Investigation of chalcogen bioisosteric replacement in a series of heterocyclic inhibitors of tryptophan 2,3-Dioxygenase

2021 ◽  
pp. 113892
Author(s):  
Arina Kozlova ◽  
Léopold Thabault ◽  
Nicolas Dauguet ◽  
Marine Deskeuvre ◽  
Vincent Stroobant ◽  
...  
Keyword(s):  
Bioisosteric Replacement

scholarly journals Design, Synthesis and Anticandidal Evaluation of Indazole and Pyrazole Derivatives

2021 ◽  
Vol 14 (3) ◽  
pp. 176
Author(s):  
Karen Rodríguez-Villar ◽  
Alicia Hernández-Campos ◽  
Lilián Yépez-Mulia ◽  
Teresita del Rosario Sainz-Espuñes ◽  
Olivia Soria-Arteche ◽  
...  
Keyword(s):  
Bloodstream Infections ◽  
Antifungal Drugs ◽  
Pyrazole Derivatives ◽  
Design Synthesis ◽  
Bioisosteric Replacement ◽  
Current Therapies ◽  
Anticandidal Activity ◽  
Resistant Strains ◽  
A Priority

Candidiasis, caused by yeasts of the genus Candida, is the second cause of superficial and mucosal infections and the fourth cause of bloodstream infections. Although some antifungal drugs to treat candidiasis are available, resistant strains to current therapies are emerging. Therefore, the search for new candicidal compounds is certainly a priority. In this regard, a series of indazole and pyrazole derivatives were designed in this work, employing bioisosteric replacement, homologation, and molecular simplification as new anticandidal agents. Compounds were synthesized and evaluated against C. albicans, C. glabrata, and C. tropicalis strains. The series of 3-phenyl-1H-indazole moiety (10a–i) demonstrated to have the best broad anticandidal activity. Particularly, compound 10g, with N,N-diethylcarboxamide substituent, was the most active against C. albicans and both miconazole susceptible and resistant C. glabrata species. Therefore, the 3-phenyl-1H-indazole scaffold represents an opportunity for the development of new anticandidal agents with a new chemotype.

scholarly journals Potent SARS-CoV-2 mRNA Cap Methyltransferase Inhibitors by Bioisosteric Replacement of Methionine in SAM Cosubstrate

2021 ◽  
Author(s):  
Olga Bobiļeva ◽  
Raitis Bobrovs ◽  
Iveta Kaņepe ◽  
Liene Patetko ◽  
Gints Kalniņš ◽  
...  
Keyword(s):  
Bioisosteric Replacement

Application of the Pentafluorosulfanyl Group as a Bioisosteric Replacement

ChemMedChem ◽  
2017 ◽  
Vol 12 (18) ◽  
pp. 1481-1490 ◽  
Author(s):  
Munia F. Sowaileh ◽  
Robert A. Hazlitt ◽  
David A. Colby
Keyword(s):  
Bioisosteric Replacement

scholarly journals The Trifluoromethyl Group as a Bioisosteric Replacement of the Aliphatic Nitro Group in CB1 Receptor Positive Allosteric Modulators

2019 ◽  
Vol 62 (10) ◽  
pp. 5049-5062 ◽  
Author(s):  
Chih-Chung Tseng ◽  
Gemma Baillie ◽  
Giulia Donvito ◽  
Mohammed A. Mustafa ◽  
Sophie E. Juola ◽  
...  
Keyword(s):  
Nitro Group ◽  
Cb1 Receptor ◽  
Allosteric Modulators ◽  
Trifluoromethyl Group ◽  
Bioisosteric Replacement ◽  
Positive Allosteric Modulators

scholarly journals Bioisosteric replacement of central 1,2,4-oxadiazole ring of high affinity CB2 ligands by regioisomeric 1,3,4-oxadiazole ring

MedChemComm ◽  
2017 ◽  
Vol 8 (8) ◽  
pp. 1697-1705 ◽  
Author(s):  
Dominik Heimann ◽  
Corinna Lueg ◽  
Henk de Vries ◽  
Bastian Frehland ◽  
Dirk Schepmann ◽  
...  
Keyword(s):  
High Affinity ◽  
Bioisosteric Replacement ◽  
Pharmacokinetic Properties

Three pairs of regioisomeric 1,2,4- and 1,3,4-oxadiazoles were synthesized as selective CB2 ligands. Although the 1,3,4-oxadiazoles should have better physicochemical and pharmacokinetic properties, their CB2 affinity was reduced.

Identification of potent type I MetAPs inhibitors by simple bioisosteric replacement. Part 2: SAR studies of 5-heteroalkyl substituted TCAT derivatives

2005 ◽  
Vol 15 (18) ◽  
pp. 4130-4135 ◽  
Author(s):  
Yong-Mei Cui ◽  
Qing-Qing Huang ◽  
Jie Xu ◽  
Ling-Ling Chen ◽  
Jing-Ya Li ◽  
...  
Keyword(s):  
Type I ◽  
Sar Studies ◽  
Bioisosteric Replacement ◽  
Replacement Part

Inhibitors of acyl-CoA:cholesterol acyltransferase (ACAT). 2. Modification of fatty acid anilide ACAT inhibitors: bioisosteric replacement of the amide bond

1993 ◽  
Vol 36 (11) ◽  
pp. 1662-1668 ◽  
Author(s):  
W. Howard Roark ◽  
Bruce D. Roth ◽  
Ann Holmes ◽  
Bharat K. Trivedi ◽  
Karen A. Kieft ◽  
...  
Keyword(s):  
Fatty Acid ◽  
Amide Bond ◽  
Bioisosteric Replacement

scholarly journals Metallo-β-lactamase inhibitors by bioisosteric replacement: Preparation, activity and binding

2017 ◽  
Vol 135 ◽  
pp. 159-173 ◽  
Author(s):  
Susann Skagseth ◽  
Sundus Akhter ◽  
Marianne H. Paulsen ◽  
Zeeshan Muhammad ◽  
Silje Lauksund ◽  
...  
Keyword(s):  
Bioisosteric Replacement
Sign in / Sign up

Export Citation Format

Share Document