Search Results - "Perello, Marcia Alberton"
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Synthesis and Antimycobacterial Activity of 3-Phenyl-1H-indoles
Published in Molecules (Basel, Switzerland) (25-08-2021)“…Tuberculosis has been described as a global health crisis since the 1990s, with an estimated 1.4 million deaths in the last year. Herein, a series of 20…”
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Crystal structure of dihydroneopterin aldolase from Mycobacterium tuberculosis associated with 8-mercaptoguanine, and development of novel S8-functionalized analogues as inhibitors: Synthesis, enzyme inhibition, in vitro toxicity and antitubercular activity
Published in Journal of enzyme inhibition and medicinal chemistry (01-12-2024)“…The crystallographic structure of the FolB enzyme from ( FolB), complexed with its inhibitor 8-mercaptoguanine (8-MG), was elucidated at a resolution of 1.95…”
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3
Exploring Scaffold Hopping for Novel 2‑(Quinolin-4-yloxy)acetamides with Enhanced Antimycobacterial Activity
Published in ACS medicinal chemistry letters (11-04-2024)“…Utilizing a scaffold-hopping strategy from the drug candidate telacebec, a novel series of 2-(quinolin-4-yloxy)acetamides was synthesized and evaluated as…”
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Antitubercular Activity of Novel 2‑(Quinoline-4-yloxy)acetamides with Improved Drug-Like Properties
Published in ACS medicinal chemistry letters (11-08-2022)“…Using cycloalkyl and electron-donating groups to decrease the carbonyl electrophilicity, a novel series of 2-(quinoline-4-yloxy)acetamides was synthesized and…”
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5
Evaluation of 3-Deoxy-D-Arabino-Heptulosonate 7-Phosphate Synthase (DAHPS) as a Vulnerable Target in Mycobacterium tuberculosis
Published in Microbiology spectrum (31-08-2022)“…Tuberculosis (TB) remains one of the leading causes of death due to a single pathogen. The emergence and proliferation of multidrug-resistant (MDR-TB) and…”
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6
EPSP Synthase-Depleted Cells Are Aromatic Amino Acid Auxotrophs in Mycobacterium smegmatis
Published in Microbiology spectrum (22-12-2021)“…The epidemiological importance of mycobacterial species is indisputable, and the necessity to find new molecules that can inhibit their growth is urgent. The…”
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Novel 4-aminoquinolines: Synthesis, inhibition of the Mycobacterium tuberculosis enoyl-acyl carrier protein reductase, antitubercular activity, SAR, and preclinical evaluation
Published in European journal of medicinal chemistry (05-01-2023)“…Herein a series of 4-aminoquinolines were synthesized in an attempt to optimize and study the structural features related to LABIO-17 biological activity, a…”
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8
Identification of potential inhibitors of Mycobacterium tuberculosis shikimate kinase: molecular docking, in silico toxicity and in vitro experiments
Published in Journal of computer-aided molecular design (01-03-2023)“…Tuberculosis (TB) is one of the main causes of death from a single pathological agent, Mycobacterium tuberculosis ( Mtb ). In addition, the emergence of…”
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9
Identification of antimycobacterial 8-hydroxyquinoline derivatives as in vitro enzymatic inhibitors of Mycobacterium tuberculosis enoyl-acyl carrier protein reductase
Published in Bioorganic chemistry (01-10-2024)“…[Display omitted] •Small library of 8-hydroxyquinoline (8HQ) was evaluated against M. tuberculosis.•9 derivatives were active against the mycobacteria.•5a, 5c,…”
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10
Synthesis and Antimycobacterial Evaluation of N -(4-(Benzyloxy)benzyl)-4-aminoquinolines
Published in Molecules (Basel, Switzerland) (15-04-2022)“…Tuberculosis remains a global health problem that affects millions of people around the world. Despite recent efforts in drug development, new alternatives are…”
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11
Targeting thymidine phosphorylase inhibition in human colorectal cancer xenografts
Published in Biomedicine & pharmacotherapy (01-07-2021)“…Human thymidine phosphorylase (hTP) is overexpressed in several solid tumors and is commonly associated with aggressiveness and unfavorable prognosis…”
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12
Identification and characterization of new structural scaffolds modulating the activity of Mycobacterium tuberculosis dihydroneopterin aldolase (FolB) in vitro
Published in Frontiers in tropical diseases (01-06-2024)“…IntroductionAntifolates were among the first broad-spectrum compounds used as antimycobacterial agents and can still be of use when no other therapeutic…”
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