Exploring the gyrase ATPase domain for tailoring newer anti-tubercular drugs: Hit to lead optimization of a novel class of thiazole inhibitors

Bioorganic and Medicinal Chemistry

Volumn 23, Issue 3, 2015, Pages 588-601

  Jeankumar, Variam Ullas ^a   Kotagiri, Sonali ^a   Janupally, Renuka ^a   Suryadevara, Priyanka ^a   Sridevi, Jonnalagadda Padma ^a   Medishetti, Raghavender ^b   Kulkarni, Pushkar ^b   Yogeeswari, Perumal ^a   Sriram, Dharmarajan ^a  

^a BIRLA INSTITUTE OF TECHNOLOGY AND SCIENCE   (India)

^b UNIVERSITY OF HYDERABAD   (India)

Author keywords

Gyrase ATPase domain; hERG; Medium throughput screening; Mycobacterium tuberculosis; Tuberculosis

Indexed keywords

1 (4 ACETYLPHENYL) 3 [1 (5 NITROTHIAZOL 2 YL)PIPERIDIN 4 YL]THIOUREA; 1 (4 ACETYLPHENYL) 3 [1 (5 NITROTHIAZOL 2 YL)PIPERIDIN 4 YL]UREA; 1 (4 CHLOROBENZYL) 3 [1 (5 NITROTHIAZOL 2 YL)PIPERIDIN 4 YL]THIOUREA; 1 (4 CHLOROBENZYL) 3 [1 (5 NITROTHIAZOL 2 YL)PIPERIDIN 4 YL]UREA; 1 (4 CHLOROPHENYL) 3 [1 (5 NITROTHIAZOL 2 YL)PIPERIDIN 4 YL]THIOUREA; 1 (4 CHLOROPHENYL) 3 [1 (5 NITROTHIAZOL 2 YL)PIPERIDIN 4 YL]UREA; 1 (4 FLUOROBENZYL) 3 [1 (5 NITROTHIAZOL 2 YL)PIPERIDIN 4 YL]THIOUREA; 1 (4 FLUOROBENZYL) 3 [1 (5 NITROTHIAZOL 2 YL)PIPERIDIN 4 YL]UREA; 1 (4 FLUOROPHENYL) 3 [1 (5 NITROTHIAZOL 2 YL)PIPERIDIN 4 YL]THIOUREA; 1 (4 FLUOROPHENYL) 3 [1 (5 NITROTHIAZOL 2 YL)PIPERIDIN 4 YL]UREA; 1 (4 METHOXYBENZYL) 3 [1 (5 NITROTHIAZOL 2 YL)PIPERIDIN 4 YL]THIOUREA; 1 (4 METHOXYBENZYL) 3 [1 (5 NITROTHIAZOL 2 YL)PIPERIDIN 4 YL]UREA; 1 (4 METHOXYPHENYL) 3 [1 (5 NITROTHIAZOL 2 YL)PIPERIDIN 4 YL]THIOUREA; 1 (4 METHOXYPHENYL) 3 [1 (5 NITROTHIAZOL 2 YL)PIPERIDIN 4 YL]UREA; 1 (4 NITROPHENYL) 3 [1 (5 NITROTHIAZOL 2 YL)PIPERIDIN 4 YL]THIOUREA; 1 (4 NITROPHENYL) 3 [1 (5 NITROTHIAZOL 2 YL)PIPERIDIN 4 YL]UREA; 1 (4 TOLYL) 3 [1 (5 NITROTHIAZOL 2 YL)PIPERIDIN 4 YL]THIOUREA; 1 (4 TOLYL) 3 [1 (5 NITROTHIAZOL 2 YL)PIPERIDIN 4 YL]UREA; 1 (5 NITROTHIAZOL 2 YL) N PHENYLPIPERIDIN 4 AMINE; 1 BENZYL 3 [1 (5 NITROTHIAZOL 2 YL)PIPERIDIN 4 YL]THIOUREA; 1 BENZYL 3 [1 (5 NITROTHIAZOL 2 YL)PIPERIDIN 4 YL]UREA; 1 [1 (5 NITROTHIAZOL 2 YL)PIPERIDIN 4 YL] 3 PHENYLTHIOUREA; 1 [1 (5 NITROTHIAZOL 2 YL)PIPERIDIN 4 YL] 3 PHENYLUREA; N (4 CHLOROBENZYL) 1 (5 NITROTHIAZOL 2 YL)PIPERIDIN 4 AMINE; N (4 FLUOROBENZYL) 1 (5 NITROTHIAZOL 2 YL)PIPERIDIN 4 AMINE; N (4 METHOXYBENZYL) 1 (5 NITROTHIAZOL 2 YL)PIPERIDIN 4 AMINE; N BENZYL 1 (5 NITROTHIAZOL 2 YL)PIPERIDIN 4 AMINE; N [1 (5 NITROTHIAZOL 2 YL)PIPERIDIN 4 YL]BENZAMIDE; TUBERCULOSTATIC AGENT; UNCLASSIFIED DRUG; UNINDEXED DRUG; ADENOSINE TRIPHOSPHATASE; DNA TOPOISOMERASE (ATP HYDROLYSING); GYRASE INHIBITOR; THIAZOLE DERIVATIVE;

ARTICLE; BACTERIAL STRAIN; CONCENTRATION RESPONSE; CONTROLLED STUDY; CYTOTOXICITY TEST; DRUG DETERMINATION; DRUG EFFECT; DRUG POTENCY; DRUG SAFETY; DRUG SCREENING; DRUG STRUCTURE; IC50; IN VITRO STUDY; MINIMUM INHIBITORY CONCENTRATION; MOLECULAR LIBRARY; MYCOBACTERIUM SMEGMATIS; MYCOBACTERIUM TUBERCULOSIS; NONHUMAN; ANIMAL; ANTAGONISTS AND INHIBITORS; CHEMICAL STRUCTURE; CHEMISTRY; DRUG DESIGN; DRUG DEVELOPMENT; DRUG EFFECTS; ENZYMOLOGY; HUMAN; METABOLISM; PROTEIN SECONDARY STRUCTURE; PROTEIN TERTIARY STRUCTURE; STRUCTURE ACTIVITY RELATION; ZEBRA FISH;

MYCOBACTERIUM TUBERCULOSIS;

ADENOSINE TRIPHOSPHATASES; ANIMALS; ANTITUBERCULAR AGENTS; DNA GYRASE; DRUG DESIGN; DRUG DISCOVERY; HUMANS; MODELS, MOLECULAR; MYCOBACTERIUM SMEGMATIS; PROTEIN STRUCTURE, SECONDARY; PROTEIN STRUCTURE, TERTIARY; STRUCTURE-ACTIVITY RELATIONSHIP; THIAZOLES; TOPOISOMERASE II INHIBITORS; ZEBRAFISH;

EID: 84921346470     PISSN: 09680896     EISSN: 14643391     Source Type: Journal    
DOI: 10.1016/j.bmc.2014.12.001     Document Type: Article

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