Annual reports in medicinal chemistry, 1969

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Ed felt a strong responsibility to be active in his professional associations. He served first as vice-chair and chair of the long-range planning committee of the Division of Medicinal Chemistry of the American Chemical Society and became chair of the Division in Because of his extraordinary talents as a researcher and teacher, Ed was in great demand as a lecturer throughout the world at conferences and universities and as a consultant at industrial laboratories.

In addition, he spent many years as a member of National Institutes of Health study sections and panels. Furthermore, he presented numerous lectures at universities and industrial laboratories all over the world.

  • Novel Approaches in Biosensors and Rapid Diagnostic Assays: 43rd OHOLO Conference Eilat, Israel, October 10–14, 1999;
  • Annual Reports in Medicinal Chemistry, Volume 42!
  • The year 1969;
  • Introduction to Vertex Operator Algebras and Their Representations?

His comprehensive knowledge of medicinal chemistry also made him attractive as a consultant to industry. Ed died unexpectedly on Sunday, July 14, He was not quite forty-nine years old. His qualities as a teacher, a scientist and a human being inspired generations of students and affected all who knew him. His influence will not soon be forgotten. The atmosphere of cooperation and goodwill which Ed fostered at KU will remain as his greatest memorial. Clarine Feir was born in in St. Louis, Missouri. She earned a bachelor's degree at The Ohio State University. She and Ed were married in while Ed was in graduate school.

They were second parents to all the graduate students and postdoctoral fellows in the department. They entertained often in their home shared with Hagen, their handsome German Shepherd , and Clare accompanied Ed on most of his travels. She obtained a law degree at KU in and practiced law in Lawrence and Baldwin City where she also was on the faculty at Baker University. Smissman Memorial Fund. We co-engineer novel ligand-receptor pairs to obtain agents with unique, orthogonal specificity, useful in gene therapy and in separating genomic and non-genomic signaling pathways. We develop novel spectroscopic methods to analyze receptor structure, conformation, and dynamics, and receptor-coregulator interactions, and how these are affected by ligand structure.

We are using chemical and molecular biological methods to fabricate protein microarrays through which receptor ligand binding and coactivator interactions can be assayed in a quantitative and high throughput manner. Based on our analysis of the key structural features important for the receptor binding and activity of steroid hormones and anti-hormones, we have undertaken a combinatorial approach to discover novel non-steroidal hormonal agents. These compounds have important receptor subtype and tissue selectivity that could be useful for menopausal hormone replacement and breast and prostate cancer prevention and therapy.

A novel approach to the diagnosis of breast and prostate cancer is the use of gamma- and positron-emitting steroids to label the receptors in these tumors. We are designing hormones labeled with the positron-emitting radionuclide fluorine The designed steroids must maximize specific to nonspecific binding and control the level of metabolism. Also, because F has a half-life of only min, synthetic methods that are rapid, convenient, and efficient are required.

We are also working to incorporate the radioactive metals technetiumm and gallium into structural mimics of steroids while maintaining high receptor binding and good bio-distribution properties. Skip to main content. Menu Admissions. Give Now. John A. Mathews Ave. Urbana, IL Edit Your Profile. Research Professor of Chemistry. Biography Professor John A.

Research Description The action of steroid hormones is mediated by their binding to specific, high-affinity binding proteins that are found in target tissues only at very low concentrations and are a challenge to isolate and purify. Novel Ligands and Dendrimers. Receptor Structure and Protein Microarrays. Combinatorial Chemistry. Selected Publications. Journal Articles Fanning, S.

Mayne, V. Fluoroquinolones: The most efficacious of the fluoroquinolones against M. Combination therapy with MXF seems to be as effective as current standard drug combinations Oxazolidinones: Oxazolidinones are a new class of compounds inhibits protein synthesis at an early stage by binding to 23S rRNA of the 50S ribosomal subunit. Linezolid is the first oxazolidinone to be developed and approved by the FDA to treat single- or multiple-resistant Gram-positive bacterial infections Concerning the use of this class against tuberculosis, many active compounds were found 73, 74, However; the long term use of linezolid 26 may be plagued with forbidding side effects including anemia and peripheral neuropathy 76, Drug classes with novel mechanisms of action undergoing clinical evaluation for a TB indication:.

PA 21 is highly active with MIC as low as 0. The mechanism of action of PA is two-fold, as it inhibits M. PA is, in fact, a prodrug that is metabolized by M. OPC 22 exhibits excellent in vitro activity against drug-susceptible and resistant M. It inhibit the synthesis of mycolic acid at the stage of methoxy-mycolic and the keto-mycolic acid syntheses like INH Modification of diarylquinolines led to the identification of diarylquinoline R 23 also known as J compound and TMC as the most potent, with minimum inhibitory concentration MIC of 0.

Itacts by blocking the function of an essential membrane-bound enzyme that makes adenosine triphosphate ATP.

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Although biochemical confirmation is now required, it is possible that the drug impedes assembly of the mobile disk or interferes with its rotational properties, leading to inadequate synthesis of ATP. This unique mechanism of action offers great potential as there is little similarity between the mycobacterial and human proteins encoded by the atpE gene that codes for the c subunit of ATP synthase, which has been identified as the specific target of TMC A number of mutations I66Mand A63P have been identified in the c subunit of TMCresistant strains 87, 88 near the glutamate residue E61, which is involved in proton transport and is necessary for the synthesis of ATP Fig.

Molecular modelling studies of M. Normally, the sidechain of Arg in the a-subunit adopts an extended conformation that reaches towards Glu in the c-subunit to transfer a proton. It is believed that the molecular mechanism of action of TMC is to mimic the side chain of Arg TMC adopts a folded conformation in solution before binding owing to intramolecular hydrogen bonding The lack of a cavity large enough to accommodate the bulky dimethyl amino group of TMC prevents the necessary rotation required for proton transfer, blocking ATP production. Several potent quinoline-based anti-TB compounds, bearing an isoxazole containing side-chain have been identified.

The most potent compounds, 24 and 25 , exhibited submicromolar activity against the replicating bacteria R-TB , with minimum inhibitory concentrations MICs of 0. Also, 24 and 25 were shown to retain their anti-TB activity against rifampin, isoniazid, and streptomycin resistant M. A new series of 20 quinoline derivatives possessing triazolo, ureido and thioureido substituents was synthesized. Molecular modelling and docking studies on well-known diarylquinoline antitubercular drug R 23 showed the presence of phenyl, naphthyl and halogen moieties seems critical Ethylene diamines: From the structure of ethambutol 9 , a modern chemical approach was undertaken leading to the synthesis of many chemical libraries of diaminated analogues.

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Moreover, the favorable pharmacological properties of compound 32 95 as well as a synergistic effect with other antituberculosis drugs 96 should lead to clinical trials which were scheduled to start in The exact mechanism of action of 34 is not known, although it is believed to target cell wall synthesis in a different manner to EMB as SQ is active against EMB-resistant strains, suggesting the existence of a different specific target or activation pathway. The TB drugs currently in use were developed 40 years ago and there is a great need for new new, shorter treatment regimens. In the long term, the availability of more new drugs should play an important role in reducing the global TB burden.

Current research involves finding better and more effective drugs that reduce time of treatment, reduce toxicity associated with drugs and provide backup measures in case of drug resistance. The approaches include: chemical modification of existing drugs such as rifampin, fluoroquinolones and macrolides ; the identification of drug targets such as persistence genes using microarray analysis and molecular biology tools; structure based drug design and in vitro and in vivo screening to identify new drugs; evaluation of novel drug combinations; and the order of drugs given in treatment.

This review has summarized the global disease burden of TB, existing drugs, drugs under clinical trials and their possible targets. Promising leading chemical entities has also been addressed. Int J Pharm Sci Res ; 4 6 ; Article Information Sr No: 7.

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It is orally active and exhibits bactereostatic action on the resting bacilli and has very low MICs 0. INH is available in tablets, syrup and injectable forms given intramuscularly and intravenously. World Health Organization. Stop TB annual report. World Health Organization, Geneva, Switzerland.


Confronting the scientific obstacles to global control of tuberculosis. J Clin Invest ; De Souza MVN. Recent Pat. Anti-Infect Drug Discov ; 1: Moszynski P.

Book Series: Annual Reports in Medicinal Chemistry

WHO launches plan to fight drug resistant tuberculosis. BMJ ; — Spigelman MK. New tuberculosis therapeutics: a growing pipeline. Novel targets for tuberculosis drug discovery. The envelope of mycobacteria.

Annu Rev Biochem ; Deciphering the biology of Mycobacterium tuberculosis from the complete genome sequence. Nature ; Tomasz A. Multiple-antibiotic-resistant pathogenic bacteria — a report on the Rockefeller University Workshop. New Eng J Med ; Courvalin P. J Antimicrob Chemother ; Webb V, Davies J. Antibiotic preparations contain DNA: a source of drug resistance genes? Agents Chemother ; Center for disease Control, Emergence of Mycobacterium tuberculosis with extensive resistance to second-line drugs—Worldwide. MMWR weekly ; Marris E. Marine natural products: drugs from the deep.

Kaufmann SH.