Syntheses and anti-HIV and human cluster of differentiation 4 (CD4) down-modulating potencies of pyridine-fused cyclotriazadisulfonamide (CADA) compounds.

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.

Second Extensor Compartment Entrapment in an Adult Following Distal Radius Fracture.

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.

Episiotomy-assisted Incarcerated Femoral Nail Removal: Technical Note.

Introduction: Incarceration of intramedullary nails can pose a significant challenge. There are many reported techniques of nail removal, but when these fail, it can be difficult to determine how to proceed. Here, it is shown that a proximal femoral episiotomy can be used with great effect. Case Report: 64-year-old male developed hip arthritis. The patient had a solid antegrade femoral nail placed 22 years ago that required removal for a hip arthroplasty. A proximal femoral episiotomy-assisted approach was used with good results and patient outcome. Conclusion: There are several well described techniques to assist with incarcerated nail removal that all trauma surgeons should be familiar with. Proximal femoral episiotomy is a useful technique, every surgeon should have in their arsenal.