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1.
J Hand Surg Glob Online ; 6(1): 137-139, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-38313609

RESUMO

Extensor tendon entrapment in the presence of distal radius fracture is a known but relatively uncommon complication. Single tendon or entire compartment entrapment has been described through the literature in youths and adults. However these findings generally are limited to a certain age demographic or are found on advanced imaging but are unable to be confirmed intraoperatively. We describe to our knowledge the first known description of second extensor compartment entrapment in an adult seen on computerized tomography scan and confirmed intraoperatively.

2.
Bioorg Med Chem ; 28(24): 115816, 2020 12 15.
Artigo em Inglês | MEDLINE | ID: mdl-33181479

RESUMO

CADA compounds selectively down-modulate human cell-surface CD4 protein and are of interest as HIV entry inhibitors and as drugs for asthma, rheumatoid arthritis, diabetes and some cancers. Postulating that fusing a pyridine ring bearing hydrophobic substituents into the macrocyclic scaffold of CADA compounds may lead to potent compounds with improved properties, 17 macrocycles were synthesized, 14 with 12-membered rings having an isobutylene head group, two arenesulfonyl side arms, and fused pyridine rings bearing a para substituent. The analogs display a wide range of CD4 down-modulating and anti-HIV potencies, including some with greater potency than CADA, proving that a highly basic nitrogen atom in the 12-membered ring is not required for potency and that hydrophobic substituents enhance potency of pyridine-fused CADA compounds. Cytotoxicities of the new compounds compared favorably with those of CADA, showing that incorporation of a pyridine ring into the macrocyclic scaffold can produce selective compounds for potently down-modulating proteins of medicinal interest.


Assuntos
Fármacos Anti-HIV/síntese química , Antígenos CD4/metabolismo , Compostos Heterocíclicos/química , Piridinas/química , Animais , Fármacos Anti-HIV/química , Fármacos Anti-HIV/farmacologia , Antígenos CD4/genética , Células CHO , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Cricetinae , Cricetulus , Regulação para Baixo/efeitos dos fármacos , HIV-1/metabolismo , Compostos Heterocíclicos/síntese química , Compostos Heterocíclicos/farmacologia , Humanos , Solubilidade , Relação Estrutura-Atividade , Sulfonamidas/síntese química , Sulfonamidas/química , Sulfonamidas/farmacologia , Termodinâmica , Replicação Viral/efeitos dos fármacos
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