Synthesis and Antioxidant Activity of 1,2,4-Triazole linked Thieno[2,3- d]pyrimidine Derivatives

Maddila, Suresh; Kumar, Ankit; Gorle, Sridevi; Singh, M.; Lavanya, P.; Jonnalagadda, Sreekantha B.

doi:10.2174/157018013804725152

Cited by 29 publications

(15 citation statements)

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“…The 1 H NMR spectra of compounds 11a-c revealed signals in 10.07-11.83 ppm range attributed to NH group. T A B L E 1 Syntheses of dihydropyrimidine derivatives (7)(8)(9)(10)(11)(12) Moreover, compound 11c showed a singlet signal due to NH 2 . Finally, reactions of hydrazinopyrimidine 1 with different cyclic ketones namely, cyclopentanone, 1Hinden-2(3H)-one and 1H-indene-1, 2, 3-trione afforded the target compounds 12a-c (Scheme 4).…”

Section: Discussionmentioning

confidence: 99%

“…[7][8][9] Meanwhile, Schiff bases have been attracting much interest from synthetic and biological aspects. [10][11][12] The literature survey revealed that Schiff bases with various heterocyclic moieties also possess cytotoxic, [13] anticonvulsant, [14,15] antiproliferative, [11,16] antimicrobial, [17,18] anticancer, [19] and antifungal activities. [7,20] Moreover, pyrazole derivatives have been reported to act as antitumor agents against various types of lung, breast, and leukemia carcinomas.…”

Section: Introductionmentioning

confidence: 99%

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Eco‐friendly synthesis of novel pyrimidine derivatives as potential anticancer agents

Abbass

Khalil

El‐Naggar

2020

Journal of Heterocyclic Chem

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Herein, a rapid and highly efficient method for the synthesis of a new series of pyrimidine derivatives was demonstrated. The strategy was emanated from the reaction of hydrazinyl pyrimidine derivative (1) with different electrophilic species such as ethyl acetoacetate, ethyl 4,4,4‐trifluoro acetoacetate, and phenyl isothiocyanate following cyclocondensation mechanism to afford the corresponding derivatives (2‐6). Furthermore, condensation of hydrazine derivative (1) with different carbonyl compounds via conventional heating and microwave irradiation conditions was employed as a source of Schiff base derivatives bearing pyrimidine moiety (7‐12). The structural features of all newly synthesized compounds were characterized by elemental and spectroscopic evidences. Some of the synthesized compounds were evaluated for in vitro cytotoxicity. The preliminary screening results showed that most of the tested compounds have moderate cytotoxic activity against HepG2 and HCT‐116 cell lines. Finally, a molecular docking study was conducted to reveal the probable interaction with the thymidylate synthase enzyme.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Eco‐friendly synthesis of novel pyrimidine derivatives as potential anticancer agents

Abbass

Khalil

El‐Naggar

2020

Journal of Heterocyclic Chem

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“…1,2,4 triazole, a class of nitrogen‐containing heterocycles, has gained considerable interest because of their assorted biological activities such as antitumor,[10] antiviral,[11] anti‐HIV, antimicrobial,[13] antifungal,[14] antioxidant,[15] anti‐inflammatory,[16] and anticonvulsant [17]. The diverse biological properties of 1,2,4 triazole can be attributed to moderate dipole character, hydrogen bonding capability, rigidity and stability under in vivo conditions.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, biological evaluation, and molecular docking studies of novel 3‐aryl‐5‐(alkyl‐thio)‐1H‐1,2,4‐triazoles derivatives targeting Mycobacterium tuberculosis

et al. 2017

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A small library of new 3-aryl-5-(alkyl-thio)-1H-1,2,4-triazoles was synthesized and screened for the antimycobacterial potency against Mycobacterium tuberculosis H Ra strain and Mycobacterium bovis BCG both in active and dormant stage. Among the synthesized library, 25 compounds exhibited promising anti-TB activity in the range of IC 0.03-5.88 μg/ml for dormant stage and 20 compounds in the range of 0.03-6.96 μg/ml for active stage. Their lower toxicity (>100 μg/ml) and higher selectivity (SI = >10) against all cancer cell lines screened make them interesting compounds with potential antimycobacterial effects. Furthermore, to rationalize the observed biological activity data and to establish a structural basis for inhibition of M. tuberculosis, the molecular docking study was carried out against a potential target MTB CYP121 which revealed a significant correlation between the binding score and biological activity for these compounds. Cytotoxicity and in vivo pharmacokinetic studies suggested that 1,2,4-triazole analogues have an acceptable safety index, in vivo stability and bio-availability.

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“…Similarly, several types of triazoles have been proved to possess valuable pharmacological properties, such as antiviral , antioxidant , antimalarial , anticonvulsant , Alzheimer's disease , antidepressant , antimicrobial , antitubercular , anti‐inflammatory , antiplatelet , antibacterial , antifungal , anticancer , antiproliferative , and anti‐HIV activities. In the pursuit of design of new drugs, the development of hybrid molecules through the combination of different pharmacophores in one frame could lead to compounds with interesting biological properties.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Insecticidal Activity of Tetrazole‐Linked Triazole Derivatives

Maddila

Pagadala

Jonnalagadda

2014

Journal of Heterocyclic Chem

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A new series of 4‐(4‐substitutedbenzylideneamino)‐5‐((1‐methyl‐1H‐tetrazol‐5‐ylthio)methyl)‐4H‐1,2,4‐triazole‐3‐thiol derivatives (5a, 5b, 5c, 5d, 5e, 5f, 5g, 5h, 5i, 5j, 5k) are prepared using 4‐amino‐5‐((1‐methyl‐1H‐tetrazol‐5‐ylthio)methyl‐4H‐1,2,4‐triazole‐3‐thiol (4), as an intermediate compound. The structures of all the newly synthesized products are established supported by their spectral 1H NMR, 13C NMR, FTIR, electrospray ionization mass spectrometry (mass), and analytical data. All the compounds are screened for their insecticidal activity against Plodia interpunctella, and six compounds exhibited significant activity.

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Synthesis and Antioxidant Activity of 1,2,4-Triazole linked Thieno[2,3- d]pyrimidine Derivatives

Cited by 29 publications

References 0 publications

Eco‐friendly synthesis of novel pyrimidine derivatives as potential anticancer agents

Eco‐friendly synthesis of novel pyrimidine derivatives as potential anticancer agents

Synthesis, biological evaluation, and molecular docking studies of novel 3‐aryl‐5‐(alkyl‐thio)‐1H‐1,2,4‐triazoles derivatives targeting Mycobacterium tuberculosis

Synthesis and Insecticidal Activity of Tetrazole‐Linked Triazole Derivatives

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