Pyrazolo[1,5-a]pyrimidine CRF-1 receptor antagonists

Wustrow, David; Capiris, Thomas; Rubin, R. J.; Knobelsdorf, J.; Akunne, Hyacinth C.; Davis, M. Duff; MacKenzie, Robert G.; Pugsley, Thomas A.; Zoski, Kim; Heffner, Thomas G.; Wise, Lawrence D.

doi:10.1016/s0960-894x(98)00372-2

Cited by 130 publications

(64 citation statements)

References 11 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Besides, pyrazole nucleus comprises an important class in the heterocylic chemistry and it has pronounced pharmacological actions as anxiolytic [14] and anticonvulsant [15][16][17][18] activities. On the other hand much attention has been focused towards pyrazoles as antimicrobial [19 -21], antiviral [22] and anticancer [23] agents of the discovery of the natural pyrazole C-glycoside, pyrazofurin; 4-hydroxy-3-b-D-ribofuranosyl-1H-pyrazole-5-carboxamide.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and antinociceptive-antimicrobial activities of some new amide derivatives of 3,5-di/-and 1,3,5-trimethylpyrazoles

Koçyığıt‐Kaymakcioğlu

Toklu

İkiz

et al. 2008

Journal of Enzyme Inhibition and Medicinal Chemistry

View full text Add to dashboard Cite

Some N-(3,5-di-/1,3,5-trimethylpyrazole-4-yl)-4-substitutedbenzamide derivatives were prepared as possible antiociceptiveantimicrobial agents. New amide derivatives (3-12) were synthesized by reacting 4-amino-3,5-di and 1,3,5-trimethylpyrazoles with 4-substitutedbenzoyl chlorides. Hotplate and tail-immersion tests were used for the determination of the antinociceptive activity. Morphine, was used as a standard test drug. All compounds were administered at a dose of 100 mg/kg ip and some of them had significant antinociceptive activity in both tests. Compound 10 (N-(1,3,5-trimethylpyrazole-4-yl)-4-bromobenzamide), was the most active one in both tests among the compounds. The antinociceptive activity of the compounds 10, 11 (N-(1,3,5-trimethylpyrazole-4-yl)-4-chlorobenzamide), and 12 (N-(1,3,5-trimethylpyrazole-4-yl)-4-fluorobenzamide), started at 30 minutes and continued up to 150 minutes in the hotplate test. Also compounds were tested for their in vitro antimicrobial activity, but exhibited weak antibacterial activity.

show abstract

Section: Introductionmentioning

confidence: 99%

Synthesis and antinociceptive-antimicrobial activities of some new amide derivatives of 3,5-di/-and 1,3,5-trimethylpyrazoles

Koçyığıt‐Kaymakcioğlu

Toklu

İkiz

et al. 2008

Journal of Enzyme Inhibition and Medicinal Chemistry

View full text Add to dashboard Cite

show abstract

“…New series of isoxazolines has been synthesized and has shown moderate antimicrobial activity 59 [70]. Pyrimidine analogues: N-fused analogues of chalcones particularly pyrimidines have received augmented interest due to their plethora of biological actions such as antifungal [71], antibacterial [72], antitumor [73], analgesics [74], anti-inflammatory [75], anti-trichomonal [76], KDR kinase inhibition [77], CRF-1 receptor antagonists [78,79] estrogen receptor ligands, and COX-2 selective inhibition [80]. Sharma et al synthesized a series of quinolinyl chalcones and quinolinyl pyrimidines and screened them against M. tuberculosis and NF-54 strains of P. falciparum among all compounds with 4-amino linkage showed promising activity against NF-54 strains of P. falciparum.…”

Section: Analogues Of Chalcones Pyrazoline Analogues With Various Phamentioning

confidence: 99%

Chalconoid Derived Heterocycles as Potent Bioactive Molecules: A Review

Sapra¹,

Sharma²

2016

Chem Sci J

View full text Add to dashboard Cite

Although chalcones symbolize an important pharmacophore for variety of biological actions, however their analogues are also reported to be equally important for plethora of biological actions. In the present review, a comprehensive study of chalcones derived molecules (like pyrazoles, isoxazoles, pyridine, pyrimidine) their pharmacological actions, mechanism of action, structure activity relationship studies have been described. which includes anti-proliferative, anti-inflammatory, antioxidant, proapoptotic, anti-bacterial and anti-adhesive effects [18]. Analogues of chalcones Pyrazoline analogues with various pharmacological activities:Pyrazole nucleus present in compounds exhibit wide range of biological activity. Introduction of a pyrazole ring in the chalcones between the two aryl rings increase the cytotoxic activity against a series of human cancer cell lines. Dhar et al. [19] synthesized a series of 1-acetyl-3,5-diaryl-4,5-dihydro-(H)-pyrazoles and assayed for in vitro cytotoxicity against PC-3, OVCAR, IMR-32, HEP-2 human cancer cell lines, compound 1 showed broad spectrum cytotoxic activity against all the four cell lines. The activity shown by the compounds conclude that (i) Substitution on phenyl ring showed marked effect on cytotoxic activity, (ii) Presence of electron donating groups on phenyl ring led to enhanced activity whereas electron withdrawing group except NO 2 reduces the cytotoxic activity, (iii) Replacement of phenyl ring with heterocyclic ring also reduces the cytotoxic potential and napthyl ring on both sides are more beneficial for cytotoxic potential Chemical Sciences JournalChem ic a l S cience s J o u rnal

show abstract

“…Pyrazoles and its derivatives are well known for their biological and medicinal, applications, such as antimicrobial [1], antitumor [2], antileukemia [3], antidepressant [4], anticonvulsant [5], antifungal [6] and antitubercular [7]. Pyrazole analogoues can selectively inhibit (cyclooxygenase enzyme) COX-2 [8] they are also expressing anti-inflammatory, analgesic, antihypertensive, antipyretic, sedatives, and antidiabetic activities [9,10].…”

Section: Introductionmentioning

confidence: 99%

Optimized Synthesis of Novel Pyrazole Based Thiazole Derivatives and their Antimicrobial Evaluation

Desai

Bhatt

2016

ILCPA

View full text Add to dashboard Cite

Abstract.A series of nitro pyrazole based thiazole derivatives compounds were synthesized by using solid base catalyst. The process was further optimized by setting up the solvent and catalyst ratio. The structures of these compounds were elucidated by spectral (IR, 1 H NMR, 13 C NMR, mass spectra) analysis. Synthesized compounds were screened for their in vitro antibacterial activity against the representative panel of Gram-positive (Staphylococcus aureus, Streptococcus pyogenes) and Gram-negative (Escherichia coli, Pseudomonas aeruginosa) bacteria. These compounds were tested for their inhibitory action against strains of fungi (Candida albicans, Aspergillus niger, Aspergillus clavatus).

show abstract

Pyrazolo[1,5-a]pyrimidine CRF-1 receptor antagonists

Cited by 130 publications

References 11 publications

Synthesis and antinociceptive-antimicrobial activities of some new amide derivatives of 3,5-di/-and 1,3,5-trimethylpyrazoles

Synthesis and antinociceptive-antimicrobial activities of some new amide derivatives of 3,5-di/-and 1,3,5-trimethylpyrazoles

Chalconoid Derived Heterocycles as Potent Bioactive Molecules: A Review

Optimized Synthesis of Novel Pyrazole Based Thiazole Derivatives and their Antimicrobial Evaluation

Contact Info

Product

Resources

About