- Design and synthesis of 1,3,5-trisubstituted 1,2,4-triazoles as CYP enzyme inhibitors
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A series of 1,3,5-trisubstituted 1,2,4-triazoles was designed and synthesized as potential inhibitors of ste-roidogenic CYP enzymes. The 1,2,4-triazole is part of the core structure fixing the geometry of the substances. A pyridine moiety was introduced as heme-binder. The target compounds were synthesized in two to four steps using silver carbonate mediated ring closure and Suzuki cross coupling reaction as key synthetic transformations. Biological testing of the synthesized compounds for the inhibition of the most important steroidogenic CYPs revealed compounds 29a and 30 as moderate inhibitors of aldo-sterone synthase (CYP11B2).
- Al-Soud, Yaseen A.,Heydel, Michael,Hartmann, Rolf W.
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p. 6372 - 6375
(2012/01/02)
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- Cyclization of 1,2,4-triazenes to 1,2,4-triazoles using oxidizing reagents - NaClO, Ca(ClO)2, Dess-Martin periodinane and Ley's TPAP/NMO
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A simple and efficient approach to 1,3,5-trisubstituted 1,2,4-triazoles via cyclization of 1,2,4-triazenes employing commonly used oxidizing agents such as NaClO, Ca(ClO)2, Dess-Martin periodinane and Ley's oxidizing agent (TPAP/NMO) is described. The reaction proceeds under mild conditions and is compatible with various functional groups. Extension of this approach to prepare triazoles on solid support has also been investigated.
- Paulvannan,Hale, Ron,Sedehi, Daniel,Chen, Tao
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p. 9677 - 9682
(2007/10/03)
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- An improved synthesis of 1,2,4-triazoles using Ag2CO3
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An improved synthesis of 1,3,5-trisubstituted 1,2,4-triazoles via Ag2CO3 mediated cyclization of triazenes has been developed. This approach is flexible and compatible with a wide range of functional groups. The reaction was complete within 3 h and the products were isolated in moderate to high yields. The influence of the β-substituents of the amines on the triazole formation was also studied. (C) 2000 Elsevier Science Ltd.
- Paulvannan,Chen, Tao,Hale, Ron
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p. 8071 - 8076
(2007/10/03)
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