169 research outputs found
Targeted Derivatization of Medicines via Novel C-H Functionalization
The most ubiquitous bond in pharmaceuticals rests between carbon and hydrogen and until
recently, however, the C-H bond has been ignored as a target for synthetic manipulation because
of its inherently inert nature and the significant energetic barrier associated with bond breakage.
The utilization of C-H bonds as a means of activation for desired functional groups reduces multi-
step syntheses to a single reaction, which drastically diminishes classical labor- and resource-
intensive strategies for the production of complex molecules. Additionally, structural analogs of
multifaceted, biologically active molecules can easily be obtained without having to individually
construct each member of a library of substrates from scratch. This innovative process may be
applied to potential anti-cancer drug candidates to increase their potency, effectivity, and
bioactivity by targeted functionalization, which may allow for an accelerated opportunity to
discover enhanced medicines directly from abundant precursors. The initial hypothesis for this C–
H directed reaction was derived from the radical-based mechanism of the Hofmann-Löffler-
Freytag reaction. As a way of generalizing this protocol to medicines, it has been sought to exclude
the harsh halogenation typically required for the sequential 1,5-hydrogen shift and cyclization.
Thus far, a method has been devised to directly cyclize amines to create a five-membered
pyrrolidine ring from unbiased long-chain amine substrates through the generation of iodine in
situ via mild reagents. Our research is currently focused on optimization and generalization of
this method to explore a variety of substrates that offer medicinal relevance. This development of
direct C–H activation has numerous applications in the medicinal, chemical, and biological target
elucidation and offers a rewarding potential for increased efficacy in modern synthetic strategies.No embargoAcademic Major: Biochemistr
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Some Thoughts About Regulating Religious Charity
Religious organizations appeal to members of the community all the time for financial and other support. The rationale that, by contributing financial and other resources, the community has a residual interest in how the charity itself is organized and operates will, if pushed to its maximum reach, undoubtedly fuel disputes for generations. Although I suspect that however these disputes get framed, the solutions are invariably political and practical, there is a real issue about the kinds and types of regulation to which religious charity can and should be subjected. This essay describes the background, the law, and the practical challenges that result from these contemporary clashes over the regulation of religious charity by the state
Webster v. Reproductive Health Services: A Path to Constitutional Equilibrium
This Article is intended as part of a symposium and a debate on substantive due process and the decision in Webster v. Reproductive Health Services. This writer, although here a commentator on the law, does have an opinion on the ultimate question: Roe v. Wade was wrongly decided
A Favorable Legal Environment for Voucher Programs
A pressing legal issue at the close of the millennium is the use of public tax dollars to assist parents, especially lower income parents, with the rising tuition at private schools. The idea of vouchers, as they have been commonly named, has been argued in legal circles for decades. However, the 1990s have seen a particular urgency on this issue as several states have passed legislation implementing pilot programs. This article summarizes the current state of the debate, reviews significant legal cases, and highlights the differences among individual states in their interpretation and application of the law. While maintaining that a properly designed voucher program could pass constitutional review by the U.S. Supreme Court, the author argues that broader public policy and justice issues are at stake
Shaping the Church: Overcoming the Twin Challenges of Secularization and Scandal
This article is based on The Brendan Brown Lecture at the Columbus School of Law, Catholic University of America, delivered January 15, 2003
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