[reaction: see text] A short-step synthesis of versatile chiral building blocks for triazole antifungal agents such as ZD0870 and Sch45450 was developed via catalytic enantioselective cyanosilylation of electron-deficient ketones as the key step. High enantioselectivity was produced using a catalyst prepared from Gd(HMDS)(3) and ligand 5 in a 2:3 ratio. This new catalyst preparation method was superior to the previous method using Gd(O(i)Pr)(3) as a metal source. A rationale for the difference is proposed on the basis of structural studies of the catalyst complexes using ESI-MS.

01 May 2001·Journal of Antimicrobial Chemotherapy

Termination of development of D0870

Letter

Author: Williams, Keith J. ; Denning, David W.

01 Jul 2000·Journal of Antimicrobial ChemotherapyQ2 · MEDICINE

In vivo activity of the bis-triazole D0870 against drug-susceptible and drug-resistant strains of the protozoan parasite Trypanosoma cruzi

Q2 · MEDICINE

Article

Author: Molina, Judith ; Brener, Zigman ; Romanha, Alvaro J. ; Urbina, Julio A.

We report the in vivo activity of the bis-triazole derivative D0870 against a variety of strains of Trypanosoma cruzi, the causative agent of Chagas' disease, including nitroimidazole/nitrofuran-resistant strains. In both acute and chronic murine models of the disease, treatment with D0870 at < or = 10 mg/kg on alternate days for a total of 20 doses provided 60-100% protection against death, regardless of the drug sensitivity of the infecting strain. In the acute model we obtained 70-100% parasitological cure in seven of the nine strains tested, including one intermediate and two highly drug-resistant strains. D0870 was able to cure 30-45% of animals chronically infected with various strains, including those harbouring the Colombiana strain, among which no cures were obtained with benznidazole. We also found that the anti-T. cruzi activity of D0870 is largely retained even if the hosts are immunosuppressed.

100 Deals associated with ICI-D0870

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Indication	Highest Phase	Country/Location	Organization	Date
Chagas Disease	Phase 2	VE	-	-
Mycoses	Phase 2	DE	-	-
Mycoses	Phase 2	NL	-	-
Mycoses	Phase 2	-	AstraZeneca Pharmaceuticals Co. Ltd.	-
Mycoses	Phase 2	JP	Mochida Pharmaceutical Co., Ltd.	-
Mycoses	Phase 2	BE	-	-
Mycoses	Phase 2	US	-	-
Mycoses	Phase 2	GB	AstraZeneca PLC	-
Mycoses	Phase 2	FR	-	-

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