Faculty Opinions recommendation of Development of PDE6D and CK1α Degraders through Chemical Derivatization of FPFT-2216.

Author(s):  
John Lowe
2016 ◽  
Vol 8 (15) ◽  
pp. 3023-3033 ◽  
Author(s):  
Hermes Licea-Perez ◽  
Venkatraman Junnotula ◽  
Sylvia Zohrabian ◽  
Molly Karlinsey

Carbohydrate analysis poses many analytical challenges, in terms of extraction, chromatographic separation, and detection.


Synthesis ◽  
2017 ◽  
Vol 49 (14) ◽  
pp. 3165-3170 ◽  
Author(s):  
Guoliang Chen ◽  
Xuefei Bao ◽  
Ziao Liu ◽  
Xinjie Liang ◽  
Dake Song ◽  
...  

A synthetic route to 3-formylbenzenesulfonyl chloride derivatives from the corresponding benzaldehydes has been developed. The key step in this procedure is the conversion of aldehyde bisulfite adducts to target compounds via a two-stage reaction in the presence of Na2SO4. A series of 3-formylbenzenesulfonyl chloride derivatives were prepared by this method and identified by chemical derivatization method.


Molecules ◽  
2021 ◽  
Vol 26 (15) ◽  
pp. 4488
Author(s):  
Aboagye Kwarteng Dofuor ◽  
Temitayo Samson Ademolue ◽  
Cynthia Mmalebna Amisigo ◽  
Kwaku Kyeremeh ◽  
Theresa Manful Gwira

The search for novel antitrypanosomals and the investigation into their mode of action remain crucial due to the toxicity and resistance of commercially available antitrypanosomal drugs. In this study, two novel antitrypanosomals, tortodofuordioxamide (compound 2) and tortodofuorpyramide (compound 3), were chemically derived from the natural N-alkylamide tortozanthoxylamide (compound 1) through structural modification. The chemical structures of these compounds were confirmed through spectrometric and spectroscopic analysis, and their in vitro efficacy and possible mechanisms of action were, subsequently, investigated in Trypanosoma brucei (T. brucei), one of the causative species of African trypanosomiasis (AT). The novel compounds 2 and 3 displayed significant antitrypanosomal potencies in terms of half-maximal effective concentrations (EC50) and selectivity indices (SI) (compound 1, EC50 = 7.3 μM, SI = 29.5; compound 2, EC50 = 3.2 μM, SI = 91.3; compound 3, EC50 = 4.5 μM, SI = 69.9). Microscopic analysis indicated that at the EC50 values, the compounds resulted in the coiling and clumping of parasite subpopulations without significantly affecting the normal ratio of nuclei to kinetoplasts. In contrast to the animal antitrypanosomal drug diminazene, compounds 1, 2 and 3 exhibited antioxidant absorbance properties comparable to the standard antioxidant Trolox (Trolox, 0.11 A; diminazene, 0.50 A; compound 1, 0.10 A; compound 2, 0.09 A; compound 3, 0.11 A). The analysis of growth kinetics suggested that the compounds exhibited a relatively gradual but consistent growth inhibition of T. brucei at different concentrations. The results suggest that further pharmacological optimization of compounds 2 and 3 may facilitate their development into novel AT chemotherapy.


2018 ◽  
Vol 60 (1) ◽  
pp. 121-134 ◽  
Author(s):  
Hui-Fang Ma ◽  
Fang Wei ◽  
Bang-Fu Wu ◽  
Chen Yang ◽  
Ya Xie ◽  
...  

2018 ◽  
Vol 9 (40) ◽  
pp. 7779-7786 ◽  
Author(s):  
Zhenwei Wei ◽  
Xiaochao Zhang ◽  
Jinyu Wang ◽  
Sichun Zhang ◽  
Xinrong Zhang ◽  
...  

The identification of trace components from an individual cell can require derivatization under mild conditions for successful analysis by mass spectrometry (MS).


2012 ◽  
Vol 60 (8) ◽  
pp. 931-944 ◽  
Author(s):  
Atul Awasthi ◽  
Majid Razzak ◽  
Raida Al-Kassas ◽  
Joanne Harvey ◽  
Sanjay Garg

Author(s):  
William N. Sanchez Luna ◽  
Vidiany A. Q. Santos ◽  
Sirlei D. Teixeira ◽  
Aneli M. Barbosa-Dekker ◽  
Robert F. H. Dekker ◽  
...  

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