A partial proteolysis targeting chimera (PROTAC) library bearing achiral phenyl dihydrouracil cereblon ligands is prepared. It is then applied to the rapid development of a full PROTAC library targeting Bruton's tyrosine kinase, which can be directly used for screening.
Chelsi M. Almodóvar‐Rivera +5 more
wiley +1 more source
Synthesis and anti-Aphid Aphis gossypii (Glover) activity of some new quinoline derivatives [PDF]
A series of quinoline derivatives have been elaborated fromreaction of 2-(m- and p-acetylanilino)-quinolines 6a-b withaldehydes under Claisen-Schmidt conditions followed by cyclization with phenyl hydrazine and hydroxylamine.
El Kafafy, Abdel Kader +3 more
core
Hypothalamic Astrocytes Exhibit Glycolytic Features Making Them Prone for Glucose Sensing
Main Points Hypothalamic astrocytes versus cortical astrocytes: are more glycolytic due to high Pkm2, Glut1 and Mct4 expression do not exhibit glutamate‐induced glycolysis detect glucose concentration variations via an AMPK sensor with altered lactate production.
Sarah Geller +11 more
wiley +1 more source
Some semicarbazide derivatives and their antimicrobial activity
Various semicarbazides and thiosemicarbazides (1-5) and their cyclised products, triazoles, oxadiazoles and thiadiazoles (6-9) have been reported to possess antibacterial, antitubercular and antifungal activities. Based on these findings it w as of interest to prepare some new arylsemicarbazide and arylthiosemicarbazide derivatives and to evaluate ...
F. Abd EL-AZEEM +2 more
openaire +2 more sources
In vitro antimicrobial activity and DNA cleavage studies: synthesis and characterization of novel M(II) complexes with tridentate [ONO] donor Schiff base ligand derived from phenylpropane hydrazide [PDF]
Three new ternary complexes of general formulation [M(L)n] (1-3), where L = N'-(5-chloro-2-hydroxybenzylidine)-3-phenylpropane hydrazide; n = 2; M = Cu, Ni, Zn, complexes are synthesized, characterized by various physicochem.
Aradhya, S.M. +4 more
core
Batch Synthesis of Primaquine Diphosphate Anti‐Malarial Drug
According to the WHO, a child under the age of five dies every 2 minutes from malaria in Africa. It is therefore paramount that access and availability of anti‐malarial drugs must be improved. We report a process for the synthesis of Primaquine Diphosphate, where key intermediates were obtained in a much shorter reaction time compared to processes ...
Faith M. Akwi +2 more
wiley +1 more source
Synthesis of Novel Dihydropyridine‐Iminium Salts Containing a Selenazine Core
An efficient method to develop novel dihydropyrido[3,2‐e][1,3]selenazines iminium salts. A comparative study of the key reagent selenourea towards thiourea and urea was carried out to assess the contribution of chalcogen to the pathway. DFT (density functional theory) calculations have predicted the optimized minimum energy structure for the hybrid ...
Reinier Lemos +6 more
wiley +1 more source
Antiviral activity of organic molecules having sulfonamide moiety: An insight of recent research [PDF]
Sulfonamide derivatives are well known for their antibacterial activity as manifested by ‘Sulfa Drugs’, for example, sulfamethoxazole etc. In addition, they are associated with a large number of pharmacological activities such as anti-microbial, anti ...
Aslam, S. +4 more
core +1 more source
A step-economical multicomponent synthesis of 3D-shaped aza-diketopiperazines and their drug-like chemical space analysis [PDF]
A rapid and atom economical multicomponent synthesis of complex aza-diketopiperazines (aza-DKPs) driven by Rh(I)-catalyzed hydroformylation of alkenylsemicarbazides is described.
Bonnet, D. (Dominique) +6 more
core +2 more sources
A pH‐programmable site‐selective cysteine modification in peptides is reported using a triazine–thiol exchange, termed TriTEx. At acidic pH, internal cysteines are targeted while preserving N‐terminal sites; at neutral pH, N‐terminal cysteines are selectively modified via an irreversible S–N shift.
Katerina Gavriel +5 more
wiley +1 more source

