SCI时时刷

search
Synthesis and antimalarial activity of 7-chloroquinoline-tethered sulfonamides and their [1,2,3]-triazole hybrids
Synthesis and antimalarial activity of 7-chloroquinoline-tethered sulfonamides and their [1,2,3]-triazole hybrids
Aim & background: Drugs with multiple bioactive moieties have the advantages of multiple modes of action and fewer cha...
Benzo[d]thiazole-2-carboxamides as new antituberculosis chemotypes inhibiting mycobacterial ATP phosphoribosyl transferase
Benzo[d]thiazole-2-carboxamides as new antituberculosis chemotypes inhibiting mycobacterial ATP phosphoribosyl transferase
Aims: The screening of antimycobacterial benzo[d]thiazole-2-carboxamides against ATP-phosphoribosyl transferase (ATP-PRTas...
Targeting FGFRs for tumor therapy: current status and novel strategies
Targeting FGFRs for tumor therapy: current status and novel strategies
The FGF receptors (FGFRs) belong to a family of receptor tyrosine kinases. Abundant evidence shows that FGFRs are closely ...
Major structure–activity relationships of resolvins, protectins, maresins and their analogues
Major structure–activity relationships of resolvins, protectins, maresins and their analogues
Resolvins, protectins and maresins are a series of polyunsaturated fatty acid-derived molecules which play important roles...
Efficacy of natural antimicrobial peptides versus peptidomimetic analogues: a systematic review
Efficacy of natural antimicrobial peptides versus peptidomimetic analogues: a systematic review
Aims: This systematic review was carried out to determine whether synthetic peptidomimetics exhibit significant advantages...
Novel Set of Highly Substituted Bis-pyridines: Synthesis, Molecular Docking and Drug-Resistant Antibacterial Profile
Novel Set of Highly Substituted Bis-pyridines: Synthesis, Molecular Docking and Drug-Resistant Antibacterial Profile
Aims: Development of antimicrobial agents having the ability to prevent bacterial biofilm formation which causes serious h...
Hitting drug-resistant malaria infection with triazole-linked flavonoid–chloroquine hybrid compounds
Hitting drug-resistant malaria infection with triazole-linked flavonoid–chloroquine hybrid compounds
Background: Malaria represents the major parasitic disease in tropical regions, and the development of new potent drugs is...
Synthesis and anti-ovarian cancer effects of benzimidazole-2-substituted pyridine and phenyl propenone derivatives
Synthesis and anti-ovarian cancer effects of benzimidazole-2-substituted pyridine and phenyl propenone derivatives
Background: Given the benzimidazole derivatives have anti-ovarian cancer effects, the authors aimed to determine whether b...
2-hydroxy-1,4-naphthoquinones with 3-alkyldiarylether groups: synthesis and Plasmodium falciparum inhibitory activity
2-hydroxy-1,4-naphthoquinones with 3-alkyldiarylether groups: synthesis and Plasmodium falciparum inhibitory activity
Background: In 1948, the synthesis and Plasmodium lophurae activity of 2-hydroxy-1,4-naphthoquinones containing 3-alkyldia...
Biological activity evaluation of novel monoamine oxidase inhibitory compounds targeting Parkinson disease
Biological activity evaluation of novel monoamine oxidase inhibitory compounds targeting Parkinson disease
Aim: Design of 5-methoxy benzofuran hybrids with 2-carbohydrazide and 2-(1,3,4-oxadiazol-2-yl) as potential inhibitors of ...
Design, synthesis and biological characteristics of pyrazolo[3,4-d]pyrimidine derivatives as potential VEGFR-2 inhibitors
Design, synthesis and biological characteristics of pyrazolo[3,4-d]pyrimidine derivatives as potential VEGFR-2 inhibitors
Aim: Several VEGFR-2 inhibitors with the structure of [3,4-d]pyrimidine and based on sorafenib were designed and synthesiz...
Advances in nonclassical phenyl bioisosteres for drug structural optimization
Advances in nonclassical phenyl bioisosteres for drug structural optimization
The phenyl group is the most prevalent ring system and plays an essential role as a pharmacophore or scaffold in marketed ...
Natural products as lead compounds for treatment of neglected tropical diseases: dream or reality?
Natural products as lead compounds for treatment of neglected tropical diseases: dream or reality?
The authors have no relevant affiliations or financial involvement with any organization or entity with a financial intere...
Photodynamic properties of lysine and arginine derivatives of bacteriopurpurinimide
Photodynamic properties of lysine and arginine derivatives of bacteriopurpurinimide
Background: O-propyloxime-N-propoxybacteriopurpurinimide methyl ester (3) is a near-infrared photosensitizer with confirme...
Serendipitous identification of Phenylhydrazine derivatives as potent inhibitors of Carbapenem-resistant Acinetobacter baumannii
Serendipitous identification of Phenylhydrazine derivatives as potent inhibitors of Carbapenem-resistant Acinetobacter baumannii
Background: In the authors' previous study, 4-(2-((3-methyl-4-oxo-2-thioxo/dioxothiazolidin-5-ylidene) methyl) hydrazineyl...
Recent approaches to mRNA vaccine delivery by lipid-based vectors prepared by continuous-flow microfluidic devices
Recent approaches to mRNA vaccine delivery by lipid-based vectors prepared by continuous-flow microfluidic devices
Advancements in nanotechnology have resulted in the introduction of several nonviral delivery vectors for the nontoxic, ef...
Synthesis of novel benzothiophene derivatives as protectors against cranial irradiation-induced neuroinflammation
Synthesis of novel benzothiophene derivatives as protectors against cranial irradiation-induced neuroinflammation
Aim: Cranial irradiation results in many deleterious effects to normal tissues, including neuroinflammation. There is a ne...
Multicomponent reactions as a privileged tool for multitarget-directed ligand strategies in Alzheimer’s disease therapy
Multicomponent reactions as a privileged tool for multitarget-directed ligand strategies in Alzheimer’s disease therapy
Among neurodegenerative pathologies affecting the older population, Alzheimer’s disease is the most common type of dementi...
Efficient one-pot synthesis of arylated pyrazole-fused pyran analogs: as leads to treating diabetes and Alzheimer's disease
Efficient one-pot synthesis of arylated pyrazole-fused pyran analogs: as leads to treating diabetes and Alzheimer's disease
Background: To discover novel lead molecules against diabetes, Alzheimer's disease and oxidative stress, a library of aryl...
Advances in AR-targeting chimeras: a case study of proteolysis-targeting chimeras from bench to bedside
Advances in AR-targeting chimeras: a case study of proteolysis-targeting chimeras from bench to bedside
Proteolysis-targeting chimera (PROTAC) is an emerging revolutionary technology that promotes degradation of target protein...
Virtual and augmented reality applications in medicinal chemistry
Virtual and augmented reality applications in medicinal chemistry
The author has no relevant affiliations or financial involvement with any organization or entity with a financial interest...
C3 regioselectivity: a major constraint in the drug development with imidazo[1,2-a]pyridines
C3 regioselectivity: a major constraint in the drug development with imidazo[1,2-a]pyridines
The authors duly acknowledge the research grant number TAR/2021/000129 from Department of Science and Technology-"Science ...
An interpretable machine learning model for selectivity of small molecules against homologous protein family
An interpretable machine learning model for selectivity of small molecules against homologous protein family
Aim: In the early stages of drug discovery, various experimental and computational methods are used to measure the specifi...
The key new techniques in the medicinal chemist’s toolkit to prioritize solubility during drug design
The key new techniques in the medicinal chemist’s toolkit to prioritize solubility during drug design
The authors have no relevant affiliations or financial involvement with any organization or entity with a financial intere...
Discovery of 1,5-diaryl-1,2,4-triazole derivatives as myoferlin inhibitors and their antitumor effects in pancreatic cancer
Discovery of 1,5-diaryl-1,2,4-triazole derivatives as myoferlin inhibitors and their antitumor effects in pancreatic cancer
Aim: The first inhibitor targeting myoferlin (MYOF), WJ460, bears poor metabolic stability and water solubility. Therefore...
Medicinal chemistry in big pharma has a gender diversity problem
Medicinal chemistry in big pharma has a gender diversity problem
S Macdonald holds stock at GSK. The author has no other relevant affiliations or financial involvement with any organizati...
Bacterial FtsZ inhibition by benzo[d]imidazole-2-carboxamide derivative with anti-TB activity
Bacterial FtsZ inhibition by benzo[d]imidazole-2-carboxamide derivative with anti-TB activity
Aims: The present study aimed to assess the mode of action of previously reported anti-Mycobacterium tuberculosis benzo[d]...
Long-term pharmacokinetic and pharmacological evaluations of a novel indole-benzazepinone derivative on obese Type 2 diabetes mellitus
Long-term pharmacokinetic and pharmacological evaluations of a novel indole-benzazepinone derivative on obese Type 2 diabetes mellitus
Background: Owing to the chronic nature of Type 2 diabetes mellitus, antidiabetic drugs must have long-lasting efficacy. C...
Bioinspired computational design of lankacidin derivatives for improvement in antitumor activity
Bioinspired computational design of lankacidin derivatives for improvement in antitumor activity
Background: The 17-membered polyketide, lankacidin C, exhibits considerable antitumor activity as a microtubule stabilizer...