoholic, carboxylic, aldehydic, phenyl, and bromo moieties in plant leaves. The ethanolic extracts (EA and EC) were significantly richer in phenolics and flavonoids as compared to the aqueous extracts (WA and WC).

Antibacterial Efficacy of -(4-methylpyridin-2-yl) Thiophene-2-Carboxamide Analogues against Extended-Spectrum-β-Lactamase Producing Clinical Strain of ST 131.

Development in the fields of natural-product-derived and synthetic small molecules is in stark contrast to the ongoing demand for novel antimicrobials to treat life-threatening infections caused by extended-spectrum β-lactamase producing (ESBL ). Therefore, there is an interest in the antibacterial activities of synthesized -(4-methylpyridin-2-yl) thiophene-2-carboxamides (-) against ESBL-producing ST131 strains. A blood sample was obtained from a suspected septicemia patient and processed in the Bactec Alert system.

Antibacterial efficacy of indigenous Pakistani honey against extensively drug-resistant clinical isolates of Salmonella enterica serovar Typhi: an alternative option to combat antimicrobial resistance.

Background: Extensively drug-resistant (XDR) Salmonella enterica serovar Typhi (S. Typhi) poses a grave threat to public health due to increased mortality and morbidity caused by typhoid fever. Honey is a promising antibacterial agent, and we aimed to determine the antibacterial activity of honey against XDR S.

Total Synthesis of Terpenes and Their Biological Significance: A Critical Review.

Terpenes are a group of natural products made up of molecules with the formula (CH) that are typically found in plants. They are widely employed in the medicinal, flavor, and fragrance industries. The total synthesis of terpenes as well as their origin and biological potential are discussed in this review.