Total synthesis of thiangazole, a novel inhibitor of HIV-1 from polyangium sp

Synthesis and bioassay of pyrrolyl oxazolines and thiazolines

“…A number of reliable preparative methods are known in the literature which includes cyclodehydration of carboxylic acids and b-amino alcohol, treatment of b-hydroxyamide with suitable cyclization reagents such as thionyl chloride [5], phosphorotris-(1,2,4)-triazolide [6], Mitsunobu conditions (DEAD/PPh 3 ) [7] and phosphorous mediated Appel reaction conditions [8]. In addition, thiazoline derivatives possess anti HIV-1 [9], antimitotic [10] and bioluminescent activities and have recently found applications as building blocks in pharmaceutical drug discovery [11e13]. Thiazolines have been prepared by the condensation of aminothiols with nitriles [9], esters [14], iminoethers [15] or iminotriflates [16] and also by cyclization of N-acyl-2-aminoethanols [17,18] or b-hydroxythioamides [19e21].…”

“…In addition, thiazoline derivatives possess anti HIV-1 [9], antimitotic [10] and bioluminescent activities and have recently found applications as building blocks in pharmaceutical drug discovery [11e13]. Thiazolines have been prepared by the condensation of aminothiols with nitriles [9], esters [14], iminoethers [15] or iminotriflates [16] and also by cyclization of N-acyl-2-aminoethanols [17,18] or b-hydroxythioamides [19e21]. Netropsin and distamycin are pyrrole polyamides and are naturally occurring anticancer antibiotics [22].…”

A simple and efficient synthesis of some novel thiazolidine‐4‐one derivatives

“…Several substituted thiazolidinones have been found to possess hypnotic, anesthetic, sedative, anticonvulsant, and microbiological activities [2][3][4]. Some thiazoline derivatives show interesting anti-HIV or anticancer activities and can inhibit cell division [5][6][7][8][9][10].…”

Synthesis of thiazolines by the reaction of aryl ketonitriles with cysteamine via microwave irradiation

“…More than 30 thiazoline structures have been identified from natural sources [4], particularly in cooked meat [3] and in certain exotic fruits such as litchis [5]. Some thiazolines derivatives present interesting anti-HIV [6] and anti-cancer [7,8] activities and can inhibit cell division [9].…”