Target Information
Target General Information | Top | |||||
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Target ID |
T22348
(Former ID: TTDI01914)
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Target Name |
Bacterial DNA gyrase (Bact gyrase)
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Synonyms |
DNA gyrase
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Gene Name |
Bact gyrA; Bact gyrB
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Target Type |
Successful target
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[1] | ||||
Disease | [+] 8 Target-related Diseases | + | ||||
1 | Bacterial infection [ICD-11: 1A00-1C4Z] | |||||
2 | Bronchitis [ICD-11: CA20] | |||||
3 | Glaucoma [ICD-11: 9C61] | |||||
4 | Gram-positive bacterial infection [ICD-11: 1B74-1F40] | |||||
5 | Impetigo [ICD-11: 1B72] | |||||
6 | Pneumonia [ICD-11: CA40] | |||||
7 | Respiratory infection [ICD-11: CA07-CA4Z] | |||||
8 | Urinary tract infection [ICD-11: GC08] | |||||
Function |
DNA gyrase negatively supercoils closed circular double- stranded DNA in an ATP-dependent manner and also catalyzes the interconversion of other topological isomers of double-stranded DNA rings, including catenanes and knotted rings.
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BioChemical Class |
ATP-hydrolyzing DNA topoisomerase
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UniProt ID | ||||||
Sequence |
MAELPQSRINERNITSEMRESFLDYAMSVIVARALPDVRDGLKPVHRRILYGLNEQGMTP
DKSYKKSARIVGDVMGKYHPHGDSSIYEAMVRMAQDFSYRYPLVDGQGNFGSMDGDGAAA MRYTEARMTKITLELLRDINKDTIDFIDNYDGNEREPSVLPARFPNLLANGASGIAVGMA TNIPPHNLTELINGVLSLSKNPDISIAELMEDIEGPDFPTAGLILGKSGIRRAYETGRGS IQMRSRAVIEERGGGRQRIVVTEIPFQVNKARMIEKIAELVRDKKIDGITDLRDETSLRT GVRVVIDVRKDANASVILNNLYKQTPLQTSFGVNMIALVNGRPKLINLKEALVHYLEHQK TVVRRRTQYNLRKAKDRAHILEGLRIALDHIDEIISTIRESDTDKVAMESLQQRFKLSEK QAQAILDMRLRRLTGLERDKIEAEYNELLNYISELEAILADEEVLLQLVRDELTEIRDRF GDDRRTEIQLGGFEDLEDEDLIPEEQIVITLSHNNYIKRLPVSTYRAQNRGGRGVQGMNT LEEDFVSQLVTLSTHDHVLFFTNKGRVYKLKGYEVPELSRQSKGIPVVNAIELENDEVIS TMIAVKDLESEDNFLVFATKRGVVKRSALSNFSRINRNGKIAISFREDDELIAVRLTSGQ EDILIGTSHASLIRFPESTLRPLGRTATGVKGITLREGDEVVGLDVAHANSVDEVLVVTE NGYGKRTPVNDYRLSNRGGKGIKTATITERNGNVVCITTVTGEEDLMIVTNAGVIIRLDV ADISQNGRAAQGVRLIRLGDDQFVSTVAKVKEDAEDETNEDEQSTSTVSEDGTEQQREAV VNDETPGNAIHTEVIDSEENDEDGRIEVRQDFMDRVEEDIQQSLDEDEE Click to Show/Hide
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Drugs and Modes of Action | Top | |||||
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Approved Drug(s) | [+] 15 Approved Drugs | + | ||||
1 | Besifloxacin | Drug Info | Approved | Ocular inflammation | [1], [2] | |
2 | Ciprofloxacin XR | Drug Info | Approved | Bacterial infection | [3] | |
3 | Finafloxacin | Drug Info | Approved | Urinary tract infection | [3], [4] | |
4 | Gatifloxacin | Drug Info | Approved | Respiratory tract infection | [5] | |
5 | Gemifloxacin | Drug Info | Approved | Bacterial infection | [6] | |
6 | Grepafloxacin | Drug Info | Approved | Chronic bronchitis | [3] | |
7 | Levofloxacin | Drug Info | Approved | Bacterial infection | [7] | |
8 | Moxifloxacin | Drug Info | Approved | Bacterial infection | [5] | |
9 | Nemonoxacin | Drug Info | Approved | Community-acquired pneumonia | [8] | |
10 | Norfloxacin | Drug Info | Approved | Bacterial infection | [9] | |
11 | Ofloxacin | Drug Info | Approved | Bacterial infection | [10] | |
12 | Ozenoxacin | Drug Info | Approved | Impetigo | [11] | |
13 | Prulifloxacin | Drug Info | Approved | Urinary tract infection | [12] | |
14 | Sparfloxacin | Drug Info | Approved | Bacterial infection | [13] | |
15 | Trovafloxacin | Drug Info | Approved | Bacterial infection | [14] | |
Clinical Trial Drug(s) | [+] 9 Clinical Trial Drugs | + | ||||
1 | AZD0914 | Drug Info | Phase 3 | Neisseria gonorrhoeae infection | [15] | |
2 | BAY-35-3377 | Drug Info | Phase 3 | Otitis media | [16] | |
3 | Pazufloxacin | Drug Info | Phase 3 | Conjunctivitis | [17] | |
4 | Zabofloxacin | Drug Info | Phase 3 | Pneumonia | [18] | |
5 | JNJ-32729463 | Drug Info | Phase 2 | Community-acquired pneumonia | [19] | |
6 | Sitafloxacin | Drug Info | Phase 2 | Escherichia coli infection | [20] | |
7 | TNP-2092 | Drug Info | Phase 2 | Skin and skin-structure infection | [21] | |
8 | VB 1953 | Drug Info | Phase 2 | Acne vulgaris | [22] | |
9 | WCK-771 | Drug Info | Phase 2 | Bacterial infection | [23] | |
Discontinued Drug(s) | [+] 27 Discontinued Drugs | + | ||||
1 | Temafloxacin | Drug Info | Withdrawn from market | Bacterial infection | [24] | |
2 | OLAMUFLOXACIN MESILATE | Drug Info | Discontinued in Phase 3 | Bacterial infection | [25] | |
3 | 99mTc-ciprofloxacin | Drug Info | Discontinued in Phase 2 | Infectious disease | [26] | |
4 | A-86719.1 | Drug Info | Discontinued in Phase 2 | Bacterial infection | [27] | |
5 | BAY-Y-3118 | Drug Info | Discontinued in Phase 2 | Bacterial infection | [28] | |
6 | Cadrofloxacin | Drug Info | Discontinued in Phase 2 | Bacterial infection | [29] | |
7 | CFC-222 | Drug Info | Discontinued in Phase 2 | Bacterial infection | [30] | |
8 | DANOFLOXACIN | Drug Info | Discontinued in Phase 2 | Bacterial infection | [31] | |
9 | DX-619 | Drug Info | Discontinued in Phase 2 | Bacterial infection | [32] | |
10 | FANDOFLOXACIN HYDROCHLORIDE | Drug Info | Discontinued in Phase 2 | Bacterial infection | [33] | |
11 | Ro-23-9424 | Drug Info | Discontinued in Phase 2 | Bacterial infection | [34] | |
12 | AZD-5099 | Drug Info | Discontinued in Phase 1 | Infectious disease | [35] | |
13 | Cetefloxacin | Drug Info | Discontinued in Phase 1 | Bacterial infection | [36] | |
14 | DV-7751A | Drug Info | Discontinued in Phase 1 | Bacterial infection | [37] | |
15 | GSK945237 | Drug Info | Discontinued in Phase 1 | Bacterial infection | [38] | |
16 | PD-131112 | Drug Info | Discontinued in Phase 1 | Bacterial infection | [39] | |
17 | A-70826 | Drug Info | Terminated | Bacterial infection | [41] | |
18 | BMY-40062 | Drug Info | Terminated | Bacterial infection | [42] | |
19 | CBR-2092 | Drug Info | Terminated | Bacterial infection | [43] | |
20 | Clinafloxacin | Drug Info | Terminated | Pneumonia | [44] | |
21 | CP-67015 | Drug Info | Terminated | Bacterial infection | [45] | |
22 | KB-5246 | Drug Info | Terminated | Bacterial infection | [46] | |
23 | MF-5137 | Drug Info | Terminated | Staphylococcus infection | [47] | |
24 | PD-117596 | Drug Info | Terminated | Bacterial infection | [48] | |
25 | Protosufloxacin | Drug Info | Terminated | Bacterial infection | [49] | |
26 | Ro-23-7777 | Drug Info | Terminated | Fungal infection | [50] | |
27 | S-34109 | Drug Info | Terminated | Staphylococcus infection | [51] | |
Preclinical Drug(s) | [+] 1 Preclinical Drugs | + | ||||
1 | Viquidacin | Drug Info | Preclinical | Bacterial infection | [40] | |
Mode of Action | [+] 2 Modes of Action | + | ||||
Modulator | [+] 45 Modulator drugs | + | ||||
1 | Besifloxacin | Drug Info | [1], [2] | |||
2 | Ciprofloxacin XR | Drug Info | [52], [53] | |||
3 | Finafloxacin | Drug Info | [4], [54] | |||
4 | Gatifloxacin | Drug Info | [52] | |||
5 | Gemifloxacin | Drug Info | [52] | |||
6 | Grepafloxacin | Drug Info | [55] | |||
7 | Levofloxacin | Drug Info | [52] | |||
8 | Moxifloxacin | Drug Info | [52] | |||
9 | Norfloxacin | Drug Info | [52] | |||
10 | Ofloxacin | Drug Info | [52] | |||
11 | Ozenoxacin | Drug Info | [56] | |||
12 | Sparfloxacin | Drug Info | [52] | |||
13 | Trovafloxacin | Drug Info | [52] | |||
14 | AZD0914 | Drug Info | [57] | |||
15 | Zabofloxacin | Drug Info | [60] | |||
16 | WCK-771 | Drug Info | [65], [66] | |||
17 | Temafloxacin | Drug Info | [67] | |||
18 | OLAMUFLOXACIN MESILATE | Drug Info | [68] | |||
19 | A-86719.1 | Drug Info | [70] | |||
20 | BAY-Y-3118 | Drug Info | [71] | |||
21 | Cadrofloxacin | Drug Info | [72] | |||
22 | CFC-222 | Drug Info | [73] | |||
23 | DANOFLOXACIN | Drug Info | [74] | |||
24 | DX-619 | Drug Info | [75] | |||
25 | FANDOFLOXACIN HYDROCHLORIDE | Drug Info | [68] | |||
26 | Ro-23-9424 | Drug Info | [76] | |||
27 | AZD-5099 | Drug Info | [77] | |||
28 | Cetefloxacin | Drug Info | [68] | |||
29 | DV-7751A | Drug Info | [78] | |||
30 | GSK945237 | Drug Info | [79] | |||
31 | PD-131112 | Drug Info | [68] | |||
32 | Viquidacin | Drug Info | [80] | |||
33 | A-70826 | Drug Info | [81] | |||
34 | BMY-40062 | Drug Info | [82] | |||
35 | CBR-2092 | Drug Info | [83] | |||
36 | Clinafloxacin | Drug Info | [84] | |||
37 | CP-67015 | Drug Info | [52] | |||
38 | KB-5246 | Drug Info | [85] | |||
39 | MF-5137 | Drug Info | [52] | |||
40 | PD-117596 | Drug Info | [86] | |||
41 | Protosufloxacin | Drug Info | [52] | |||
42 | Ro-23-7777 | Drug Info | [52] | |||
43 | S-34109 | Drug Info | [87] | |||
44 | NSFQ-105 | Drug Info | [88] | |||
45 | PD-117558 | Drug Info | [89] | |||
Inhibitor | [+] 9 Inhibitor drugs | + | ||||
1 | Nemonoxacin | Drug Info | [8] | |||
2 | Prulifloxacin | Drug Info | [12] | |||
3 | BAY-35-3377 | Drug Info | [58] | |||
4 | Pazufloxacin | Drug Info | [59] | |||
5 | JNJ-32729463 | Drug Info | [61] | |||
6 | Sitafloxacin | Drug Info | [62] | |||
7 | TNP-2092 | Drug Info | [63] | |||
8 | VB 1953 | Drug Info | [64] | |||
9 | 99mTc-ciprofloxacin | Drug Info | [69] |
Drug Property Profile of Target | Top | |
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(1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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(5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five |
Co-Targets | Top | |||||
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Co-Targets |
References | Top | |||||
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REF 1 | Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92. | |||||
REF 2 | Besifloxacin ophthalmic suspension, 0.6%: a novel topical fluoroquinolone for bacterial conjunctivitis. Adv Ther. 2012 Jun;29(6):473-90. | |||||
REF 3 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
REF 4 | 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81. | |||||
REF 5 | Novel agents in the management of Mycobacterium tuberculosis disease. Curr Med Chem. 2007;14(18):2000-8. | |||||
REF 6 | Emerging drugs for bacterial urinary tract infections. Expert Opin Emerg Drugs. 2005 May;10(2):275-98. | |||||
REF 7 | How many modes of action should an antibiotic have Curr Opin Pharmacol. 2008 Oct;8(5):564-73. | |||||
REF 8 | Nemonoxacin: first global approval. Drugs. 2014 Aug;74(12):1445-53. | |||||
REF 9 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 074690. | |||||
REF 10 | Emerging therapies for the treatment and prevention of otitis media. Expert Opin Emerg Drugs. 2006 May;11(2):251-64. | |||||
REF 11 | 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85. | |||||
REF 12 | Prulifloxacin: a new antibacterial fluoroquinolone. Expert Rev Anti Infect Ther. 2006 Feb;4(1):27-41. | |||||
REF 13 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 020677. | |||||
REF 14 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 050762. | |||||
REF 15 | ClinicalTrials.gov (NCT03959527) Zoliflodacin in Uncomplicated Gonorrhoea. U.S. National Institutes of Health. | |||||
REF 16 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012837) | |||||
REF 17 | ClinicalTrials.gov (NCT03696342) Efficacy of the Ophthalmic Pazufloxacin 0.6% for Bacterial Conjunctivitis, Compared to Gatifloxacin 0.3%. (PRO-157). U.S. National Institutes of Health. | |||||
REF 18 | ClinicalTrials.gov (NCT01658020) A Study to Evaluate Efficacy and Safety Profile of Zabofloxacin Tablet 400mg and Moxifloxacin Tablet 400mg. U.S. National Institutes of Health. | |||||
REF 19 | ClinicalTrials.gov (NCT01198626) Efficacy and Safety Study of JNJ-32729463 Compared With Moxifloxacin for the Treatment of Subjects Requiring Hospitalization for Community-Acquired Bacterial Pneumonia. U.S. National Institutes of Health. | |||||
REF 20 | ClinicalTrials.gov (NCT02537847) Sitafloxacin and Ertapenem Treatment for Acute Pyelonephritis Caused by Escherichia Coli (SETAP). U.S. National Institutes of Health. | |||||
REF 21 | ClinicalTrials.gov (NCT03964493) TNP-2092 to Treat Acute Bacterial Skin and Skin Structure Infection (P2_ABSSSI). U.S. National Institutes of Health. | |||||
REF 22 | ClinicalTrials.gov (NCT03900676) Efficacy and Safety Study of VB-1953 Topical Gel for Inflammatory Facial Acne Vulgaris. U.S. National Institutes of Health. | |||||
REF 23 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016734) | |||||
REF 24 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000542) | |||||
REF 25 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006301) | |||||
REF 26 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016416) | |||||
REF 27 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004047) | |||||
REF 28 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001782) | |||||
REF 29 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002693) | |||||
REF 30 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004010) | |||||
REF 31 | Pharmacokinetic and pharmacodynamic profiles of danofloxacin administered by two dosing regimens in calves infected with Mannheimia (Pasteurella) haemolytica. Antimicrob Agents Chemother. 2002 Sep;46(9):3013-9. | |||||
REF 32 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019670) | |||||
REF 33 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004009) | |||||
REF 34 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000529) | |||||
REF 35 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800034406) | |||||
REF 36 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001898) | |||||
REF 37 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002052) | |||||
REF 38 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027355) | |||||
REF 39 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001614) | |||||
REF 40 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017450) | |||||
REF 41 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001978) | |||||
REF 42 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000465) | |||||
REF 43 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027165) | |||||
REF 44 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000525) | |||||
REF 45 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003590) | |||||
REF 46 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000463) | |||||
REF 47 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004011) | |||||
REF 48 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000523) | |||||
REF 49 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003745) | |||||
REF 50 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003620) | |||||
REF 51 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007670) | |||||
REF 52 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | |||||
REF 53 | DOI: 10.1093/jac/48.4.479 | |||||
REF 54 | Antibacterial activity of finafloxacin under different pH conditions against isogenic strains of Escherichia coli expressing combinations of defined mechanisms of fluoroquinolone resistance.J Antimicrob Chemother.2010 Dec;65(12):2530-3. | |||||
REF 55 | Grepafloxacin, a dimethyl derivative of ciprofloxacin, acts preferentially through gyrase in Streptococcus pneumoniae: role of the C-5 group in tar... Antimicrob Agents Chemother. 2002 Feb;46(2):582-5. | |||||
REF 56 | In vitro and in vivo antibacterial activity of T-3912, a novel non-fluorinated topical quinolone. J Antimicrob Chemother. 2002 Mar;49(3):455-65. | |||||
REF 57 | High in vitro activity of the novel spiropyrimidinetrione AZD0914, a DNA gyrase inhibitor, against multidrug-resistant Neisseria gonorrhoeae isolates suggests a new effective option for oral treatment of gonorrhea.Antimicrob Agents Chemother.2014 Sep;58(9):5585-8. | |||||
REF 58 | Antibiotics in the clinical pipeline in 2013. J Antibiot (Tokyo). 2013 Oct;66(10):571-91. | |||||
REF 59 | Target preference of 15 quinolones against Staphylococcus aureus, based on antibacterial activities and target inhibition. Antimicrob Agents Chemother. 2001 Dec;45(12):3544-7. | |||||
REF 60 | DNA gyrase and topoisomerase IV are dual targets of zabofloxacin in Streptococcus pneumoniae.Int J Antimicrob Agents.2010 Jul;36(1):97-8. | |||||
REF 61 | Antistaphylococcal activities of the new fluoroquinolone JNJ-Q2. Antimicrob Agents Chemother. 2011 Dec;55(12):5512-21. | |||||
REF 62 | Dual-targeting properties of the 3-aminopyrrolidyl quinolones, DC-159a and sitafloxacin, against DNA gyrase and topoisomerase IV: contribution to reducing in vitro emergence of quinolone-resistant Streptococcus pneumoniae. J Antimicrob Chemother. 2008 Jul;62(1):98-104. | |||||
REF 63 | Clinical pipeline report, company report or official report of TenNor Therapeutics. | |||||
REF 64 | Clinical pipeline report, company report or official report of Vyome Therapeutics. | |||||
REF 65 | Antistaphylococcal Activity of WCK 771, a Tricyclic Fluoroquinolone, in Animal Infection Models | |||||
REF 66 | The anti-methicillin-resistant Staphylococcus aureus quinolone WCK 771 has potent activity against sequentially selected mutants, has a narrow mutant selection window against quinolone-resistant Staphylococcus aureus, and preferentially targets DNA gyrase.Antimicrob Agents Chemother.2006 Nov;50(11):3568-79. | |||||
REF 67 | Mechanisms and frequency of resistance to temafloxacin. Am J Med. 1991 Dec 30;91(6A):27S-30S. | |||||
REF 68 | Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41. | |||||
REF 69 | Binding of ciprofloxacin labelled with technetium Tc 99m versus 99mTc-pertechnetate to a live and killed equine isolate of Escherichia coli. Can J Vet Res. 2005 October; 69(4): 272-277. | |||||
REF 70 | Efficacy of ABT-719, a 2-pyridone antimicrobial, against enterococci, Escherichia coli, and Pseudomonas aeruginosa in experimental murine pyeloneph... J Antimicrob Chemother. 1996 Oct;38(4):641-53. | |||||
REF 71 | Bay Y 3118, a new quinolone derivative, rapidly eradicates Listeria monocytogenes from infected mice and L929 cells. | |||||
REF 72 | Hydrophilicity of quinolones is not an exclusive factor for decreased activity in efflux-mediated resistant mutants of Staphylococcus aureus. Antimicrob Agents Chemother. 1996 Aug;40(8):1835-42. | |||||
REF 73 | Fluoroquinolone resistance in Mycoplasma gallisepticum: DNA gyrase as primary target of enrofloxacin and impact of mutations in topoisomerases on r... J Antimicrob Chemother. 2002 Oct;50(4):589-92. | |||||
REF 74 | Pharmacokinetics and penetration of danofloxacin from the blood into the milk of cows. J Vet Pharmacol Ther. 1998 Jun;21(3):209-13. | |||||
REF 75 | DX-619, a novel des-fluoro(6) quinolone manifesting low frequency of selection of resistant Staphylococcus aureus mutants: quinolone resistance beyond modification of type II topoisomerases. Antimicrob Agents Chemother. 2005 Dec;49(12):5051-7. | |||||
REF 76 | Mode of action of the dual-action cephalosporin Ro 23-9424. Antimicrob Agents Chemother. 1989 Jul;33(7):1067-71. | |||||
REF 77 | Optimization of pyrrolamide topoisomerase II inhibitors toward identification of an antibacterial clinical candidate (AZD5099). J Med Chem. 2014 Jul 24;57(14):6060-82. | |||||
REF 78 | Antimicrobial activity of DV-7751a, a new fluoroquinolone. | |||||
REF 79 | Company report (gsk) | |||||
REF 80 | Selenophene-containing inhibitors of type IIA bacterial topoisomerases.J Med Chem.2011 May 12;54(9):3418-25. | |||||
REF 81 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001978) | |||||
REF 82 | Relationships among antibacterial activity, inhibition of DNA gyrase, and intracellular accumulation of 11 fluoroquinolones. Antimicrob Agents Chemother. 1992 Dec;36(12):2622-7. | |||||
REF 83 | In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.Antimicrob Agents Chemother.2008 Jul;52(7):2313-23. | |||||
REF 84 | DNA gyrase and topoisomerase IV are dual targets of clinafloxacin action in Streptococcus pneumoniae. Antimicrob Agents Chemother. 1998 Nov;42(11):2810-6. | |||||
REF 85 | Activity of KB-5246 against outer membrane mutants of Escherichia coli and Salmonella typhimurium.. Antimicrob Agents Chemother. 1990 July; 34(7): 1323-1325. | |||||
REF 86 | In vitro antibacterial activities of the fluoroquinolones PD 117596, PD 124816, and PD 127391. Diagn Microbiol Infect Dis. 1991 May-Jun;14(3):245-58. | |||||
REF 87 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007670) | |||||
REF 88 | Engineering the specificity of antibacterial fluoroquinolones: benzenesulfonamide modifications at C-7 of ciprofloxacin change its primary target i... Antimicrob Agents Chemother. 2000 Feb;44(2):320-5. | |||||
REF 89 | 1-Substituted 7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8- difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids.New quantitative structure-activity relationships at N1 for the quinolone antibacterials.J Med Chem.1988 May;31(5):991-1001. |
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