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Article: Conformationally Constrained Cinnolinone Nucleoside Analogues as Siderophore Biosynthesis Inhibitors for Tuberculosis.

Dawadi, Surendra / Boshoff, Helena I M / Park, Sae Woong / Schnappinger, Dirk / Aldrich, Courtney C

ACS medicinal chemistry letters

2018 Volume 9, Issue 4, Page(s) 386–391

Abstract: 5'- ...

Abstract	5'-
Language	English
Publishing date	2018-03-16
Publishing country	United States
Document type	Journal Article
ISSN	1948-5875
ISSN	1948-5875
DOI	10.1021/acsmedchemlett.8b00090
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: Synthesis and Analysis of Bacterial Folate Metabolism Intermediates and Antifolates.

Dawadi, Surendra / Kordus, Shannon L / Baughn, Anthony D / Aldrich, Courtney C

Organic letters

2017 Volume 19, Issue 19, Page(s) 5220–5223

Abstract: The mechanism of action of para-aminosalicylic acid (PAS), a drug used to treat drug-resistant tuberculosis (TB), has been confirmed through the first synthesis and biochemical characterization of its active metabolite 7. The synthesis features the ... ...

Abstract	The mechanism of action of para-aminosalicylic acid (PAS), a drug used to treat drug-resistant tuberculosis (TB), has been confirmed through the first synthesis and biochemical characterization of its active metabolite 7. The synthesis features the coupling of N
MeSH term(s)	Aminosalicylic Acid ; Antitubercular Agents ; Drug Resistance, Bacterial ; Folic Acid/chemistry ; Folic Acid Antagonists ; Kinetics ; Molecular Structure ; Mutation ; Mycobacterium tuberculosis
Chemical Substances	Antitubercular Agents ; Folic Acid Antagonists ; Aminosalicylic Acid (5B2658E0N2) ; Folic Acid (935E97BOY8)
Language	English
Publishing date	2017-09-19
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ISSN	1523-7052
ISSN (online)	1523-7052
DOI	10.1021/acs.orglett.7b02487
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article: Trapping Hemiacetals with Phosphono Substituted Palladium π-Allyl Complexes for the Synthesis of Substituted Cyclic Ethers.

Sutivisedsak, Nongnuch / Dawadi, Surendra / Spilling, Christopher D

Tetrahedron letters

2015 Volume 56, Issue 23, Page(s) 3534–3537

Abstract: Oxidation of hydroxy substituted phosphono allylic carbonates gave the aldehyde substituted phosphonates in good yield. Stereospecific palladium (0)-catalyzed cyclization in the presence of methanol or water gave acetal tetrahydrofuran and ... ...

Abstract	Oxidation of hydroxy substituted phosphono allylic carbonates gave the aldehyde substituted phosphonates in good yield. Stereospecific palladium (0)-catalyzed cyclization in the presence of methanol or water gave acetal tetrahydrofuran and tetrahydropyran vinyl phosphonate products derived from hemiacetal trapping. The tetrahydrofuran acetals undergo Lewis acid catalyzed addition of nucleophiles to give diastereoisomeric mixtures of substituted tetrahydrofurans.
Language	English
Publishing date	2015-07-30
Publishing country	England
Document type	Journal Article
ZDB-ID	204287-3
ISSN	1873-3581 ; 0040-4039
ISSN (online)	1873-3581
ISSN	0040-4039
DOI	10.1016/j.tetlet.2015.01.050
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Article ; Online: Mutual potentiation drives synergy between trimethoprim and sulfamethoxazole.

Minato, Yusuke / Dawadi, Surendra / Kordus, Shannon L / Sivanandam, Abiram / Aldrich, Courtney C / Baughn, Anthony D

Nature communications

2018 Volume 9, Issue 1, Page(s) 1003

Abstract: Trimethoprim (TMP)-sulfamethoxazole (SMX) is a widely used synergistic antimicrobial combination to treat a variety of bacterial and certain fungal infections. These drugs act by targeting sequential steps in the biosynthetic pathway for tetrahydrofolate ...

Abstract	Trimethoprim (TMP)-sulfamethoxazole (SMX) is a widely used synergistic antimicrobial combination to treat a variety of bacterial and certain fungal infections. These drugs act by targeting sequential steps in the biosynthetic pathway for tetrahydrofolate (THF), where SMX inhibits production of the THF precursor dihydropteroate, and TMP inhibits conversion of dihydrofolate (DHF) to THF. Consequently, SMX potentiates TMP by limiting de novo DHF production and this mono-potentiation mechanism is the current explanation for their synergistic action. Here, we demonstrate that this model is insufficient to explain the potent synergy of TMP-SMX. Using genetic and biochemical approaches, we characterize a metabolic feedback loop in which THF is critical for production of the folate precursor dihydropterin pyrophosphate (DHPPP). We reveal that TMP potentiates SMX activity through inhibition of DHPPP synthesis. Our study demonstrates that the TMP-SMX synergy is driven by mutual potentiation of the action of each drug on the other.
MeSH term(s)	Drug Synergism ; Escherichia coli ; Feedback, Physiological ; Microbial Sensitivity Tests ; Pterins/metabolism ; Tetrahydrofolates/biosynthesis ; Trimethoprim, Sulfamethoxazole Drug Combination/pharmacology
Chemical Substances	7,8-dihydropterin pyrophosphate ; Pterins ; Tetrahydrofolates ; Trimethoprim, Sulfamethoxazole Drug Combination (8064-90-2)
Language	English
Publishing date	2018-03-08
Publishing country	England
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ISSN	2041-1723
ISSN (online)	2041-1723
DOI	10.1038/s41467-018-03447-x
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: Discovery of potent thrombin inhibitors from a protease-focused DNA-encoded chemical library.

Dawadi, Surendra / Simmons, Nicholas / Miklossy, Gabriella / Bohren, Kurt M / Faver, John C / Ucisik, Melek Nihan / Nyshadham, Pranavanand / Yu, Zhifeng / Matzuk, Martin M

Proceedings of the National Academy of Sciences of the United States of America

2020 Volume 117, Issue 29, Page(s) 16782–16789

Abstract: DNA-encoded chemical libraries are collections of compounds individually coupled to unique DNA tags serving as amplifiable identification barcodes. By bridging split-and-pool combinatorial synthesis with the ligation of unique encoding DNA oligomers, ... ...

Abstract	DNA-encoded chemical libraries are collections of compounds individually coupled to unique DNA tags serving as amplifiable identification barcodes. By bridging split-and-pool combinatorial synthesis with the ligation of unique encoding DNA oligomers, million- to billion-member libraries can be synthesized for use in hundreds of healthcare target screens. Although structural diversity and desirable molecular property ranges generally guide DNA-encoded chemical library design, recent reports have highlighted the utility of focused DNA-encoded chemical libraries that are structurally biased for a class of protein targets. Herein, a protease-focused DNA-encoded chemical library was designed that utilizes chemotypes known to engage conserved catalytic protease residues. The three-cycle library features functional moieties such as guanidine, which interacts strongly with aspartate of the protease catalytic triad, as well as mild electrophiles such as sulfonamide, urea, and carbamate. We developed a DNA-compatible method for guanidinylation of amines and reduction of nitriles. Employing these optimized reactions, we constructed a 9.8-million-membered DNA-encoded chemical library. Affinity selection of the library with thrombin, a common protease, revealed a number of enriched features which ultimately led to the discovery of a 1 nM inhibitor of thrombin. Thus, structurally focused DNA-encoded chemical libraries have tremendous potential to find clinically useful high-affinity hits for the rapid discovery of drugs for targets (e.g., proteases) with essential functions in infectious diseases (e.g., severe acute respiratory syndrome coronavirus 2) and relevant healthcare conditions (e.g., male contraception).
MeSH term(s)	Combinatorial Chemistry Techniques ; DNA/chemistry ; DNA/metabolism ; Drug Discovery ; Gene Library ; Humans ; Protease Inhibitors/chemistry ; Protease Inhibitors/pharmacology ; Small Molecule Libraries/chemistry ; Small Molecule Libraries/pharmacology ; Thrombin/antagonists & inhibitors
Chemical Substances	Protease Inhibitors ; Small Molecule Libraries ; DNA (9007-49-2) ; Thrombin (EC 3.4.21.5)
Keywords	covid19
Language	English
Publishing date	2020-07-08
Publishing country	United States
Document type	Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
ZDB-ID	209104-5
ISSN	1091-6490 ; 0027-8424
ISSN (online)	1091-6490
ISSN	0027-8424
DOI	10.1073/pnas.2005447117
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Zs.A 1148: Show issues

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Jg. 1995 - 2021: Lesesall (1.OG)
ab Jg. 2022: Lesesaal (EG)

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Article: Synthesis and Analysis of Bacterial Folate Metabolism Intermediates and Antifolates

Dawadi, Surendra / Kordus Shannon L / Baughn Anthony D / Aldrich Courtney C

Organic letters. 2017 Oct. 06, v. 19, no. 19

2017

Abstract	The mechanism of action of para-aminosalicylic acid (PAS), a drug used to treat drug-resistant tuberculosis (TB), has been confirmed through the first synthesis and biochemical characterization of its active metabolite 7. The synthesis features the coupling of NÂ²-acetyl-6-formylpterin obtained from the degradation of folic acid and appropriately functionalized arylamines to form Schiff bases. The sequential chemoselective reduction of the imine and pterin ring led to the formation of dihydrofolate analogue 7 and two other dihydropteroate species.
Keywords	chemical reactions ; chemical structure ; chemoselectivity ; drug resistance ; drugs ; folic acid ; imines ; mechanism of action ; metabolites ; schiff bases ; tuberculosis ; vitamin metabolism
Language	English
Dates of publication	2017-1006
Size	p. 5220-5223.
Publishing place	American Chemical Society
Document type	Article
ISSN	1523-7052
DOI	10.1021%2Facs.orglett.7b02487
Database	NAL-Catalogue (AGRICOLA)

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Article ; Online: Avoiding Antibiotic Inactivation in Mycobacterium tuberculosis by Rv3406 through Strategic Nucleoside Modification.

Bockman, Matthew R / Engelhart, Curtis A / Dawadi, Surendra / Larson, Peter / Tiwari, Divya / Ferguson, David M / Schnappinger, Dirk / Aldrich, Courtney C

ACS infectious diseases

2018 Volume 4, Issue 7, Page(s) 1102–1113

Abstract: 5'-[ N-(d-biotinoyl)sulfamoyl]amino-5'-deoxyadenosine (Bio-AMS, 1) possesses selective activity against Mycobacterium tuberculosis ( Mtb) and arrests fatty acid and lipid biosynthesis through inhibition of the Mycobacterium tuberculosis biotin protein ... ...

Abstract	5'-[ N-(d-biotinoyl)sulfamoyl]amino-5'-deoxyadenosine (Bio-AMS, 1) possesses selective activity against Mycobacterium tuberculosis ( Mtb) and arrests fatty acid and lipid biosynthesis through inhibition of the Mycobacterium tuberculosis biotin protein ligase ( MtBPL). Mtb develops spontaneous resistance to 1 with a frequency of at least 1 × 10
MeSH term(s)	Antitubercular Agents/chemistry ; Antitubercular Agents/pharmacology ; Carbon-Nitrogen Ligases/metabolism ; Drug Resistance, Bacterial ; Microbial Sensitivity Tests ; Molecular Structure ; Mycobacterium tuberculosis/drug effects ; Mycobacterium tuberculosis/enzymology ; Nucleosides/chemistry ; Nucleosides/metabolism ; Structure-Activity Relationship ; Substrate Specificity
Chemical Substances	Antitubercular Agents ; Nucleosides ; Carbon-Nitrogen Ligases (EC 6.3.-)
Language	English
Publishing date	2018-04-17
Publishing country	United States
Document type	Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
ISSN	2373-8227
ISSN (online)	2373-8227
DOI	10.1021/acsinfecdis.8b00038
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article: Trapping hemiacetals with phosphono substituted palladium Ï-allyl complexes for the synthesis of substituted cyclic ethers

Sutivisedsak, Nongnuch / Surendra Dawadi / Christopher D. Spilling

Tetrahedron letters. 2015 June 03, v. 56

2015

Abstract	Oxidation of hydroxy substituted phosphono allylic carbonates gave the aldehyde substituted phosphonates in good yield. Stereospecific palladium (0)-catalyzed cyclization in the presence of methanol or water gave acetal tetrahydrofuran and tetrahydropyran vinyl phosphonate products derived from hemiacetal trapping. The tetrahydrofuran acetals undergo Lewis acid catalyzed addition of nucleophiles to give diastereoisomeric mixtures of substituted tetrahydrofurans.
Keywords	Lewis acids ; Lewis bases ; aldehydes ; carbonates ; chemical structure ; methanol ; oxidation ; palladium ; phosphonates ; tetrahydrofuran
Language	English
Dates of publication	2015-0603
Size	p. 3534-3537.
Publishing place	Elsevier Ltd
Document type	Article
ZDB-ID	204287-3
ISSN	1873-3581 ; 0040-4039
ISSN (online)	1873-3581
ISSN	0040-4039
DOI	10.1016/j.tetlet.2015.01.050
Database	NAL-Catalogue (AGRICOLA)

In stock of ZB MED Cologne/Königswinter

Zs.A 2837: Show issues

Location:
Je nach Verfügbarkeit (siehe Angabe bei Bestand)
bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
Jg. 1995 - 2021: Lesesall (2.OG)
ab Jg. 2022: Lesesaal (EG)

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Article ; Online: Mutual potentiation drives synergy between trimethoprim and sulfamethoxazole

Yusuke Minato / Surendra Dawadi / Shannon L. Kordus / Abiram Sivanandam / Courtney C. Aldrich / Anthony D. Baughn

Nature Communications, Vol 9, Iss 1, Pp 1-

2018 Volume 7

Abstract: The antibiotics trimethoprim (TMP) and sulfamethoxazole (SMX) synergistically inhibit bacterial tetrahydrofolate biosynthesis, apparently because SMX potentiates TMP activity. Here, Minato et al. identify a metabolic feedback loop in this pathway, ... ...

Abstract	The antibiotics trimethoprim (TMP) and sulfamethoxazole (SMX) synergistically inhibit bacterial tetrahydrofolate biosynthesis, apparently because SMX potentiates TMP activity. Here, Minato et al. identify a metabolic feedback loop in this pathway, revealing that TMP also potentiates SMX activity.
Keywords	Science ; Q
Language	English
Publishing date	2018-03-01T00:00:00Z
Publisher	Nature Publishing Group
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Mutual potentiation drives synergy between trimethoprim and sulfamethoxazole

Yusuke Minato / Surendra Dawadi / Shannon L. Kordus / Abiram Sivanandam / Courtney C. Aldrich / Anthony D. Baughn

Nature Communications, Vol 9, Iss 1, Pp 1-

2018 Volume 7

Abstract	The antibiotics trimethoprim (TMP) and sulfamethoxazole (SMX) synergistically inhibit bacterial tetrahydrofolate biosynthesis, apparently because SMX potentiates TMP activity. Here, Minato et al. identify a metabolic feedback loop in this pathway, revealing that TMP also potentiates SMX activity.
Keywords	Science ; Q
Language	English
Publishing date	2018-03-01T00:00:00Z
Publisher	Nature Portfolio
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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