SYNTHESIS AND ANTIBACTERIAL ACTIVITY OF NEW SULFONAMIDE ISOXAZOLO[5,4-b]PYRIDINE DERIVATIVES.

A series of novel sulfonamide isoxazolo[5,4-b]pyridines were synthesized. The substrates for their synthesis were 3-aminoisoxazolo[5,4-b]pyridine and selected aryl sulfonic chlorides, chlorosulfonic acid and selected amines. Reactions were carried out using the classical and microwave methods.

The synthesis of 3,5,6,7-tetrasubstituted isoxazolo[4,5-b]pyridines and an evaluation of their in vitro antiproliferative activity.

Background: Derivatives of isoxazolopyridines exhibit diverse biological activity. One method of synthesizing isoxazolo[4,5-b]pyridines is Friedlander condensation.

Objectives: To establish the conditions necessary for conventional and microwave synthesis of new 3,5,6,7-tetrasubstituted isoxazolo[4,5-b]pyridines and their antiproliferative activity.

Synthesis and antiproliferative activity in vitro of new 2-, 3- or 4-substituted pyrido[2',3':3,4]pyrazolo[1, 5-a]pyrimidines.

The synthesis of several new 2-, 3- or 4-substituted pyrido[2',3':3,4]pyrazolo[1,5-a]pyrimidines is described. The obtained compounds were tested for their antiproliferative activity in vitro. Two of them: 3-chloro-2-methylpyrido[2',3':3,4]pyrazolo[1,5-a] pyrimidin-4-one [X] and 2,3-cyclopentylpyrido [2',3':3,4] pyrazole[1,5-a]pyrimidin-4-one [XII] revealed weak cytotoxic activity against the cells of human bladder cancer cell lines: LoVo, MCF-7, MES-SA and HCTV29T.

Synthesis and antiproliferative activity in vitro of new 3-substituted aminoisoxazolo[5,4-b]pyridines.

The synthesis of 3-aminoisoxazolo[5,4-b]pyridine [III] and of several new 3-substituted aminoisoxazolo[5,4-b]pyridines is described. 3-Aminoisoxazlo[5,4-b]pyridine [III] was subjected to reactions with the acid halides and substituted aromatic aldehydes, leading to the production of the corresponding amides IV-VII, IX, XI-XVI and new tricyclic pyridoisoxazolopyrimidine VIII and Schiff bases XX-XXIV. 4-Chlorobutyroamide IX cyclized into 3-(pyrrolidinon-1-yl)isoxazolo[5,4-b]pyridine [X].

Synthesis and antiproliferative activity in vitro of new 3-substituted aminopyrazolo[3,4-b]pyridines.

The synthesis of several new 3-substituted aminopyrazolo[3,4-b]pyridines is described. The obtained compounds were tested for their antiproliferative activity in vitro. Two of them: 3-chloroacetylaminopyrazolo[3,4-b]pyridine [II] and 3-(2-bromopropionyl-amino)pyrazolo[3.