Synthesis, Modeling and Biological Evaluation of Hybrids from Pyrazolo[1,5C]Pyrimidine as Antileishmanial Agents

Atta, Kamal F. M.; Ibrahim, Tamer M.; Farahat, Omaima O.M.; Al-Shargabi, Tareq Q.; Marei, M. G.; Bekhit, Adnan A.; Ashry, El Sayed H. El

doi:10.4155/fmc-2017-0120

Cited by 15 publications

(3 citation statements)

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“…[105] The triazoles, a class of azoles are demonstrated as potential anti-leishmanial drugs. [106,107] Encouraged by these findings, a series of amino acid-coupled 1,2,4-triazoles are engineered as antiprotozoal agents. [108] The synthesized derivatives possessed 3,4-dihydro-1,2,4-triazole ring which has amino and H/methyl functionalities at triazole 3,5-positions respectively.…”

Section: Triazole Scaffoldsmentioning

confidence: 99%

“…The toxicity and severe side effects are reported for the anti‐leishmanial agents such as miltefosine, pentamidine, and paromomycin thereby leading to requirements of the discovery of new drugs with fewer side effects . The triazoles, a class of azoles are demonstrated as potential anti‐leishmanial drugs . Encouraged by these findings, a series of amino acid‐coupled 1,2,4‐triazoles are engineered as antiprotozoal agents .…”

Section: Introductionmentioning

confidence: 99%

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Pharmacology Profile of Recently Developed Multi‐Functional Azoles; SAR‐Based Predictive Structural Modification

Dorababu¹

2020

ChemistrySelect

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Fungal infections have become ubiquitous diseases and their persistent nature and development of drug resistance have led to a global threat. Thereby urgent need to develop efficient antifungal agents is a must. Menace of protozoal diseases cannot be ruled out as the vaccines are not available currently and available anti-protozoal drugs are of low efficacy. Multidrug-resistant tuberculosis is responsible for the inefficient treatment of tuberculosis. Regarding cancer control, the fivemembered heterocyclic compounds such as triazoles and tetrazoles are significant pharmacores that play prominent roles in drug design. In this regard, the research is being carried out in the field of drug design and synthesis considering azole-containing scaffolds as promising target molecules. In this review, the research on azoles having inhibitory properties against various disease causative factors such as fungi, protozoa, bacteria, mycobacteria, etc and various cancer cell lines is described. The whole research is classified on the basis of the type of the azole pharmacore on which the drug molecules are synthesized. The pharmacology of the designed molecules is expressed alongside emphasizing the moieties responsible for the potent activity. Besides, possible structural modification speculating higher biological properties is demonstrated based on SAR.

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Section: Triazole Scaffoldsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Pharmacology Profile of Recently Developed Multi‐Functional Azoles; SAR‐Based Predictive Structural Modification

Dorababu¹

2020

ChemistrySelect

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“…Among the four pyrazolopyrimidine isomers (see Scheme 1), pyrazolo [1,5-c]pyrimidines are the least studied in terms of synthesis, structure or biological activities (Elnagdi et al, 1987). Chemotypes based on pyrazolo [1,5-c]pyrimidines have been shown to possess antileishmanial activity (Atta et al, 2017;Goyal et al, 2021) and antiviral activity against herpesviruses (Gudmundsson et al, 2009). Pyrazolotriazolo-[1,5-c]pyrimidine derivatives have been reported as adenosine receptor antagonists (Federico et al, 2012;Baraldi et al, 2012;Redenti et al, 2016).…”

Section: Introductionmentioning

confidence: 99%

Crystal structure and self-assembly on graphite of a pyrazolo[1,5-c]pyrimidine derivative

Trivedi¹,

Gupta²,

Mishra³

et al. 2021

Acta Crystallogr C

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The crystal structure of the heterocyclic compound 2-(4-methoxyphenyl)-7-phenylpyrazolo[1,5-c]pyrimidine, C19H15N3O, has been determined and its self-assembly on the surface of graphite has been examined using atomic force microscopy (AFM). The title compound crystallized in the monoclinic space group P21/c, with two independent molecules in the asymmetric unit. The packing of the L-shaped molecules in the crystal is governed by arene interactions, in the absence of any conventional hydrogen-bonding interactions. The packing arrangement reveals four types of dimeric motifs stabilized by π–π and C—H...π interactions. At low coverage, molecules assemble into long needle-like islands on the graphite surface. High-resolution AFM images reveal that the molecules interact through weak noncovalent interactions between the aromatic H atoms and the methoxy O atoms.

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Modern Drug Discovery and Development in the Area of Leishmaniasis

Goyal

Patel

Batra

2021

Drug Discovery and Drug Development

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Synthesis, Modeling and Biological Evaluation of Hybrids from Pyrazolo[1,5C]Pyrimidine as Antileishmanial Agents

Abstract: This study provides novel chemotype class for antileishmanial activity. [Formula: see text].

Cited by 15 publications

References 46 publications

Pharmacology Profile of Recently Developed Multi‐Functional Azoles; SAR‐Based Predictive Structural Modification

Pharmacology Profile of Recently Developed Multi‐Functional Azoles; SAR‐Based Predictive Structural Modification

Crystal structure and self-assembly on graphite of a pyrazolo[1,5-c]pyrimidine derivative

Modern Drug Discovery and Development in the Area of Leishmaniasis

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