Results 171 to 180 of about 77,925 (335)

Designing Cyclic Nitrogen‐Bridged Sulfonamides with Anti‐Cancer Activity

open access: yesChemMedChem, EarlyView.
Nitrogen bridgehead compounds, especially cyclic sulfonamides, are an abundant motif in bioactive compounds. simple methods for the synthesis of nitrogen bridgehead sulfonamides is developed and their activity against cancer cell lines is explored. The N‐bridgehead heterocyclic structure is an abundant motif in a multitude of natural products.
Benedikt W. Grau   +4 more
wiley   +1 more source

Effect of Sulfonamides on Action of Penicillin [PDF]

open access: bronze, 1946
Gladys L. Hobby, Martin H. Dawson
openalex   +1 more source

A Novel Inhibitor against the Bromodomain Protein 1 of the Malaria Pathogen Plasmodium Falciparum

open access: yesChemMedChem, EarlyView.
This article presents the development of a first‐in‐class inhibitor targeting the bromodomain protein PfBDP1 in Plasmodium falciparum, the deadliest variant of the malaria‐causing Plasmodium parasites. Through structure‐based drug design, the inhibitor interactions were characterized via X‐ray crystallography and isothermal titration calorimetry ...
Marius Amann   +10 more
wiley   +1 more source

Is Mycobacterial InhA a Suitable Target for Rational Drug Design?

open access: yesChemMedChem, EarlyView.
InhA is the target of isoniazid, a first‐line antituberculosis drug. Isoniazid is, in fact, a prodrug that needs to be activated. Researchers are trying to develop direct inhibitors of InhA. This includes the resolution of crystallographic structures. The Protein Data Bank contains over a hundred InhA structures.
Julien Rizet   +7 more
wiley   +1 more source

New Pyridobenothiazolone Derivatives Display Nanomolar Pan‐Serotype Anti‐Dengue Virus Activity

open access: yesChemMedChem, EarlyView.
A ligand‐based strategy is employed, starting from hit compound 2, to develop the C‐2 modified pyridobenzothiazolone 19 as a pan‐serotype nanomolar DENV‐1‐4 inhibitor. Investigations of the mechanism reveal the peculiar ability to abolish the infectivity of virions in a second infection.
Tommaso Felicetti   +13 more
wiley   +1 more source

Deferasirox Derivatives as Inhibitors of Kallikrein‐Related Peptidases Associated to Neurodegenerative Diseases

open access: yesChemMedChem, EarlyView.
Dysregulated proteolysis mediated by kallikrein‐related peptidases (KLKs) and iron overload are involved in the progression of neurodegenerative diseases. Deferasirox, an clinically‐approved iron chelator, and its newly synthesized derivatives have been identified as inhibitors of major central nervous system KLKs with low cytotoxicity and effective ...
Rilès Boumali   +11 more
wiley   +1 more source

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