Synthesis and antifolate activity of 2,4‐diamino‐5,6,7,8‐tetrahydropyrido[4,3‐d]pyrimidine analogues of trimetrexate and piritrexim

Abstract

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Identification of Cryptosporidium parvum Dihydrofolate Reductase Inhibitors by Complementation in Saccharomyces cerevisiae

“…These lipophilic DHFR inhibitors are assumed to cross the plasma membrane by passive or facilitated diffusion and, therefore, to obviate drug susceptibility and resistance problems associated with carrier-or receptor-mediated folate transport mechanisms (7). Many of these compounds have previously been assayed against P. carinii DHFR and T. gondii DHFR-TS in vitro (48,49,(51)(52)(53)(54)(55)(56). For example, the IC 50 of PY875 against the P. carinii DHFR enzyme in vitro was ϳ7 M (51), suggesting that PY875 might also inhibit the growth of Pc-yeast; Table 6 shows this to indeed be the case.…”

An Efficient Synthesis of Pyrido[2,3-<i>d</i>]pyrimidine Derivatives via One-Pot Three-Component Reaction in Aqueous Media

“…The importance of pyridopyrimidines as biologically active compounds includes their use as antibacterial [1][2][3], antiallergic [4], antitumor [2,3] antifolate [5], tyrosine kinase [6], antimicroibial [7], calcium channel antagonists [8], antibacterial [9][10][11][12], anti-inflammatory, analgesic [13], antihypertensive [14], antileishmanial [15], tuber-culostatic [16], anticonvulsants [17], diuretic, potassiumsparing [18], and antiaggressive activities [19]. The need to reduce the amount of toxic waste and byproduct arising from chemical processes requires increasing emphasis on the use of less toxic and environmentally compatible materials in the design of new synthetic methods.…”

New strategy for the synthesis of novel spiro[indoline-3,2'-thiazolo[5,4-e]pyrimido[1,2-a]pyrimidine] derivatives

“…[4][5] Spiro[indole-thiazolidinones] are known to possess various biological activities including antiinflammatory, 6 antimicrobial, 7 bacteriostatic, 8 anticonvulsant 9 and used as antifungal agents. 10 In addition, the synthesis of pyridopyrimidine and their derivatives is of high interest in organic chemistry due to their potential biological and pharmacological activities such as antiviral, [11][12] antiinflammatory, 13 insecticidal, 14 antifolate, 15 tyrosine kinase inhibitor, 16 antimicrobial, 17 calcium channel antagonists, 18 antileishmanial, 19 diuretic and potassium-sparing. 20 On the other hand thiazolo-pyrimidines are important class of compounds with wide range of biological activity.…”