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Annual Reports in Medicinal Chemistry | 1979

Chapter 13 Antiparasitic Agents

Leslie M. Werbel; Donald F. Worth; Sarah M. Weitzel

Publisher Summary This chapter presents an effective summary that has appeared on the philosophy of a pharmaceutical company toward the involvement with tropical diseases. The discussion includes a review on new experimental antimalarial drugs and a volume on “new trends in malaria chemotherapy;” major forthcoming therapeutic advances for Leishmaniasis disease entity; human and animal Trypanosomiasis as world public health problems has appeared; Trichomoniasis as the metronidazole drug, although having typoxic effect, continues to be used as very likely the best available agent for this infection. The discussion has been made enriched by the discussion on both protozoal diseases and helminth diseases that include filaria, other nematodes, and schistosomiasis. The first clinical reports using praziquantel against schistosomiasis appear promising. The pharmacokinetic behavior was dominated by rapid metabolism. No clinically relevant changes were found for any of the laboratory parameters measured in healthy volunteers given total doses as high as 7.5 mg/kg. Amoebiasis, giardiasis, toxoplasmosis, coccidiosis, and are few more have been focused in the chapter. Ionophorous antibiotics recently have been found effective in poultry and mammals. Lasalocid added to feed in a dose to produce the equivalent of about 3.0 mg/kg has been found effective in controlling clinical coccidiosis in calves. This is supported by a review of a variety of drug types.


Journal of Medicinal Chemistry | 1988

1-Substituted 7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids. New quantitative structure activity relationships at N1 for the quinolone antibacterials

John M. Domagala; Carl L. Heifetz; Marland P. Hutt; Thomas F. Mich; Jeffry B. Nichols; Marjorie Solomon; Donald F. Worth


Journal of Medicinal Chemistry | 1987

Synthesis and structure-activity relationships of pyrazolo[4,3-d]pyrimidin-7-ones as adenosine receptor antagonists.

Harriet W. Hamilton; Daniel F. Ortwine; Donald F. Worth; James A. Bristol


Journal of Medicinal Chemistry | 1986

Synthesis, antimalarial activity, and quantitative structure-activity relationships of tebuquine and a series of related 5-[(7-chloro-4-quinolinyl)amino]-3-[(alkylamino)methyl] [1,1'-biphenyl]-2-ols and N omega-oxides.

Leslie M. Werbel; P. Dan Cook; Edward F. Elslager; Jocelyn Hung; Judith L. Johnson; Stephen J. Kesten; Dennis Joseph Mcnamara; Daniel F. Ortwine; Donald F. Worth


Journal of Medicinal Chemistry | 1985

Synthesis of xanthines as adenosine antagonists, a practical quantitative structure-activity relationship application.

Harriet W. Hamilton; Daniel F. Ortwine; Donald F. Worth; Edward W. Badger; James A. Bristol; Robert F. Bruns; Stephen J. Haleen; Robert P. Steffen


Journal of Medicinal Chemistry | 1972

Antimalarial drugs. 25. Folate antagonists. 3. 2,4-Diamino-6-(heterocyclic)quinazolines, a novel class of antimetabolites with potent antimalarial and antibacterial activity

Edward F. Elslager; Jane Clarke; Leslie M. Werbel; Donald F. Worth; John Davoll


Journal of Medicinal Chemistry | 1986

Basically substituted ellipticine analogues as potential antitumor agents

Leslie M. Werbel; Mario M. Angelo; David W. Fry; Donald F. Worth


Journal of Medicinal Chemistry | 1969

Respository drugs. IV. 4',4'''-Sulfonylbisacetanilide (Acedapsone, DADDS) and related sulfanilylanilides with prolonged antimalarial and antileprotic action.

Edward F. Elslager; Zoe B. Gavrilis; Annette A. Phillips; Donald F. Worth


Journal of Heterocyclic Chemistry | 1970

1,4-Cyeloaddition reactions. IV. preparation of Cyclopenta[g]furo[3,2-c]quinolines, Cyclopenta- [f]furo[3,2-c]quinolines, Benzo[H]furo[3,2-c]quinolines, and Furo- [3,2-c]indeno[1,7-gh] quinolines from 2,3-Dihydro-5-methylfuran and schiff bases †

Donald F. Worth; S. C. Perricone; Edward F. Elslager


Journal of Medicinal Chemistry | 1978

Antimalarial drugs. 39. Folate antagonists. 13. 2,4-Diamino-6-[(.alpha.,.alpha.,.alpha.-trifluoro-m-tolyl)thio]quinazoline and related 2,4-diamino-6-[(phenyl- and naphthyl)thio]quinazolines, a unique class of antimetabolites with extraordinary antimalarial and antibacterial effects

Edward F. Elslager; Patricia Jacob; Judith L. Johnson; Leslie M. Werbel; Donald F. Worth; Leo Rane

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