3-cyanoacetylindole as a building block in the synthesis of nonfused and fused pyridine, pyrimidine, diazepine and pyranone derivatives

The reaction of 3-cyanoacctylindole I with trichloroacetonitrile afforded trichloroll1cthylpropen-1-one derivative 3 which upon the reaction with an excess of trichloroacetonitrilc yielded the ditrichlorome-thylpyrimidine derivative 5. It was converted to a variety of pyrazolo 7, dihydrazino 9. and isoxazolo pyrimidine II derivatives. The enaminonitrile 2 was used as a substrate to form the pyridine 13, 14, 16, diazepine 20 and pyranone 22 as well as 1, 2, 4-triazolo-25. 1, 2, 3, 4-tetrazolo-27, and benzimidazolo-pyrimidine 29 derivatives

New furobenzopyrone analogues as photochemotherapeutic agents

The present work described the synthesis and investigation of some new linear and angular furobenzo-alpha-pyrone analogues as photochemotherapeutic agents with the aim of producing compounds with high activity and reduced toxicity. Besides, 3 D-models have been simulated to study the effect of peripheral substituents on the photosensitizing activity of the new furobenzo-alpha-pyrone

New furobensopyrones as possible agents for the photochemotherapy of psoriasis with expected monofunctional mode for DNA

This work involved the synthesis of linear furobenzopyrone analogs as monofunctional photochemotherapeutic agents, aiming to obtain compounds with increased activity and reduced toxicity. A rough investigation was carried out on the conformation of a new bulky substituent like phenyl group in the furobenzopyrone system to produce compounds that could react with DNA in a monofunctional sense, therefore reducing or eliminating skin phototoxicity or the risk of skin cancer and, at the same time, maintaining the same selectivity of action as psoralen, [linear furobenzopyrone]. So, they have synthesized linear furobenzopyrone derivatives [3a-c and 8a1-6], in which methyl and phenyl groups were systematically varied at the 2, 3, 5, and 9 positions. Preliminary screening for the photosensitizing activity of some of the new analogs have revealed that compound [8a1] is more active as photosensitizer than xanthotoxin [reference], while 3b, c and 8a4-6 are less active. In addition, 3a and 8a2-3 showed no photosensitizing activity

Novel benzo-O-pyrone analogues as antimicrobial agents

New cyclic analogues derived from 8-allyl-7-hydroxy-4- methyl-2H-1-benzopyran-2-one have been synthesized. Ten of the new compounds were screened for antibacterial as well as antifungal activity. The results were presented