Design and synthesis of novel lactam/thiazole derivatives having five membered thiazolyl ring and their antimicrobial activity

N.A.

Makale detayları

Design and synthesis of novel lactam/thiazole derivatives having five membered thiazolyl ring and their antimicrobial activity

Yazarlar:

N.A.

Yayıncı:

Marmara University

Ana Başlıklar:

Pharmacology and Pharmaceutical Sciences (Other)

Dergi:

Journal of Research in Pharmacy Vol.27 Issue 1, pp.251-263

Belge Tipi:

Makale

Yayın Tarihi:

6/2025

Belge Dili:

İngilizce

Document ID (Org No.):

2001345956

pISSN:

2630-6344

Anahtar kelimeler:

Özet:

 In the present communication, we conceived a new synthetic approach for the preparation of novel thiazolyl-lactamthiazole analogs. The reaction was started through cyclization of ketone with thiourea along with substituted aryl aldehydes to culminate imine derivatives which subsequently cyclized with thioglycolic acidchloroacetyl chloride to produce final compounds. The structural elucidation of newly synthesized compounds was performed through elemental detections, FT-IR, 1HNMR, and Mass spectrometric techniques. Antimicrobial studies were performed for all synthesized molecules by serial dilution method by tacking the positive K. pneumonia, S. aureus, B. subtills and negative P. aeruginosa and E. coli. bacterial strains. The in vitro antimicrobial screening results show that the compounds 2e, 3c, and 3d containing o-hydroxy, p-chloro, and p-nitro substituent respectively exhibit exceptional activity against S. aureus while compounds 2d and 3f bearing p-nitro and o-chloro substituent respectively were deemed to be the most competent against B. subtilis. Compounds 2d p-nitro and 2f o-chloro were found to be most potent against E. coli. In gram-negative bacterial strains, compounds 2c p-chloro, 2g 4-OH,-OCH3, 3b p-hydroxy, and 3e o-hydroxy were extremely potent against P. aeruginosa while compound 2e containing o-hydroxy group shows excellent activity against E.coli.

 In the present communication, we conceived a new synthetic approach for the preparation of novel thiazolyl-lactamthiazole analogs. The reaction was started through cyclization of ketone with thiourea along with substituted aryl aldehydes to culminate imine derivatives which subsequently cyclized with thioglycolic acidchloroacetyl chloride to produce final compounds. The structural elucidation of newly synthesized compounds was performed through elemental detections, FT-IR, 1HNMR, and Mass spectrometric techniques. Antimicrobial studies were performed for all synthesized molecules by serial dilution method by tacking the positive K. pneumonia, S. aureus, B. subtills and negative P. aeruginosa and E. coli. bacterial strains. The in vitro antimicrobial screening results show that the compounds 2e, 3c, and 3d containing o-hydroxy, p-chloro, and p-nitro substituent respectively exhibit exceptional activity against S. aureus while compounds 2d and 3f bearing p-nitro and o-chloro substituent respectively were deemed to be the most competent against B. subtilis. Compounds 2d p-nitro and 2f o-chloro were found to be most potent against E. coli. In gram-negative bacterial strains, compounds 2c p-chloro, 2g 4-OH,-OCH3, 3b p-hydroxy, and 3e o-hydroxy were extremely potent against P. aeruginosa while compound 2e containing o-hydroxy group shows excellent activity against E.coli.

 In the present communication, we conceived a new synthetic approach for the preparation of novel thiazolyl-lactamthiazole analogs. The reaction was started through cyclization of ketone with thiourea along with substituted aryl aldehydes to culminate imine derivatives which subsequently cyclized with thioglycolic acidchloroacetyl chloride to produce final compounds. The structural elucidation of newly synthesized compounds was performed through elemental detections, FT-IR, 1HNMR, and Mass spectrometric techniques. Antimicrobial studies were performed for all synthesized molecules by serial dilution method by tacking the positive K. pneumonia, S. aureus, B. subtills and negative P. aeruginosa and E. coli. bacterial strains. The in vitro antimicrobial screening results show that the compounds 2e, 3c, and 3d containing o-hydroxy, p-chloro, and p-nitro substituent respectively exhibit exceptional activity against S. aureus while compounds 2d and 3f bearing p-nitro and o-chloro substituent respectively were deemed to be the most competent against B. subtilis. Compounds 2d p-nitro and 2f o-chloro were found to be most potent against E. coli. In gram-negative bacterial strains, compounds 2c p-chloro, 2g 4-OH,-OCH3, 3b p-hydroxy, and 3e o-hydroxy were extremely potent against P. aeruginosa while compound 2e containing o-hydroxy group shows excellent activity against E.coli.

 In the present communication, we conceived a new synthetic approach for the preparation of novel thiazolyl-lactamthiazole analogs. The reaction was started through cyclization of ketone with thiourea along with substituted aryl aldehydes to culminate imine derivatives which subsequently cyclized with thioglycolic acidchloroacetyl chloride to produce final compounds. The structural elucidation of newly synthesized compounds was performed through elemental detections, FT-IR, 1HNMR, and Mass spectrometric techniques. Antimicrobial studies were performed for all synthesized molecules by serial dilution method by tacking the positive K. pneumonia, S. aureus, B. subtills and negative P. aeruginosa and E. coli. bacterial strains. The in vitro antimicrobial screening results show that the compounds 2e, 3c, and 3d containing o-hydroxy, p-chloro, and p-nitro substituent respectively exhibit exceptional activity against S. aureus while compounds 2d and 3f bearing p-nitro and o-chloro substituent respectively were deemed to be the most competent against B. subtilis. Compounds 2d p-nitro and 2f o-chloro were found to be most potent against E. coli. In gram-negative bacterial strains, compounds 2c p-chloro, 2g 4-OH,-OCH3, 3b p-hydroxy, and 3e o-hydroxy were extremely potent against P. aeruginosa while compound 2e containing o-hydroxy group shows excellent activity against E.coli.

Makale detayları

Design and synthesis of novel lactam/thiazole derivatives having five membered thiazolyl ring and their antimicrobial activity

Yazarlar:

N.A.

Yayıncı:

Marmara University

Ana Başlıklar:

Pharmacology and Pharmaceutical Sciences (Other)

Dergi:

Journal of Research in Pharmacy Vol.27 Issue 1, pp.251-263

Belge Tipi:

Makale

Yayın Tarihi:

6/2025

Belge Dili:

İngilizce

Document ID (Org No.):

2001345956

pISSN:

2630-6344

Synthesis

Lactam

Thiazolyl ring

Antimicrobial activity

Thiourea

Sayı

Makale detayları

Design and synthesis of novel lactam/thiazole derivatives having five membered thiazolyl ring and their antimicrobial activity

Yazarlar: N.A.

Yayıncı: Marmara University

Ana Başlıklar: Pharmacology and Pharmaceutical Sciences (Other)

Dergi: Journal of Research in Pharmacy Vol.27 Issue 1, pp.251-263

Belge Tipi: Makale

Yayın Tarihi: 6/2025

Belge Dili: İngilizce

Document ID (Org No.): 2001345956

pISSN: 2630-6344

Synthesis

Lactam

Thiazolyl ring

Antimicrobial activity

Thiourea

Sayı

Yazarlar:

N.A.

Yayıncı:

Marmara University

Ana Başlıklar:

Pharmacology and Pharmaceutical Sciences (Other)

Dergi:

Journal of Research in Pharmacy Vol.27 Issue 1, pp.251-263

Belge Tipi:

Makale

Yayın Tarihi:

6/2025

Belge Dili:

İngilizce

Document ID (Org No.):

2001345956

pISSN:

2630-6344