Synthesis and Biological Evaluation of Novel Phenothiazine-Sulfonamide Based Isoxazole Derivatives as Potent Antibacterial Agents

Mallam, None Vasudha; Kumar, Manoj; Vijayakumar, Baru

doi:10.1134/s1068162022030219

Cited by 3 publications

(2 citation statements)

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“…[24][25][26][27] 1,2,3-Triazole-containing compounds received more attention due to their varied biological activities such as antifungal, [28][29][30][31][32][33][34] antimicrobial, [35,36] antivirals, [37,38] antimalarial, [39,40] anticancer [41][42][43] and anti-inflammatory activities. [44,45] The isoxazole containing natural and synthetic compounds reported for a wide range of biological activities such as antimicrobial, [46,47] antibacterial, [48][49][50] antifungal, [51,52] antitubercular, [16,[53][54][55] antiviral, [56,57] anticancer, [58][59][60] and anti-inflammatory. [61][62][63] Some of the FDA-approved and commercialized drugs containing isoxazole and triazole pharmacophore are shown in Figure 1 1) The hybrids of 1,2,4-triazole drugs by clubbing with azole or structural modifications of the fluconazole, isavuconazole, ravuconazole and albaconazole were reported for potential antifungal activity.…”

Section: Introductionmentioning

confidence: 99%

“…1,2,3‐Triazole‐containing compounds received more attention due to their varied biological activities such as antifungal, [28–34] antimicrobial, [35,36] antivirals, [37,38] antimalarial, [39,40] anticancer [41–43] and anti‐inflammatory activities [44,45] . The isoxazole containing natural and synthetic compounds reported for a wide range of biological activities such as antimicrobial, [46,47] antibacterial, [48–50] antifungal, [51,52] antitubercular, [16,53–55] antiviral, [56,57] anticancer, [58–60] and anti‐inflammatory [61–63] …”

Section: Introductionmentioning

confidence: 99%

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An Efficient Synthesis, Antimicrobial Evaluation and In Silico Studies of 1,2,3‐Triazolyl‐isoxazolyl‐ethanol Derivatives

Bhoye,

Latif Shaikh,

Walunj

et al. 2024

ChemistrySelect

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A series of 2‐(1‐substituted benzyl‐1H‐1,2,3‐triazol‐4‐yl)‐1‐(5‐arylisoxazol‐3‐yl)ethanol (8 a–p) have been designed and efficiently synthesized. The structure of the compounds 8 a–p was characterized by spectral methods. The newly synthesized 1,2,3‐triazolyl‐isoxazolyl‐ethanol (8 a–p) derivatives were evaluated for in vitro antimicrobial activity against P. mirabilis, E. coli, S. albus, B. subtilis, C. albicans and A. niger. Eleven derivatives showed good activity against the Gram‐negative strains. Compounds 8 b, 8 c, 8 d, 8 g, 8 h, 8 i, 8 j, 8 k, 8 n, 8 o, and 8 p showed good antibacterial against E. coli activity. Against P. mirabilis, compounds 8 a, 8 b, 8 d, 8 g, 8 h, 8 k, 8 l, 8 m, 8 n, 8 o, and 8 p showed good activity, compounds 8 o, and 8 p showed two‐fold less activity than the reference drug streptomycin. Against the Gram‐positive strain, B. subtilis, compounds 8 c, 8 d and 8 f showed good activity, from which the compounds 8 d and 8 f were found only two‐fold less potent than the reference drug streptomycin. Against fungal strains, C. albicans, compound 8 g and against A. niger, compounds 8 f, 8 h and 8 j showed good antifungal activity. Against A. niger strain, the compounds 8 f and 8 h reported only two‐fold less activity than the reference drug fluconazole. The active compounds were studied for molecular docking and molecular dynamics simulations.

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